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Artykuły w czasopismach na temat „DPP Derivatives”

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Data publikacji: 6 września 2023

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1

Luo, Nan, Guanxin Zhang i Zitong Liu. "Keep glowing and going: recent progress in diketopyrrolopyrrole synthesis towards organic optoelectronic materials". Organic Chemistry Frontiers 8, nr 16 (2021): 4560–81. http://dx.doi.org/10.1039/d1qo00613d.

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Recent progress in the syntheses of DPP derivatives is summarized as well as the structure–property relationships of the derivatives, including the syntheses of DPP cores, N-functionalization reactions, and π-extensions on and along the DPP cores.

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Leidel, Fabienne, Martin Eiden, Markus Geissen, Hans A. Kretzschmar, Armin Giese, Thomas Hirschberger, Paul Tavan, Hermann M. Schätzl i Martin H. Groschup. "Diphenylpyrazole-Derived Compounds Increase Survival Time of Mice after Prion Infection". Antimicrobial Agents and Chemotherapy 55, nr 10 (11.07.2011): 4774–81. http://dx.doi.org/10.1128/aac.00151-11.

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ABSTRACTTransmissible spongiform encephalopathies (TSEs) represent a group of fatal neurodegenerative disorders that can be transmitted by natural infection or inoculation. TSEs include scrapie in sheep, bovine spongiform encephalopathy (BSE) in cattle, and Creutzfeldt-Jakob disease (CJD) in humans. The emergence of a variant form of CJD (vCJD), which has been associated with BSE, produced strong pressure to search for effective treatments with new drugs. Up to now, however, TSEs have proved incurable, although many efforts have been made bothin vitroandin vivoto search for potent therapeutic and prophylactic compounds. For this purpose, we analyzed a compound library consisting of 10,000 compounds with a cell-based high-throughput screening assay dealing with scrapie-infected scrapie mouse brain and ScN2A cells and identified a new class of inhibitors consisting of 3,5-diphenylpyrazole (DPP) derivatives. The most effective DPP derivative showed half-maximal inhibition of PrPScformation at concentrations (IC50) of 0.6 and 1.2 μM, respectively. This compound was subsequently subjected to a number of animal experiments using scrapie-infected wild-type C57BL/6 and transgenic Tga20 mice. The DPP derivative induced a significant increase of incubation time both in therapeutic and prophylactic experiments. The onset of the prion disease was delayed by 37 days after intraperitoneal and 42 days after oral application, respectively. In summary, we demonstrate a highin vitroefficiency of DPP derivatives against prion infections that was substantiatedin vivofor one of these compounds. These results indicate that the novel class of DPP compounds should comprise excellent candidates for future therapeutic studies.

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3

He, Ran, Michael Forman, Bryan T. Mott, Rajkumar Venkatadri, Gary H. Posner i Ravit Arav-Boger. "Unique and Highly Selective Anticytomegalovirus Activities of Artemisinin-Derived Dimer Diphenyl Phosphate Stem from Combination of Dimer Unit and a Diphenyl Phosphate Moiety". Antimicrobial Agents and Chemotherapy 57, nr 9 (17.06.2013): 4208–14. http://dx.doi.org/10.1128/aac.00893-13.

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ABSTRACTWe report that the artemisinin-derived dimer diphenyl phosphate (DPP; dimer 838) is the most selective inhibitor of human cytomegalovirus (CMV) replication among a series of artemisinin-derived monomers and dimers. Dimer 838 was also unique in being an irreversible CMV inhibitor. The peroxide unit within artemisinins' chemical structures is critical to their activities, and its absence results in loss of anti-CMV activities. Surprisingly, the deoxy dimer of 838 retained modest anti-CMV activity, suggesting that the DPP moiety of dimer 838 contributes to its anti-CMV activities. DPP alone did not inhibit CMV replication, but triphenyl phosphate (TPP) had modest CMV inhibition, although its selectivity index was low. Artemisinin DPP derivatives dimer 838 and monomer diphenyl phosphate (compound 558) showed stronger CMV inhibition and a higher selectivity index than their analogs lacking the DPP unit. An add-on and removal assay revealed that removing DPP derivatives (compounds 558 and 838) but not the non-DPP backbones (artesunate and compound 606) at 24 h postinfection (hpi) already resulted in dominant CMV inhibition. CMV inhibition was fully irreversible with 838 and partially irreversible with 558, while non-DPP artemisinins were reversible inhibitors. While all artemisinin derivatives and TPP reduced the expression of the CMV immediate early 2 (IE2), UL44, and pp65 proteins at or after 48 hpi, only TPP inhibited the expression of both IE1 and IE2. Combination of a non-DPP dimer (compound 606) with TPP was synergistic in CMV inhibition, while ganciclovir and TPP were additive. Although TPP shared structural similarity with monomer DPP (compound 558) and dimer DPP (compound 838), its pattern of CMV inhibition was significantly different from the patterns of the artemisinins. These findings demonstrate that the DPP group contributes to the unique activities of compound 838.

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4

Wang, Yu, Xialian Tang i Lianghong Yi. "Design and Discovery of Novel 1,3,5-Triazines as Dipeptidyl Peptidase-4 Inhibitor against Diabetes". Pharmacology 103, nr 5-6 (2019): 273–81. http://dx.doi.org/10.1159/000494060.

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This study aims at synthesizing novel di-morpholine 1,3,5-triazine derivatives as antidiabetic agent via inhibition of dipeptidyl peptidase-4 (DPP-4). The molecules were developed via sequential nucleophilic reaction to afford target derivatives 5(a–f) and subsequently tested for inhibitory potency against DPP iso-enzymes, such as DPP-4, DPP-8, and DPP-9. The in vitro inhibition assay suggested that these derivatives prominently and selectively inhibit DPP-4 over DPP-8 and DPP-9. These molecules also showed no presence of cardiotoxicity, as confirmed by no activity against human Ether-à-go-go related gene channel. The study disclosed compound 5c as the most potent inhibitor of DPP-4 with IC50 of 1.10 nmol/L as compared to the standard. Compound 5c was further evaluated for oral glucose tolerance test (OGTT) and antidiabetic activity in ICR mice and Wistar rats, respectively. In OGTT, compound 5c showed dose-dependent improvement of glucose tolerance with a maximum at 30 mg/kg. It also showed reduction in area under the curve from 0 to 120 min, similar to alogliptin (standard). In Wistar rats, compound 5c causes reduction in the blood glucose level, total cholesterol, triglyceride, low density lipoprotein (LDL) and very LDL level as compared to the diabetic control group, whereas the level of high-density lipoprotein was found to be increased. Compound 5c causes improvement in antioxidant defense mechanism, as confirmed via improving superoxide dismutase, catalase, glutathione peroxidase and reducing the malondialdehyde level as compared to normal control group rats.

