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Relevant bibliographies by topics / Piperazinic scaffolds

Academic literature on the topic 'Piperazinic scaffolds'

Author: Grafiati

Published: 10 March 2023

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Journal articles on the topic "Piperazinic scaffolds"

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Hafeez, Freeha, Ameer Fawad Zahoor, Azhar Rasul, Asim Mansha, Razia Noreen, Zohaib Raza, Kulsoom Ghulam Ali, Ali Irfan, and Gamal A. El-Hiti. "Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs." Molecules 27, no. 15 (July 26, 2022): 4776. http://dx.doi.org/10.3390/molecules27154776.

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Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological activities. Under ultrasound conditions, the corresponding piperazine-1-carbodithioates 5a–5j were synthesized from monosubstituted piperazine 2 and N-phenylacetamides 4a–4j in the presence of sodium acetate and carbon disulfide in methanol. The structures of the newly synthesized piperazines were confirmed, and their anti-lung carcinoma effects were evaluated. A cytotoxic assay was performed to assess the hemolytic and thrombolytic potential of the synthesized piperazines 5a–5j. The types of substituents on the aryl ring were found to affect the anticancer activity of piperazines 5a–5j. Piperazines containing 2-chlorophenyl (5b; cell viability = 25.11 ± 2.49) and 2,4-dimethylphenyl (5i; cell viability = 25.31 ± 3.62) moieties demonstrated the most potent antiproliferative activity. On the other hand, piperazines containing 3,4-dichlorophenyl (5d; 0.1%) and 3,4-dimethylphenyl (5j; 0.1%) rings demonstrated the least cytotoxicity. The piperazine with the 2,5-dimethoxyphenyl moiety (5h; 60.2%) showed the best thrombolytic effect. To determine the mode of binding, in silico modeling of the most potent piperazine (i.e., 5b) was performed, and the results were in accordance with those of antiproliferation. It exhibits a similar binding affinity to PQ10 and an efficient conformational alignment with the lipophilic site of PDE10A conserved for PQ10A.

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Wierschem, Frank, and Karola Rück-Braun. "Introduction of Substituents on the 2-Oxo-piperazine Skeleton by [3+2] Cycloaddition and Subsequent Transformation." Zeitschrift für Naturforschung B 61, no. 4 (April 1, 2006): 431–36. http://dx.doi.org/10.1515/znb-2006-0410.

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The 3,4-substituted 2-oxo-piperazines 5 - 9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly discussed for adducts derived from N-substituted maleic imides

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Ye, Zhishi, Kristen E. Gettys, and Mingji Dai. "Opportunities and challenges for direct C–H functionalization of piperazines." Beilstein Journal of Organic Chemistry 12 (April 13, 2016): 702–15. http://dx.doi.org/10.3762/bjoc.12.70.

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Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C–H functionalization on piperazines in order to lend structural diversity to this privileged drug scaffold. Multiple approaches such as those involving α-lithiation trapping, transition-metal-catalyzed α-C–H functionalizations, and photoredox catalysis are discussed. We also highlight the difficulties experienced when successful methods for α-C–H functionalization of acyclic amines and saturated mono-nitrogen heterocyclic compounds (such as piperidines and pyrrolidines) were applied to piperazine substrates.

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Zoidis, Grigoris, María Isabel Loza, and Marco Catto. "Design, Synthesis and 5-HT1A Binding Affinity of N-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)tricyclo[3.3.1.13,7]decan-1-amine and N-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)-3,5-dimethyl-tricylo[3.3.1.13,7]decan-1-amine." Molbank 2022, no. 1 (March 10, 2022): M1353. http://dx.doi.org/10.3390/m1353.

