Готові списки джерел за темами / Benzamidine analogues

Добірка наукової літератури з теми "Benzamidine analogues"

Автор: Grafiati
Опубліковано: 10 грудня 2022
Оновлено: 28 січня 2023

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Статті в журналах з теми "Benzamidine analogues"

1

Fouda, A. S., M. A. Ismail, A. S. Abousalem, and G. Y. Elewady. "Experimental and theoretical studies on corrosion inhibition of 4-amidinophenyl-2,2′-bifuran and its analogues in acidic media." RSC Adv. 7, no. 73 (2017): 46414–30. http://dx.doi.org/10.1039/c7ra08092a.

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Анотація:
Corrosion inhibition studies of carbon steel (CS) in 1 M HCl by newly synthesized bichalcophene compounds namely; 4-(2,2′-bifuran-5-yl)benzamidine (MA-0947) and 6-(2,2′-bifuran-5-yl)nicotinamidine (MA-0941) and 6-[5-(thiophen-2-yl)furan-2-yl]nicotinamidine (MA-0940).
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2

Sa’ad, Mohammad Auwal, Ramasamy Kavitha, Shivkanya Fuloria, Neeraj Kumar Fuloria, Manickam Ravichandran, and Pattabhiraman Lalitha. "Synthesis, Characterization and Biological Evaluation of Novel Benzamidine Derivatives: Newer Antibiotics for Periodontitis Treatment." Antibiotics 11, no. 2 (February 7, 2022): 207. http://dx.doi.org/10.3390/antibiotics11020207.

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Periodontal disease (PD) is complex polymicrobial disease which destroys tooth-supporting tissue. Although various synthetic inhibitors of periodontitis-triggering pathogens have been recognized, their undesirable side effects limit their application. Hence, the present study intended to perform the synthesis, characterization, antimicrobial evaluation, and cytotoxicity analysis of novel benzamidine analogues (NBA). This study involved the synthesis of novel imino bases of benzamidine (4a–c), by reacting different aromatic aldehydes with 2-(4-carbamimidoylphenoxy) acetohydrazide (3), which was synthesized by the hydrazination of ethyl 2-(4-carbamimidoylphenoxy) acetate (2), the derivative of 4-hydroxybenzene carboximidamide (1). This was followed by characterization using FTIR, 1H, 13C NMR and mass spectrometry. All synthesized compounds were further tested for antimicrobial potential against PD-triggering pathogens by the micro broth dilution method. The cytotoxicity analysis of the NBA against HEK 293 cells was conducted using an MTT assay. The present study resulted in a successful synthesis of NBA and elucidated their structures. The synthesized NBA exhibited significant antimicrobial activity values between 31.25 and 125 µg/mL against tested pathogens. All NBA exhibited weak cytotoxicity against HEK 293 cells at 7.81 µg, equally to chlorhexidine at 0.2%. The significant antimicrobial activity of NBA against PD-triggering pathogens supports their potential application in periodontitis treatment.
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3

Atassi, M. Z. "Surface-simulation synthesis of the substrate-binding site of an enzyme. Demonstration with trypsin." Biochemical Journal 226, no. 2 (March 1, 1985): 477–85. http://dx.doi.org/10.1042/bj2260477.

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Анотація:
From the X-ray co-ordinates of bovine trypsin and its complexes with substrate analogues (benzamidine) and with soya-bean trypsin inhibitor, a peptide (TP) was designed and synthesized by surface-simulation synthesis, a concept previously introduced by this laboratory, to mimic the binding site of trypsin. Also, a control peptide (CTP) was synthesized that contained all the amino acids present in the TP peptide, except that their order was randomized. The radioiodinated TP peptide bound specifically to adsorbents of benzamidine, whereas the control CTP peptide exhibited no binding activity. Conjugates to succinyl (3-carboxypropionyl)-lysozyme of the TP peptide, control CTP peptide and other unrelated peptides were examined by a radiometric binding assay for the ability to bind soya-bean trypsin inhibitor and human alpha 1-antitrypsin. Conjugates of the TP peptide exhibited considerable binding activity to adsorbents of soya-bean trypsin inhibitor or alpha 1-antitrypsin. None of the other peptide conjugates possessed any binding activity. Action of the active-site-directed reagents phenylmethanesulphonyl fluoride and di-isopropyl phosphorofluoridate on free TP and CTP peptides resulted in the modification of a serine residue in the TP peptide whereas the CTP peptide remained unaltered. The TP peptide, either in the free form or as a conjugate on succinyl-lysozyme, had no enzymic activity on protein substrates or on tosylarginine methyl ester. These findings indicated that the binding activity of an enzyme was well mimicked by the surface-stimulation peptide but that reproduction of the catalytic activity was not obtained.
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4