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5

Wang, Bing, Nannan He, Bo Li, Shuangying Jiang, Yi Qu, Sanyin Qu i Jianli Hua. "Aggregation-Induced Emission and Large Two-Photon Absorption Cross-Sections of Diketopyrrolopyrrole (DPP) Derivatives". Australian Journal of Chemistry 65, nr 4 (2012): 387. http://dx.doi.org/10.1071/ch11410.

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In this work, a new series of triphenylamine-based diketo-pyrrolo-pyrrole (DPP) compounds (DPP-I, DPP-II, DPP-III) have been designed and synthesized by a concise route. Their one- and two-photon absorption properties have been investigated. It was found that DPP-based compounds are very weakly fluorescent in THF solution, but their intensities are increased by almost 29, 9, and 24 times in water/THF (v/v 90 %) mixtures, respectively, in which they exhibit a strongly enhanced red fluorescence. The result indicates that the intramolecular vibration and rotation of these dyes is considerably restricted in nano-aggregates formed in water/THF mixtures, which leads to significant increases in fluorescence. The two-photon absorption (2PA) cross-sections measured by the open aperture Z-scan technique were determined to be 188, 275 and 447 GM for DPP-I, DPP-II, and DPP-III, respectively; DPP-III with the symmetrical structure shows the highest value of 2PA cross-section. The excellent properties of aggregation-induced emission (AIE) and 2PA provide an attractive alternative for the biophotonic materials.

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6

Wang, Lingyun, Bihong Lai, Xueguang Ran, Hao Tang i Derong Cao. "Recent Advances of Diketopyrrolopyrrole Derivatives in Cancer Therapy and Imaging Applications". Molecules 28, nr 10 (15.05.2023): 4097. http://dx.doi.org/10.3390/molecules28104097.

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Cancer is threatening the survival of human beings all over the world. Phototherapy (including photothermal therapy (PTT) and photodynamic therapy (PDT)) and bioimaging are important tools for imaging–mediated cancer theranostics. Diketopyrrolopyrrole (DPP) dyes have received more attention due to their high thermal and photochemical stability, efficient reactive oxygen species (ROS) generation and thermal effects, easy functionalization, and tunable photophysical properties. In this review, we outline the latest achievements of DPP derivatives in cancer therapy and imaging over the past three years. DPP-based conjugated polymers and small molecules for detection, bioimaging, PTT, photoacoustic imaging (PAI)-guided PTT, and PDT/PTT combination therapy are summarized. Their design principles and chemical structures are highlighted. The outlook, challenges, and future opportunities for the development of DPP derivatives are also presented, which will give a future perspective for cancer treatment.

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7

Yang, Sheng-Hsiung, i Chia-Hao Hsieh. "Novel Linear and Hyperbranched Polythiophene Derivatives Containing Diketopyrrolopyrroles as Linking Groups". MRS Proceedings 1771 (2015): 213–19. http://dx.doi.org/10.1557/opl.2015.497.

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ABSTRACTThe goal of this research is to synthesize novel linear and hyperbranched polythiophene derivatives containing diketopyrrolopyrrole (DPP) as linking groups, and to investigate thermal, optical, electrochemical, and photovoltaic properties of those derivatives. Polymers with high regioregularity were synthesized via the Universal Grignard metathesis polymerization. Those linear or hyperbranched polythiophenes containing DPP bridging moieties showed higher molecular weights and better thermal stability compared with normal P3HT. The UV-vis absorption spectra of the DPP-containing polymers are similar to that of P3HT in film state, while they show distinct attenuation in fluorescent emission. Finally, all polymers were blended with PC61BM and used as active layers for fabrication of inverted solar devices. The devices based on those DPP-containing polythiophenes revealed the open-circuit voltage (VOC) of 0.55–0.58 V, the short-circuit current (JSC) of 8.62–16.21 mA/cm2, the fill factor (FF) of 36–41%, and the power conversion efficiency (PCE) of 1.73–3.74%.

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8

Santoprete, Alessia, Elena Capitò, Paul E. Carrington, Alessandro Pocai, Marco Finotto, Annunziata Langella, Paolo Ingallinella i in. "DPP-IV-resistant, long-acting oxyntomodulin derivatives". Journal of Peptide Science 17, nr 4 (3.02.2011): 270–80. http://dx.doi.org/10.1002/psc.1328.

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9

Khalaf, Reema A., Dalal Masalha i Dima Sabbah. "DPP-IV Inhibitory Phenanthridines: Ligand, Structure-Based Design and Synthesis". Current Computer-Aided Drug Design 16, nr 3 (2.06.2020): 295–307. http://dx.doi.org/10.2174/1573409915666181211114743.

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Background: Lately, diabetes has become the main health concern for millions of people around the world. Dipeptidyl peptidase-IV (DPP-IV) inhibitors have emerged as a new class of oral antidiabetic agents. Formerly, acridines, N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives, and sulfamoyl-phenyl acid esters were designed and developed as new DPP-IV inhibitors. Objective: This study aims to develop a pharmacophore model of DPP-IV inhibitors and to evaluate phenanthridines as a novel scaffold for inhibiting DPP-IV enzyme. In addition, to assess their binding interactions with the enzyme through docking in the binding site of 4A5S (PDB). Methods: Herein, Quantum–Polarized Ligand Docking (QPLD) and ligand-based pharmacophore modeling investigations were performed. Three novel 3,8-disubstituted-6-phenyl phenanthridine derivatives 3-5 have been designed, synthesized and characterized. In vitro biological testing against DPP-IV was carried out using fluorometric assay kit. Results: QPLD study demonstrates that compounds 3-5 forms H-bond with Lys554, Trp629, and Tyr631, besides charge transfer interaction between their aromatic rings and the aromatic rings of Tyr547 and Tyr666. Moreover, they fit the three pharmacophoric point features of DPP-IV inhibitors and were proven to have in vitro DPP-IV inhibitory activity where compound 5 displayed a % inhibition of 45.4 at 100 μM concentration. Conclusion: Phenanthridines may serve as a potential lead compound for developing new DPP-IV inhibitors as a promising antidiabetic agent. Computational results suggest future structural simplification.

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10

Ivanova, E. A., N. N. Zolotov, V. F. Pozdnev i T. A. Voronina. "Effect of cyanopyrrolidine derivatives on the activity of prolylendopeptidase, acute exudative inflammation and visceral pain in mice". Biomeditsinskaya Khimiya 66, nr 1 (styczeń 2020): 77–82. http://dx.doi.org/10.18097/pbmc20206601077.