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Based on previously highlighted structural features, the development of highly selective 5-HT1A receptor inhibitors is closely linked to the incorporation of a 4-alkyl-1-arylpiperazine scaffold on them. In this paper, we present the synthesis of two new compounds bearing the 2-MeO-Ph-piperazine moiety linked via a three carbon atom linker to the amine group of 1-adamantanamine and memantine, respectively. Both were tested for their binding affinity against 5-HT1A receptor. N-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)tricyclo[3.3.1.13,7]decan-1-amine fumarate (8) and N-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)-3,5-dimethyl-tricylo[3.3.1.13,7]decan-1-amine fumarate (10) proved to be highly selective ligands towards 5-HT1A receptor with a binding constant of 1.2 nM and 21.3 nM, respectively, while 5-carboxamidotriptamine (5-CT) (2) was used as an internal standard for this assay with a measured Ki = 0.5 nM.

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Aboutabl, Mona Elsayed, Ahmed Ragab Hamed, Mohamed Farouk Hamissa, and Emad Khairy Ahmed. "Anti-Inflammatory and Analgesic Activities of 7-Chloro-4-(Piperazin-1-yl) Quinoline Derivative Mediated by Suppression of InflammatoryMediators Expression in Both RAW 264.7 and Mouse Models." Pharmaceutical Sciences 27, no. 3 (December 30, 2020): 326–38. http://dx.doi.org/10.34172/ps.2020.101.

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Background: 4-Aminoquinoline derivatives possess various potential biological properties.The introduction of additional piperazine heterocyclic pharmacophoric moiety tends to haveprofound impact in increasing the activity. The present work was undertaken to investigate thein-vitro and in-vivo anti-inflammatory activity as well as the peripheral and central analgesicactivities of compound 1-(4-(7-chloroquinoline-4-yl)piperazin-1-yl)-2-(4-phenylpiperazin-1-yl)ethanone (5) in experimental models. Methods: The percentage inhibition of the lipopolysaccharide induced NO release of 7-chloro-4-(piperazin-1-yl)quinoline derivatives 1-9 was determined in RAW 264.7 murine macrophagemodel. Western blot analysis was performed to evaluate the effect of compound 5 on proteinexpression of inducible nitric oxide synthase (iNOS). Gene expression of inflammatory markerswas evaluated using real-time polymerase chain reaction. The peripheral and central analgesicactivities of compound 5 were evaluated in mice using writhing and hot-plate tests, respectively.Anti-inflammatory activity was assessed using carrageenan-induced paw edema assay in miceand serum NO and COX-2 levels were measured. Results: Compound 5 demonstrated the highest NO inhibitory activity that was accompaniedby inhibition of iNOS protein expression and decreased gene expression levels of inflammatorymarkers. It revealed a potential peripheral analgesic effect through inhibition of abdominalwrithing in mice treated with doses of 15 and 30 mg/kg and its effect was comparable to diclofenacsodium. Compound 5 possessed an analgesic activity starting from 15 min post administrationand reached its peak at 45 min which was significantly higher than that of tramadol hydrochloridesuggesting its potential as central analgesic agent. It also showed percentage of inhibition ofedema of 34, 50 and 64% at 1, 2, and 3 h respectively, post carrageenan challenge together with asignificant decrease in serum NO and COX-2 levels. Conclusion: The remarkable anti-inflammatory and analgesic activities of compound 5 couldbe attributed to the advantageous introduction of the heterocyclic 7-chloro-4-(piperazin1-yl)quinoline scaffold incorporated with N-phenylpiperzine functional groups linked together withthe ethanone pharmacophoric chain.

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Rani, Anu, Sumit Kumar, Jenny Legac, Adebayo A. Adeniyi, Paul Awolade, Parvesh Singh, Philip J. Rosenthal, and Vipan Kumar. "Design, synthesis, heme binding and density functional theory studies of isoindoline-dione-4-aminoquinolines as potential antiplasmodials." Future Medicinal Chemistry 12, no. 3 (February 2020): 193–205. http://dx.doi.org/10.4155/fmc-2019-0260.