Kalinichenko, Elena, Aliaksandr Faryna, Viktoria Kondrateva, Alena Vlasova, Valentina Shevchenko, Alla Melnik, Olga Avdoshko, and Alla Belko. "Synthesis, Biological Activities and Docking Studies of Novel 4-(Arylaminomethyl)benzamide Derivatives as Potential Tyrosine Kinase Inhibitors." Molecules 24, no. 19 (September 30, 2019): 3543. http://dx.doi.org/10.3390/molecules24193543.

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A number of new compounds containing the 4-(aminomethyl)benzamide fragment as a linker were designed and synthesized, and their biological activities were evaluated as potential anticancer agents. The cytotoxicity activity of the designed compounds was studied in two hematological and five solid cell lines in comparison with the reference drugs. Targeted structures against eight receptor tyrosine kinases including EGFR, HER-2, HER-4, IGF1R, InsR, KDR, PDGFRa, and PDGFRb were investigated. The majority of the compounds showed a potent inhibitory activity against the tested kinases. The analogues 11 and 13 with the (trifluoromethyl)benzene ring in the amide or amine moiety of the molecule were proven to be highly potent against EGFR, with 91% and 92% inhibition at 10 nM, respectively. The docking of synthesized target compounds for nine protein kinases contained in the Protein Data Bank (PDB) database was carried out. The molecular modeling results for analogue 10 showed that the use of the 4-(aminomethyl)benzamide as a flexible linker leads to a favorable overall geometry of the molecule, which allows one to bypass the bulk isoleucine residue and provides the necessary binding to the active center of the T315I-mutant Abl (PDB: 3QRJ).
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5

Veselinović, Aleksandar M., Andrey Toropov, Alla Toropova, Dobrila Stanković-Đorđević, and Jovana B. Veselinović. "Design and development of novel antibiotics based on FtsZ inhibition – in silico studies." New Journal of Chemistry 42, no. 13 (2018): 10976–82. http://dx.doi.org/10.1039/c8nj01034j.

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6

Sugano, Kiyohiko, Shoshin Yoshida, Mikio Takaku, Masayuki Haramura, Ryoichi Saitoh, Yoshiaki Nabuchi, and Hidetoshi Ushio. "Quantitative structure–intestinal permeability relationship of benzamidine analogue thrombin inhibitor." Bioorganic & Medicinal Chemistry Letters 10, no. 17 (September 2000): 1939–42. http://dx.doi.org/10.1016/s0960-894x(00)00367-x.

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7

Elkamhawy, Ahmed, Na Kyoung Oh, Noha A. Gouda, Magda H. Abdellattif, Saud O. Alshammari, Mohammed A. S. Abourehab, Qamar A. Alshammari, et al. "Novel Hybrid Indole-Based Caffeic Acid Amide Derivatives as Potent Free Radical Scavenging Agents: Rational Design, Synthesis, Spectroscopic Characterization, In Silico and In Vitro Investigations." Metabolites 13, no. 2 (January 17, 2023): 141. http://dx.doi.org/10.3390/metabo13020141.