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Cyanopyrrolidine derivatives benzyloxycarbonyl-methionyl-cyanopyrrolidine (ZMetPrdN), benzyloxycarbonylphenylalanyl- cyanopyrrolidine (ZPhePrdN), tert-butyl-hydroxycarbonyl-glycyl-cyanopyrrolidine (BocGlyPrdN), tert-butyl-hydroxycarbonyl-methionyl-cyanopyrrolidine (BocMetPrdN) are inhibitors of prolylendopeptidase (PREP; EC 3.4.21.26) with an IC50 of 2 nM to 12 nM. ZMetPrdN, ZPhePrdN and BocMetPrdN additionally inhibited dipeptidyl peptidase IV (DPP-4; EC 3.4.14.5) with an IC50 of 1100 nM to 3200 nM. All the compounds have antinociceptive properties in the acetic acid writhing test in mice. But only cyanopyrrolidine derivatives with aromatic substituents decrease exudative inflammation. The cyanopyrrolidine derivatives also increase PREP activity and compensatorily reduce DPP-4 activity in the serum of mice three hours after the induction of inflammation. Thus, cyanopyrrolidine derivatives exhibit antinociceptive and antiexudative properties in part via their effect on PREP.

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11

Stas, Sara, Sergey Sergeyev i Yves Geerts. "Synthesis of diketopyrrolopyrrole (DPP) derivatives comprising bithiophene moieties". Tetrahedron 66, nr 10 (marzec 2010): 1837–45. http://dx.doi.org/10.1016/j.tet.2010.01.027.

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12

Sharma, Lisa, i Hugo Bronstein. "Synthesis of fully asymmetric diketopyrrolopyrrole derivatives". RSC Advances 11, nr 9 (2021): 5276–83. http://dx.doi.org/10.1039/d0ra01564d.

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Diaryl-diketopyrrolopyrroles (DPP) are a widely studied class of chromophore that possesses unique properties which have been of great interest for use in conjugated polymers and as small molecules in optoelectronic devices.

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13

Fujii, Mikiya, Woong Shin, Takuma Yasuda i Koichi Yamashita. "Photon-absorbing charge-bridging states in organic bulk heterojunctions consisting of diketopyrrolopyrrole derivatives and PCBM". Physical Chemistry Chemical Physics 18, nr 14 (2016): 9514–23. http://dx.doi.org/10.1039/c5cp06183k.

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14

Ying, Shian, Mingshuai Chen, Zhongwei Liu, Kai Zhang, Yuyu Pan, Shanfeng Xue i Wenjun Yang. "9-Anthryl-capped DPP-based dyes: aryl spacing induced differential optical properties". Journal of Materials Chemistry C 4, nr 34 (2016): 8006–13. http://dx.doi.org/10.1039/c6tc02761j.

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15

Li, Qing, Li Han, Bin Zhang, Jinpei Zhou i Huibin Zhang. "Synthesis and biological evaluation of triazole based uracil derivatives as novel DPP-4 inhibitors". Organic & Biomolecular Chemistry 14, nr 40 (2016): 9598–611. http://dx.doi.org/10.1039/c6ob01818a.

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16

Musoev, Numonov, You i Gao. "Discovery of Novel DPP-IV Inhibitors as Potential Candidates for the Treatment of Type 2 Diabetes mellitus Predicted by 3D QSAR Pharmacophore Models, Molecular Docking and de novo Evolution". Molecules 24, nr 16 (7.08.2019): 2870. http://dx.doi.org/10.3390/molecules24162870.

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Dipeptidyl peptidase-IV (DPP-IV) rapidly breaks down the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Thus, the use of DPP-IV inhibitors to retard the degradation of endogenous GLP-1 is a possible mode of therapy correcting the defect in incretin-related physiology. The aim of this study is to find a new small molecule and explore the inhibition activity to the DPP-IV enzyme using a computer aided simulation. In this study, the predicted compounds were suggested as potent anti-diabetic candidates. Chosen structures were applied following computational strategies: The generation of the three-dimensional quantitative structure-activity relationship (3D QSAR) pharmacophore models, virtual screening, molecular docking, and de novo Evolution. The method also validated by performing re-docking and cross-docking studies of seven protein systems for which crystal structures were available for all bound ligands. The molecular docking experiments of predicted compounds within the binding pocket of DPP-IV were conducted. By using 25 training set inhibitors, ten pharmacophore models were generated, among which hypo1 was the best pharmacophore model with the best predictive power on account of the highest cost difference (352.03), the lowest root mean squared deviation (RMSD) (2.234), and the best correlation coefficient (0.925). Hypo1 pharmacophore model was used for virtual screening. A total of 161 compounds including 120 from the databases, 25 from the training set, 16 from the test set were selected for molecular docking. Analyzing the amino acid residues of the ligand-receptor interaction, it can be concluded that Arg125, Glu205, Glu206, Tyr547, Tyr662, and Tyr666 are the main amino acid residues. The last step in this study was de novo Evolution that generated 11 novel compounds. The derivative dpp4_45_Evo_1 by all scores CDOCKER_ENERGY (CDOCKER, -41.79), LigScore1 (LScore1, 5.86), LigScore2 (LScore2, 7.07), PLP1 (-112.01), PLP2 (-105.77), PMF (-162.5)—have exceeded the control compound. Thus the most active compound among 11 derivative compounds is dpp4_45_Evo_1. Additionally, for derivatives dpp4_42_Evo_1, dpp4_43_Evo2, dpp4_46_Evo_4, and dpp4_47_Evo_2, significant upward shifts were recorded. The consensus score for the derivatives of dpp4_45_Evo_1 from 1 to 6, dpp4_43_Evo2 from 4 to 6, dpp4_46_Evo_4 from 1 to 6, and dpp4_47_Evo_2 from 0 to 6 were increased. Generally, predicted candidates can act as potent occurring DPP-IV inhibitors given their ability to bind directly to the active sites of DPP-IV. Our result described that the 6 re-docked and 27 cross-docked protein-ligand complexes showed RMSD values of less than 2 Å. Further investigation will result in the development of novel and potential antidiabetic drugs.

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17

Bidan, G., B. Divisia-Blohorn, M. Billon, J. M. Kern i J. P. Sauvage. "Tangled 3-functionalized polypyrrole derivatives built around Cu(dpp)2+ (dpp = 2,9-diphenyl-1,10-phenanthroline)". Journal of Electroanalytical Chemistry 360, nr 1-2 (listopad 1993): 189–98. http://dx.doi.org/10.1016/0022-0728(93)87012-k.