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Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% of deaths affecting the African region. Results/methodology: Microwave promoted the synthesis of cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmodial activities. Compound with the optimum combination of propyl chain length and hydroxyethyl piperazine proved to be the most potent among the synthesized scaffolds against chloroquine-resistant W2 strain of Plasmodium falciparum with an IC50 value of 0.006 μM. Heme-binding along with density functional theory studies were further carried out in order to delineate the mechanism of action of the most active compound. Conclusion: The synthesized scaffold can act as a therapeutic template for further synthetic modifications toward the search for a new antimalarial agent.

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Stucchi, Mattia, Silvia Cairati, Rengul Cetin-Atalay, Michael S. Christodoulou, Giovanni Grazioso, Gennaro Pescitelli, Alessandra Silvani, Deniz Cansen Yildirim, and Giordano Lesma. "Application of the Ugi reaction with multiple amino acid-derived components: synthesis and conformational evaluation of piperazine-based minimalist peptidomimetics." Organic & Biomolecular Chemistry 13, no. 17 (2015): 4993–5005. http://dx.doi.org/10.1039/c5ob00218d.

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Okitsu, Takashi, Arisa Horike, Natsumi Shimazawa, and Akimori Wada. "A dearomative ipso-iodocyclization/desymmetrization sequence leading to optically active tricyclic piperazine scaffolds." Organic & Biomolecular Chemistry 18, no. 18 (2020): 3501–11. http://dx.doi.org/10.1039/d0ob00510j.

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9

Darapaneni, Chandra Mohan, Prathap Jeya Kaniraj, and Galia Maayan. "Water soluble hydrophobic peptoids via a minor backbone modification." Organic & Biomolecular Chemistry 16, no. 9 (2018): 1480–88. http://dx.doi.org/10.1039/c7ob02928d.

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10

Derbyshire, Emily R., Jaeki Min, W. Armand Guiguemde, Julie A. Clark, Michele C. Connelly, Andreia D. Magalhães, R. Kiplin Guy, and Jon Clardy. "Dihydroquinazolinone Inhibitors of Proliferation of Blood and Liver Stage Malaria Parasites." Antimicrobial Agents and Chemotherapy 58, no. 3 (December 23, 2013): 1516–22. http://dx.doi.org/10.1128/aac.02148-13.

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ABSTRACTDrugs that target both the liver and blood stages of malaria will be needed to reduce the disease's substantial worldwide morbidity and mortality. Evaluation of a 259-member library of compounds that block proliferation of the blood stage of malaria revealed several scaffolds—dihydroquinazolinones, phenyldiazenylpyridines, piperazinyl methyl quinolones, and bis-benzimidazoles—with promising activity against the liver stage. Focused structure-activity studies on the dihydroquinazolinone scaffold revealed several molecules with excellent potency against both blood and liver stages. One promising early lead with dual activity is 2-(p-bromophenyl)-3-(2-(diethylamino)ethyl)-2,3-dihydroquinazolin-4(1H)-one with 50% effective concentrations (EC50s) of 0.46 μM and 0.34 μM against liver stagePlasmodium bergheiANKA and blood stagePlasmodium falciparum3D7 parasites, respectively. Structure-activity relationships revealed that liver stage activity for this compound class requires a 3-dialkyl amino ethyl group and is abolished by substitution at theortho-position of the phenyl moiety. These compounds have minimal toxicity to mammalian cells and are thus attractive compounds for further development.

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Dissertations / Theses on the topic "Piperazinic scaffolds"

1

CATALANI, MARIA PIA. "Stereoselective synthesis of new piperazinic polycyclic scaffolds with potential biological activity." Doctoral thesis, 2014. http://hdl.handle.net/2158/850912.

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Book chapters on the topic "Piperazinic scaffolds"

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Yamamoto, Koki. "Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Synthesis and Application of Fused Piperazine Derivatives for Investigation of Degradable Core Motifs." In Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists, 27–70. Singapore: Springer Singapore, 2020. http://dx.doi.org/10.1007/978-981-15-2965-8_3.

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