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Анотація:
Antioxidant small molecules can prevent or delay the oxidative damage caused by free radicals. Herein, a structure-based hybridization of two natural antioxidants (caffeic acid and melatonin) afforded a novel hybrid series of indole-based amide analogues which was synthesized with potential antioxidant properties. A multiple-step scheme of in vitro radical scavenging assays was carried out to evaluate the antioxidant activity of the synthesized compounds. The results of the DPPH assay demonstrated that the indole-based caffeic acid amides are more active free radical scavenging agents than their benzamide analogues. Compared to Trolox, a water-soluble analogue of vitamin E, compounds 3a, 3f, 3h, 3j, and 3m were found to have excellent DPPH radical scavenging activities with IC50 values of 95.81 ± 1.01, 136.8 ± 1.04, 86.77 ± 1.03, 50.98 ± 1.05, and 67.64 ± 1.02 µM. Three compounds out of five (3f, 3j, and 3m) showed a higher capacity to neutralize the radical cation ABTS•+ more than Trolox with IC50 values of 14.48 ± 0.68, 19.49 ± 0.54, and 14.92 ± 0.30 µM, respectively. Compound 3j presented the highest antioxidant activity with a FRAP value of 4774.37 ± 137.20 μM Trolox eq/mM sample. In a similar way to the FRAP assay, the best antioxidant activity against the peroxyl radicals was demonstrated by compound 3j (10,714.21 ± 817.76 μM Trolox eq/mM sample). Taken together, compound 3j was validated as a lead hybrid molecule that could be optimized to maximize its antioxidant potency for the treatment of oxidative stress-related diseases.
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8

Balkrishna, Shah Jaimin, Shailesh Kumar, Gajendra Kumar Azad, Bhagat Singh Bhakuni, Piyush Panini, Navjeet Ahalawat, Raghuvir Singh Tomar, Michael R. Detty, and Sangit Kumar. "An ebselen like catalyst with enhanced GPx activity via a selenol intermediate." Org. Biomol. Chem. 12, no. 8 (2014): 1215–19. http://dx.doi.org/10.1039/c4ob00027g.

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Анотація:
Benzamide ring-substituted, quinine-derived ebselen analogue is synthesized which exists in selenol form upon addition of PhSH. It catalyses oxidation of PhSH with H2O2 faster (103-fold) than ebselen.
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9

Ong, Xandria, Manan Ahmed, Luonan Xu, Ashley T. Brennan, Carol Hua, Katrina A. Zenere, Zixi Xie, Cameron J. Kepert, Benjamin J. Powell, and Suzanne M. Neville. "Spin-Crossover 2-D Hofmann Frameworks Incorporating an Amide-Functionalized Ligand: N-(pyridin-4-yl)benzamide." Chemistry 3, no. 1 (March 1, 2021): 360–72. http://dx.doi.org/10.3390/chemistry3010026.

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Анотація:
Two analogous 2-D Hofmann-type frameworks, which incorporate the novel ligand N-(pyridin-4-yl)benzamide (benpy) [FeII(benpy)2M(CN)4]·2H2O (M = Pd (Pd(benpy)) and Pt (Pt(benpy))) are reported. The benpy ligand was explored to facilitate spin-crossover (SCO) cooperativity via amide group hydrogen bonding. Structural analyses of the 2-D Hofmann frameworks revealed benpy-guest hydrogen bonding and benpy-benpy aromatic contacts. Both analogues exhibited single-step hysteretic spin-crossover (SCO) transitions, with the metal-cyanide linker (M = Pd or Pt) impacting the SCO spin-state transition temperature and hysteresis loop width (Pd(benpy): T½↓↑: 201, 218 K, ∆T: 17 K and Pt(benpy): T½↓↑: 206, 226 K, ∆T: 20 K). The parallel structural and SCO changes over the high-spin to low-spin transition were investigated using variable-temperature, single-crystal, and powder X-ray diffraction, Raman spectroscopy, and differential scanning calorimetry. These studies indicated that the ligand–guest interactions facilitated by the amide group acted to support the cooperative spin-state transitions displayed by these two Hofmann-type frameworks, providing further insight into cooperativity and structure–property relationships.
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10

Sugano, Kiyohiko, Shoshin Yoshida, Mikio Takaku, Masayuki Haramura, Ryoichi Saitoh, Yoshiaki Nabuchi, and Hidetoshi Ushio. "Corrigendum to “Quantitative structure–Intestinal permeability relationship of benzamidine analogue thrombin inhibitor”." Bioorganic & Medicinal Chemistry Letters 11, no. 8 (April 2001): 1097. http://dx.doi.org/10.1016/s0960-894x(01)00121-4.