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18

Patil, S., i R. Sharma. "INSIGHT INTO AMINOMETHYL-PIPERIDONES BASED DPP-IV INHIBITORS FOR TREATMENT OF DIABETES: AN APPLICATION OF RATIONAL DRUG DESIGN". INDIAN DRUGS 54, nr 04 (28.04.2017): 5–21. http://dx.doi.org/10.53879/id.54.04.10808.

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DPP IV is an important biological target for treatment of diabetes. The CoMFA, CoMSIA and HQSAR models have been developed on thirty two aminomethyl piperidones derivatives. The data set consisting of twenty one training set compounds and eleven test set compounds that showed good statistical significance with internal cross validation (q2) 0.849, 0.790 and 0.901, non-cross validation (r2) 0.863, 0.793 and 0.903 and predicted (pred. r2) 0.845, 0.822 and 0.901 for CoMFA, CoMSIA and HQSAR, respectively for anti-diabetic activity. The docking study explored with active site of DPP IV, in particular, the contribution of the –NH, 2,5 di-F (Ar) with Asn 151, Asn 169 and Asn 170 of the compound 22, respectively, which is important for the bioactive conformation for DPP IV inhibition. The QSAR models, contour maps, and docking binding affinity obtained could be successfully utilized as a guiding tool for design and discovery of novel derivatives.

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19

Kalli, Swarna Bharathi, i V. Velmurugan. "Design, synthesis and anti-diabetic activity of piperazine sulphonamide derivatives as dipeptidyl peptidase-4 inhibitors". Pharmacia 69, nr 4 (11.11.2022): 987–93. http://dx.doi.org/10.3897/pharmacia.69.e95096.

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Type II diabetes (T2DM) is considered one of the most prevalent metabolic disorders in the world. It is known as insulin resistance and persistent hyperglycemia. Over the past decade, inhibition of the enzymatic dipeptidyl peptidase-4 (DPP-4) has indeed been demonstrated to be an efficient and safe intervention for type 2 diabetes. In order to develop innovative DPP-4 inhibitors, several in silico techniques including 3D-QSAR, molecular docking, in-silico toxicity has been performed to confirm a total of 18 novel piperazine and pyridine derivatives to be synthesized from many designed molecules. These molecules have indeed been docked onto the protein surface of the DPP-4 enzyme, and ADMET characteristics have also been generated in silico. The compounds were then developed and analysed using FT-IR. Then, these compounds were investigated for DPP-4 inhibition in vitro. The most promising compound 8h showed 27.32% inhibition at 10μmol L-1 concentration over DPP-4 so selected for further in-vivo anti-diabetic evaluation. Compound 8h decreased blood glucose excursion in a dose-dependent manner during the OGTT and STZ-induced glucose models in normal Albino Wistar rats. Low-dose streptozotocin-induced type 2 diabetes in Albino Wistar rats treated chronically for 21 days with compound 8h resulted in a reduction in serum glucose levels. This highlighted that 8h is a moderately strong and specific blockbuster molecule that can be structurally modified to boost its effectiveness and overall pharmacological profile as a DPP-4 inhibitor.

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Abramić, Marija, i Dejan Agić. "Survey of Dipeptidyl Peptidase III Inhibitors: From Small Molecules of Microbial or Synthetic Origin to Aprotinin". Molecules 27, nr 9 (7.05.2022): 3006. http://dx.doi.org/10.3390/molecules27093006.

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Dipeptidyl peptidase III (DPP III) was originally thought to be a housekeeping enzyme that contributes to intracellular peptide catabolism. More specific roles for this cytosolic metallopeptidase, in the renin-angiotensin system and oxidative stress regulation, were confirmed, or recognized, only recently. To prove indicated (patho)physiological functions of DPP III in cancer progression, cataract formation and endogenous pain modulation, or to reveal new ones, selective and potent inhibitors are needed. This review encompasses natural and synthetic compounds with experimentally proven inhibitory activity toward mammalian DPP III. Except for the polypeptide aprotinin, all others are small molecules and include flavonoids, coumarin and benzimidazole derivatives. Presented are current strategies for the discovery or development of DPP III inhibitors, and mechanisms of inhibitory actions. The most potent inhibitors yet reported (propioxatin A and B, Tyr-Phe- and Phe-Phe-NHOH, and JMV-390) are active in low nanomolar range and contain hydroxamic acid moiety. High inhibitory potential possesses oligopeptides from the hemorphin group, valorphin and tynorphin, which are poor substrates of DPP III. The crystal structure of human DPP III-tynorphin complex enabled the design of the transition-state peptidomimetics inhibitors, effective in low micromolar concentrations. A new direction in the field is the development of fluorescent inhibitor for monitoring DPP III activity.

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Khalaf, Reema Abu, Ghassan Abu Sheikha, Mahmoud Al-Sha'er i Mutasem Taha. "Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors". Open Medicinal Chemistry Journal 7, nr 1 (29.11.2013): 39–48. http://dx.doi.org/10.2174/1874104501307010039.

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As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.

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22

Wang, Xiaohua, Bin Jiang, Chenchen Du, Xiaolei Ren, Zhiming Duan i Hongyu Wang. "Fluorinated dithienyl-diketopyrrolopyrrole: a new building block for organic optoelectronic materials". New Journal of Chemistry 43, nr 41 (2019): 16411–20. http://dx.doi.org/10.1039/c9nj04060a.

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The synthesis of monofluorinated and difluorinated dithienyl-DPP was reported using a stepwise synthesis method starting from the preparation of pyrrolinone followed by condensation with methyl thiophene-2-carbimidate derivatives.

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23

Sunil, Sreeja, Arul G. D. A. Smith i Mathan S. "Design, Synthesis and Biological Evaluation of 2-Aminobenzimidazole Derivatives as DPP4 Inhibitors". Current Bioactive Compounds 16, nr 5 (16.07.2020): 696–702. http://dx.doi.org/10.2174/1573407215666190318121902.

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Background: The objective of the research was to examine the DPPIV inhibitor activity of synthetic derivatives of 2-aminobenzimidazole derivatives by the in-vivo method. Methods: Molecular docking was performed using homology model of receptors to identify the binding sites for the inhibitory activity of diabetes by means of- CDocker energy using the Discovery Studio (DS) 4.5 Novel 2-amino benzimidazole derivatives were synthesized from orthophenylene diamine with cyanogens bromide. The synthesized compounds were identified by IR,1HNMR,13CNMR, and MASS spectroscopic techniques. The products were analyzed for their DPPIV inhibitory effects on Wistar Albino rat. Results: The results revealed that benzimidazole with para-aminobenzoic acid possesses best DPPIV inhibitor activity. 2- amino benzimidazole incorporated with aromatic compounds were synthesized and assessed for their DPP-IV inhibitor activity. Conclusion: 2- amino benzimidazole with para-aminobenzoic acid can be used as a lead compound for the development of a new class of DPP-IV inhibitor.

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Vawhal, Pallavi Kishor, Shailaja B. Jadhav, Sumit Kaushik, Kahnu Charan Panigrahi, Chandan Nayak, Humaira Urmee, Sharuk L. Khan i in. "Coumarin-Based Sulfonamide Derivatives as Potential DPP-IV Inhibitors: Pre-ADME Analysis, Toxicity Profile, Computational Analysis, and In Vitro Enzyme Assay". Molecules 28, nr 3 (19.01.2023): 1004. http://dx.doi.org/10.3390/molecules28031004.

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Recent research on dipeptidyl peptidase-IV (DPP-IV) inhibitors has made it feasible to treat type 2 diabetes mellitus (T2DM) with minimal side effects. Therefore, in the present investigation, we aimed to discover and develop some coumarin-based sulphonamides as potential DPP-IV inhibitors in light of the fact that molecular hybridization of many bioactive pharmacophores frequently results in synergistic activity. Each of the proposed derivatives was subjected to an in silico virtual screening, and those that met all of the criteria and had a higher binding affinity with the DPP-IV enzyme were then subjected to wet lab synthesis, followed by an in vitro biological evaluation. The results of the pre-ADME and pre-tox predictions indicated that compounds 6e, 6f, 6h, and 6m to 6q were inferior and violated the most drug-like criteria. It was observed that 6a, 6b, 6c, 6d, 6i, 6j, 6r, 6s, and 6t displayed less binding free energy (PDB ID: 5Y7H) than the reference inhibitor and demonstrated drug-likeness properties, hence being selected for wet lab synthesis and the structures being confirmed by spectral analysis. In the in vitro enzyme assay, the standard drug Sitagliptin had an IC50 of 0.018 µM in the experiment which is the most potent. All the tested compounds also displayed significant inhibition of the DPP-IV enzyme, but 6i and 6j demonstrated 10.98 and 10.14 µM IC50 values, respectively, i.e., the most potent among the synthesized compounds. Based on our findings, we concluded that coumarin-based sulphonamide derivatives have significant DPP-IV binding ability and exhibit optimal enzyme inhibition in an in vitro enzyme assay.

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Syam, Yasmin M., Somaia S. Abd El-Karim, Tamer Nasr, Samia A. Elseginy, Manal M. Anwar, Mohsen M. Kamel i Hanan F. Ali. "Design, Synthesis and Biological Evaluation of Spiro Cyclohexane-1,2- Quinazoline Derivatives as Potent Dipeptidyl Peptidase IV Inhibitors". Mini-Reviews in Medicinal Chemistry 19, nr 3 (11.01.2019): 250–69. http://dx.doi.org/10.2174/1389557517666170828121018.

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Objective: Inhibition of dipeptidyl peptidase IV (DPP-4) is currently one of the most valuable and potential chemotherapeutic regimes for the medication of Type 2 Diabetes Mellitus (T2DM). Method: Based on linagliptin, this study discusses the design, synthesis and biological evaluation of spiro cyclohexane-1,2'-quinazoline scaffold hybridized with various heterocyclic ring systems through different atomic spacers as a highly potent DPP-4 inhibitors. DPP-4 enzyme assay represented that most of the target compounds are 102-103 folds more active than the reference drug linagliptin (IC50: 0.0005-0.0089 nM vs 0.77 nM; respectively). Moreover, in vivo oral hypoglycemic activity assay revealed that most of the tested candidates were more potent than the reference drug, sitagliptin, producing rapid onset with long duration of activity that extends to 24 h. Interestingly, the derivatives 11, 16, 18a and 23 showed evidence of mild cytochrome P450 3A4 (CYP3A4) inhibition (IC50; > 210 µM) and their acute toxicity (LD50) was more than 1.9 gm/kg. Molecular simulation study of the new quinazoline derivatives explained the obtained biological results. Conclusion: Finally, we conclude that our target compounds could be highly beneficial for diabetic patients in the clinic.

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26

Khalaf, Reema Abu, Ebtisam Alwarafi i Dima Sabbah. "Piperazine sulfonamides as DPP-IV inhibitors: Synthesis, induced-fit docking and in vitro biological evaluation". Acta Pharmaceutica 71, nr 4 (3.04.2021): 631–43. http://dx.doi.org/10.2478/acph-2021-0034.

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Abstract Diabetes mellitus is a chronic illness that needs persistent medical attention and continuous patient self-management to avoid acute complications. Dipeptidyl peptidase-IV (DPP-IV) inhibitors minimize glucagon and blood glucose levels by increasing the incretin levels, glucagon-like peptide (GLP-1) and glucose-dependent insulinotropic poly-peptide (GIP), leading to insulin secretion from pancreatic beta cells. In the present study, nine 1,4-bis(phenylsulfonyl) piperazine derivatives 1a-i were synthesized and identified using 1H NMR, 13C NMR, MS and IR spectroscopies. These compounds were tested in vitro and showed inhibitory activity ranging from 11.2 to 22.6 % at 100 µmol L–1 concentration. Piperazine sulfonamide derivatives were found to be promising DPP-IV inhibitors, where the presence of electron-withdrawing groups such as Cl (1a-c) improved the activity of the compounds more than electron-donating groups such as CH3 ( 1d-f) at the same position. Additionally, meta-substitution is disfavored (1b, 1e, 1g). Induced-fit docking studies suggested that the targeted compounds 1a-i occupy the binding domain of DPP-IV and form H-bonding with the backbones of R125, E205, E206, F357, K554, W629, Y631, Y662 and R669.

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27

Yang, Ji, Haoqi Tan, Dongyu Li, Tao Jiang, Yuting Gao, Bo Li, Xue Qu i Jianli Hua. "Synthesis, two-photon absorption and aggregation-induced emission properties of multi-branched triphenylamine derivatives based on diketopyrrolopyrrole for bioimaging". RSC Advances 6, nr 63 (2016): 58434–42. http://dx.doi.org/10.1039/c6ra11269b.

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Three new DPP-based multi-branched derivatives (YJ-1–3) with AIE and 2PA properties were synthesized. YJ-1 was applied for cell imaging and two-photon excited fluorescence in vivo imaging of mouse ear.

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28

Bharath, D., S. Chithiravel, M. Sasikumar, Narendra Reddy Chereddy, Balaiah Shanigaram, K. Bhanuprakash, K. Krishnamoorthy i V. Jayathirtha Rao. "A detailed study on the thermal, photo-physical and electrochemical properties and OFET applications of D–π–A–π–D structured unsymmetrical diketopyrrolopyrrole materials". RSC Advances 5, nr 115 (2015): 94859–65. http://dx.doi.org/10.1039/c5ra16653e.