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Більше джерел

Дисертації з теми "Benzamidine analogues"

1

Ni, Liming. "Synthesis and evaluation of new peptidyl phosphonate analogs of benzamidine, lysine and homolysine as irreversible inhibitors for thrombin and other trypsin-like enzymes." Diss., Georgia Institute of Technology, 1997. http://hdl.handle.net/1853/27080.

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2

Zalavadia, Ankit. "QUANTITATIVE ANALYSIS OF 5-CHLORO-2-METHOXY-N-[2-(4-SULFAMOYLPHENYL)ETHYL]BENZAMIDE (GLYBURIDE ANALOGUE, GA) IN MOUSE PLASMA AND WHOLE BLOOD USING A MICRO-EXTRACTION AND LIQUID CHROMATOGRAPHY-TANDEM MASS SPECTROMETRY." VCU Scholars Compass, 2016. http://scholarscompass.vcu.edu/etd/4279.

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Анотація:
Pharmacokinetic evaluation of 5-chloro-2-methoxy-N-[2-(4- sulfamoylphenyl)ethyl]benzamide in mouse plasma demanded for a suitable bioanalytical method. No reported bioanalytical method exists to-date that can quantify concentration of this compound in any biological matrix. The purpose of this study was 1) to develop and validate a new bioanalytical method using a micro-extraction and LC-MS/MS to quantify the target analyte in mouse plasma and 2) to partially validate the method in whole blood. A bioanalytical method was developed and validated in both matrices for a linear concentration range of 2-1000 ng/ml. For both matrices, the reverse predicted concentration of calibration standards (-8.95% to 12.16% and -9.54% to 12.90% respectively) and precision and accuracy (QCs) were within ±15% (%RSD and %BIAS). Four-hour bench top stability and post preparative stability results for plasma and whole blood matrices were within ±15% and ±20% respectively. Blood –plasma concentration correlation co-efficient was 0.9956 with a slope value of 1.018.
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3

Gunay, Neset Batuhan. "Studies Directed Towards The Synthesis Of Imatinib Mesylate ((gleevec), 4-(4-methyl-piperazin-1- Ylmethyl)-n-[4- Methyl-3-(4-pyridin-3-yl-pyrimidin-2- Ylamino)-phenyl]- Benzamide Methanesulfonate) Analogs." Master's thesis, METU, 2008. http://etd.lib.metu.edu.tr/upload/12610181/index.pdf.

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Анотація:
Imatinib mesylate is indicated for the treatment of chronic myeloid leukemia (CML) and unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST). By the application of this anticancer drug, problems occurs in terms of stability and activity. Computer assisted design (CAD) works showed that the modification of the B and C part molecule can increase the effectivity of the drug. The new derivatives of the drug will be obtained to change some part of the B and C segments. The total synthesis of a new imatinib mesylate will be done and the activity tests are going to be determined in collaboration with other groups.
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Тези доповідей конференцій з теми "Benzamidine analogues"

1

Kim, Joongsoo, Rakesh Kumar, and Jung-Mo Ahn. "Tris-Benzamide Analogs for Inhibiting Bcl-2 Proteins in Prostate Cancer." In The 24th American Peptide Symposium. Prompt Scientific Publishing, 2015. http://dx.doi.org/10.17952/24aps.2015.170.

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2

SHEN, Li-wen, Yan-ling WU, Min CHEN, Yoshimasa Tanaka, and Wen ZHANG. "Anti-Proliferative Activity of Benzamide Analogs in A549 Tumor Cells in Vitro." In 2nd International Conference on Biomedical and Biological Engineering 2017 (BBE 2017). Paris, France: Atlantis Press, 2017. http://dx.doi.org/10.2991/bbe-17.2017.32.

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