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Seven unsymmetrical DPP-derivatives with a D–π–A–π–D architecture have been synthesized and the effect of the electron donating ability and extent of electronic conjugation of the end capping units on their properties are explored.

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29

Song, Hao, Yao Gao, Weili Li, Hongkun Tian, Donghang Yan, Yanhou Geng i Fosong Wang. "Synthesis and characterization of diketopyrrolopyrrole-based conjugated molecules flanked by indenothiophene and benzoindenothiophene derivatives". Journal of Materials Chemistry C 3, nr 42 (2015): 11135–43. http://dx.doi.org/10.1039/c5tc02288f.

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Hwang, Tae Gyu, Jeong Yun Kim, Jin Woong Namgoong, Jae Moon Lee, Sim Bum Yuk, Se Hun Kim i Jae Pil Kim. "Aggregation induced emission of diketopyrrolopyrrole (DPP) derivatives for highly fluorescent red films". Photochemical & Photobiological Sciences 18, nr 5 (2019): 1064–74. http://dx.doi.org/10.1039/c8pp00403j.

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Yambulatov, Dmitriy S., Irina A. Lutsenko, Stanislav A. Nikolaevskii, Pavel A. Petrov, Ivan V. Smolyaninov, Irina K. Malyants, Victoria O. Shender i in. "α-Diimine Cisplatin Derivatives: Synthesis, Structure, Cyclic Voltammetry and Cytotoxicity". Molecules 27, nr 23 (5.12.2022): 8565. http://dx.doi.org/10.3390/molecules27238565.

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Three new Pt(II) complexes [(dpp-DAD)PtCl2] (I), [(Mes-DAD(Me)2)PtCl2] (II) and [(dpp-DAD(Me)2)PtCl2] (III) were synthesized by the direct reaction of [(CH3CN)2PtCl2] and corresponding redox-active 1,4-diaza-1,3-butadienes (DAD). The compounds were isolated in a single crystal form and their molecular structures were determined by X-ray diffraction. The purity of the complexes and their stability in solution was confirmed by NMR analysis. The Pt(II) ions in all compounds are in a square planar environment. The electrochemical reduction of complexes I–III proceeds in two successive cathodic stages. The first quasi-reversible reduction leads to the relatively stable monoanionic complexes; the second cathodic stage is irreversible. The coordination of 1,4-diaza-1,3-butadienes ligands with PtCl2 increases the reduction potential and the electron acceptor ability of the DAD ligands. The synthesized compounds were tested in relation to an adenocarcinoma of the ovary (SKOV3).

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32

Ogawa, Futa, Masanori Takeda, Kanae Miyanaga, Keita Tani, Ryuji Yamazawa, Kiyoshi Ito, Atsushi Tarui, Kazuyuki Sato i Masaaki Omote. "Development of a fluorogenic small substrate for dipeptidyl peptidase-4". Beilstein Journal of Organic Chemistry 13 (14.12.2017): 2690–97. http://dx.doi.org/10.3762/bjoc.13.267.

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A series of aniline and m-phenylenediamine derivatives with electron-withdrawing 3,3,3-trifluoropropenyl substituents were synthesized as small and chemically stable fluorescent organic compounds. Their fluorescence performances were evaluated by converting 2,4-disubstituted aniline 1 to the non-fluorescent dipeptide analogue H-Gly-Pro-1 for the use as a fluorogenic substrate for dipeptidyl peptidase-4 (DPP-4). The progress of the enzymatic hydrolysis of H-Gly-Pro-1 with DPP-4 was monitored by fluorometric determination of 1 released into the reaction medium. The results suggest that 1 could be used as fluorophore in OFF–ON-type fluorogenic probes.

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33

Hong, Lin, Bowen Zhou, Xiangxu Meng, Ding Zhang, Yihua Jiang, Dajun Liu, Guiqiu Wang, Jianli Hua i Yaochuan Wang. "Nonlinear Optical Properties of Several π Conjugated Bridge Groups based on Diketo-Pyrrole-Pyrrole: Study on the Length and Symmetry of N-atom Position Substituted Alkyl Chains". Journal of Physics: Conference Series 2470, nr 1 (1.03.2023): 012025. http://dx.doi.org/10.1088/1742-6596/2470/1/012025.

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Abstract In this paper, three modified π-conjugated bridges, were selected to study the relationship between substituted alkyl chains and two photon absorption ability as well as intramolecular charge transfer property. The modification is on the N-atom position of Diketo-Pyrrole-Pyrrole bridges. Some nonlinear optical measurements as well as several spectra methods, were used. DPP-J0, DPP-J1 and DPP-J2 exhibit cross-section of 5.6 GM, 8.1 GM, and 6.4 GM. The results exhibit obvious relation on the length and symmetry of N-atom position substituted alkyl chains. A pump-probe measurement was operated at 800 nm. Ultrafast dynamics results exhibit slight difference on the intramolecular charge transfer of these conjugated bridge derivatives. The quantum chemical calculations results are well accorded with the nonlinear optical properties. The results obtained may provide some useful information on molecular design and optimization of new advanced materials.

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Lukina, Daria A., Alexandra A. Skatova, Anton N. Lukoyanov, Ekaterina A. Kozlova i Igor L. Fedushkin. "Alkali metal reduction of 1,3,2-diazaborol and 1,3,2-diazagermol derivatives based on 1,2-bis[(2,6-diisopropylphenyl)imino]acenaphthene". Dalton Transactions 49, nr 9 (2020): 2941–46. http://dx.doi.org/10.1039/c9dt04652f.

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The reduction of borol (5) and germol (7) derivatives with sodium in thf proceeds with a transfer of two electrons and one proton to dpp-bian ligand and results in the formation of the products 6 and 8, which consist of the diamagnetic mono-anionic ligand.

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35

Jiang, Bin, Chen Chen Du, Min Jie Li, Ke Gao, Li Kou, Ming Chen, Feng Liu, Thomas P. Russell i Hongyu Wang. "Synthesis of fluorinated diphenyl-diketopyrrolopyrrole derivatives as new building blocks for conjugated copolymers". Polymer Chemistry 7, nr 19 (2016): 3311–24. http://dx.doi.org/10.1039/c6py00346j.

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A series of conjugated copolymers with an identical backbone (PBDT-DPP) but different fluorination numbers and positions were synthesized, and the impact of fluorine atoms on the structure–property-device performance was comprehensively investigated.

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36

Periasamy, Mariappan, Boda Venkanna, Miriyala Nagaraju i Lakavathu Mohan. "Methods for the Synthesis of Piperazine Derivatives Containing a Chiral Bi-2-naphthyl Moiety". Synthesis 52, nr 01 (1.10.2019): 127–34. http://dx.doi.org/10.1055/s-0037-1610731.

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Piperazine derivatives containing 1,1′-bi-2-naphthyl moiety were synthesized starting from 2,2′-dimethoxy-1,1′-bi-naphthalene via acylation using ethyl chlorooxoacetate and subsequent condensation with 1,2-diamines followed by reduction of the corresponding dihydro-2-piperazinone intermediate using the NaBH4/I2 reagent system. The corresponding chiral piperazine derivatives containing bi-2-napthyl moiety was synthesized by asymmetric reduction of ethyl dimethoxy-bi-2-naphthyloxoacetate by chiral oxazoborolidine catalyst prepared in situ using S-diphenylprolinol (S-DPP), B(OCH3)3 and H3B·THF. The resulting diols were mesylated and cyclized using 1,2-diamines to obtain the corresponding chiral piperazine derivatives.

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37

Park, Woul Seong, Mi Ae Jun, Mi Sik Shin, Sung Wook Kwon, Seung Kyu Kang, Ki Young Kim, Sang Dal Rhee i in. "Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors". Journal of Fluorine Chemistry 130, nr 11 (listopad 2009): 1001–10. http://dx.doi.org/10.1016/j.jfluchem.2009.08.001.

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38

Bura, Thomas, Serge Beaupré, Marc-André Légaré, Olzhas Ibraikulov, Nicolas Leclerc i Mario Leclerc. "Theoretical Calculations for Highly Selective Direct Heteroarylation Polymerization: New Nitrile-Substituted Dithienyl-Diketopyrrolopyrrole-Based Polymers". Molecules 23, nr 9 (12.09.2018): 2324. http://dx.doi.org/10.3390/molecules23092324.

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Direct Heteroarylation Polymerization (DHAP) is becoming a valuable alternative to classical polymerization methods being used to synthesize π-conjugated polymers for organic electronics applications. In previous work, we showed that theoretical calculations on activation energy (Ea) of the C–H bonds were helpful to rationalize and predict the selectivity of the DHAP. For readers’ convenience, we have gathered in this work all our previous theoretical calculations on Ea and performed new ones. Those theoretical calculations cover now most of the widely utilized electron-rich and electron-poor moieties studied in organic electronics like dithienyl-diketopyrrolopyrrole (DT-DPP) derivatives. Theoretical calculations reported herein show strong modulation of the Ea of C–H bond on DT-DPP when a bromine atom or strong electron withdrawing groups (such as fluorine or nitrile) are added to the thienyl moiety. Based on those theoretical calculations, new cyanated dithienyl-diketopyrrolopyrrole (CNDT-DPP) monomers and copolymers were prepared by DHAP and their electro-optical properties were compared with their non-fluorinated and fluorinated analogues.

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39

Belal, Fathalla, Ibrahim A. Al-Zaagi i Mohamed A. Abounassif. "Voltammetric Determination of Benazepril and Ramipril in Dosage Forms and Biological Fluids through Nitrosation". Journal of AOAC INTERNATIONAL 84, nr 1 (1.01.2001): 1–8. http://dx.doi.org/10.1093/jaoac/84.1.1.

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Abstract A simple and highly sensitive voltammetric method was developed for the determination of benazepril (I) and ramipril (II). The compounds were treated with nitrous acid, and the cathodic current produced by the resulting nitroso derivatives was measured. The voltammetric behavior was studied by adopting direct current (DCt), differential pulse (DPP), and alternating current (ACt) polarography. Both compounds produced well-defined, diffusion-controlled cathodic waves over the whole pH range in Britton-Robinson buffers (BRb). At pH 3 and 5, the values of diffusion-current constants (Id), were 5.90 ± 0.40 and 6.66 ± 0.61 for I and II, respectively. The current–concentration plots for I were rectilinear over the range of 1.5–40 and 0.1–30 μg/mL in the DCt and DPP modes, respectively; for II, the range was 2–30 and 0.1–20 μg/mL in the DCt and DPP modes, respectively. The minimum detectabilities (S/N = 2) were 0.015 μg/mL (about 3.25 × 10−8M) and 0.012 μg/mL (about 2.88 × 10−8M) for I and II, respectively, adopting the DPP mode. Results obtained for the proposed method when applied to the determination of both compounds in dosage forms were in good agreement with those obtained using reference methods. Hydrochlorthiazide, which is frequently co-formulated with these drugs, did not interfere with the assay. The method was also applied to the determination of benazepril in spiked human urine and plasma. The percentage recoveries adopting the DPP mode were 96.2 ± 1.21 and 95.7 ± 1.61, respectively.

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40

Sannes, P. L., B. H. Schofield i D. F. McDonald. "Histochemical localization of cathepsin B, dipeptidyl peptidase I, and dipeptidyl peptidase II in rat bone." Journal of Histochemistry & Cytochemistry 34, nr 8 (sierpień 1986): 983–88. http://dx.doi.org/10.1177/34.8.3016074.

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The histochemical distribution of the thiol proteases cathepsin B and dipeptidyl peptidase I and the serine protease dipeptidyl peptidase II was examined in rat bone and joint using amino acid derivatives of 4-methoxy-2-naphthylamine (MNA). The liberated MNA was then visualized by simultaneous coupling with fast blue B. Cathepsin B was examined with CBZ-Arg-Arg-MNA, dipeptidyl peptidase I (DPP I) with Gly-Arg- or Pro-Arg-MNA, and dipeptidyl peptidase II (DPP II) with Lys-ALA- or Lys-Pro-MNA. Bright red reaction product indicative of proteolytic activity was observed in most cell types associated with bone and its surrounding connective tissues, including osteocytes, osteoblasts, chondrocytes, chondroblasts, fibroblasts, and macrophages. Surprisingly, protease activity in osteoclasts could not be established with certainty, and it was concluded that these enzymes are either absent, present in very low amounts, or secreted as soon as they are synthesized rather than stored within the cell. The cells of the resting zone of the growth plate were intensely reactive for DPP II but were only moderately reactive for cathepsin B and DPP I. The reverse was true of the proliferating and hypertrophic layers. The protease activity observed in bone, cartilage, tendon, ligament, and synovium would be expected to contribute significantly to normal protein metabolism as well as to pathological destruction in these tissues.

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Agrawal, Ritesh, Pratima Jain, Subodh Dikshit i Radhe Bahare. "3D QSAR and Docking Study of Gliptin Derivatives as DPP-IV Inhibitors". Combinatorial Chemistry & High Throughput Screening 16, nr 4 (1.02.2013): 249–73. http://dx.doi.org/10.2174/1386207311316040001.

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42

Han, Bei, Jing Long Liu, Yi Huan, Peng Li, Qi Wu, Zi Yun Lin, Zhu Fang Shen, Da Li Yin i Hai Hong Huang. "Design, synthesis and primary activity of thiomorpholine derivatives as DPP-IV inhibitors". Chinese Chemical Letters 23, nr 3 (marzec 2012): 297–300. http://dx.doi.org/10.1016/j.cclet.2011.12.007.

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Areephong, Jetsuda, Arthur D. Hendsbee i Gregory C. Welch. "Facile synthesis of unsymmetrical and π-extended furan-diketopyrrolopyrrole derivatives through C–H direct (hetero)arylation using a heterogeneous catalyst system". New Journal of Chemistry 39, nr 9 (2015): 6714–17. http://dx.doi.org/10.1039/c5nj01150g.

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Emami, Leila, Zahra Faghih, Amirhossein Sakhteman, Zahra Rezaei, Zeinab Faghih, Farnaz Salehi i Soghra Khabnadideh. "Design, synthesis, molecular simulation, and biological activities of novel quinazolinone-pyrimidine hybrid derivatives as dipeptidyl peptidase-4 inhibitors and anticancer agents". New Journal of Chemistry 44, nr 45 (2020): 19515–31. http://dx.doi.org/10.1039/d0nj03774e.

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Song, Xuejing, Lingqian Kong, Hongmei Du, Xiangyu Li, Hanlin Feng, Jinsheng Zhao i Yu Xie. "Effects of Pyrazine Derivatives and Substituted Positions on the Photoelectric Properties and Electromemory Performance of D–A–D Series Compounds". Materials 11, nr 10 (22.10.2018): 2063. http://dx.doi.org/10.3390/ma11102063.

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Pyrazine derivatives quinoxaline and pyridopyrazine were selected as the acceptors, and benzocarbazole was used as the donor to synthesize four different D–A–D compounds. The results showed that 2,3-bis(decyloxy)pyridine[3,4-b]pyrazine (DPP) exhibited stronger electron-withdrawing ability than that of 2,3-bis(decyloxy)quinoxaline (DPx), because DPP possesses one more nitrogen (N) atom, resulting in a red-shift of the intramolecular charge transfer (ICT) absorption bands and fluorescent emission spectra for compounds with DPP as the acceptor compared with those that use DPx as the acceptor. The band-gap energy (Eg) of the four D–A–D compounds were 2.82 eV, 2.70 eV, 2.48 eV, and 2.62 eV, respectively, for BPC-2DPx, BPC-3DPx, BPC-2DPP, and BPC-3DPP. The solvatochromic effect was insignificant when the four compounds were in the ground state, which became significant in an excited state. With increasing solvent polarity, a 30–43 nm red shift was observed in the emissive spectra of the compounds. The thermal decomposition temperatures of the four compounds between 436 and 453 °C had very high thermal stability. Resistor-type memory devices based on BPC-2DPx and BPC-2DPP were fabricated in a simple sandwich configuration, Al/BPC-2DPx/ITO or Al/BPC-2DPP/ITO. The two devices showed a binary non-volatile flash memory, with lower threshold voltages and better repeatability.

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Agić, Dejan, Maja Karnaš, Domagoj Šubarić, Melita Lončarić, Sanja Tomić, Zrinka Karačić, Drago Bešlo i in. "Coumarin Derivatives Act as Novel Inhibitors of Human Dipeptidyl Peptidase III: Combined In Vitro and In Silico Study". Pharmaceuticals 14, nr 6 (5.06.2021): 540. http://dx.doi.org/10.3390/ph14060540.

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Dipeptidyl peptidase III (DPP III), a zinc-dependent exopeptidase, is a member of the metalloproteinase family M49 with distribution detected in almost all forms of life. Although the physiological role of human DPP III (hDPP III) is not yet fully elucidated, its involvement in pathophysiological processes such as mammalian pain modulation, blood pressure regulation, and cancer processes, underscores the need to find new hDPP III inhibitors. In this research, five series of structurally different coumarin derivatives were studied to provide a relationship between their inhibitory profile toward hDPP III combining an in vitro assay with an in silico molecular modeling study. The experimental results showed that 26 of the 40 tested compounds exhibited hDPP III inhibitory activity at a concentration of 10 µM. Compound 12 (3-benzoyl-7-hydroxy-2H-chromen-2-one) proved to be the most potent inhibitor with IC50 value of 1.10 μM. QSAR modeling indicates that the presence of larger substituents with double and triple bonds and aromatic hydroxyl groups on coumarin derivatives increases their inhibitory activity. Docking predicts that 12 binds to the region of inter-domain cleft of hDPP III while binding mode analysis obtained by MD simulations revealed the importance of 7-OH group on the coumarin core as well as enzyme residues Ile315, Ser317, Glu329, Phe381, Pro387, and Ile390 for the mechanism of the binding pattern and compound 12 stabilization. The present investigation, for the first time, provides an insight into the inhibitory effect of coumarin derivatives on this human metalloproteinase.

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Li, Ning, Li-Jun Wang, Bo Jiang, Shu-Ju Guo, Xiang-Qian Li, Xue-Chun Chen, Jiao Luo, Chao Li, Yi Wang i Da-Yong Shi. "Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors". Bioorganic & Medicinal Chemistry Letters 28, nr 12 (lipiec 2018): 2131–35. http://dx.doi.org/10.1016/j.bmcl.2018.05.022.

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Guild, Jonathan, Michael J. Morris, Craig C. Robertson i Alexander W. H. Speed. "One-pot synthesis of new iso-DPP derivatives from terminal alkynes and isocyanates". Tetrahedron Letters 60, nr 39 (wrzesień 2019): 151079. http://dx.doi.org/10.1016/j.tetlet.2019.151079.

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Soni, Rina, i Shubhangi S. Soman. "Design and synthesis of aminocoumarin derivatives as DPP-IV inhibitors and anticancer agents". Bioorganic Chemistry 79 (wrzesień 2018): 277–84. http://dx.doi.org/10.1016/j.bioorg.2018.05.008.

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Fang, Yuanying, Shaokun Zhang, Wenting Wu, Yanhua Liu, Juan Yang, Yuyuan Li, Min Li i in. "Design and synthesis of tetrahydropyridopyrimidine derivatives as dual GPR119 and DPP-4 modulators". Bioorganic Chemistry 94 (styczeń 2020): 103390. http://dx.doi.org/10.1016/j.bioorg.2019.103390.

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