Synthesis,anti-diabetic evaluation and molecular docking studies of 4-(1-aryl-1H-1, 2, 3-triazol-4-yl)-1,4-dihydropyridine derivatives as novel 11-β hydroxysteroid dehydrogenase-1 (11β-HSD1) inhibitors |
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| Institution: | 1. Department of Chemistry, University College of Science, Osmania University, Hyderabad, Telangana 500 007, India;2. Bio-organic & Medicinal Chemistry Research Division, Vishnu Institute of Pharmaceutical Education and Research (VIPER), Narsapur, Medak, Telangana 502 313, India;3. Department of Genetics and Biotechnology, University College of Science, Osmania University, Hyderabad, Telangana 500 007, India;1. Kolbe Laboratory of Organic Synthesis, School of Chemistry and Food, Federal University of Rio Grande-FURG, Rio Grande, RS, Brazil;2. Institute of Biological Sciences, Federal University of Rio Grande-FURG, Rio Grande, RS, Brazil;3. Laboratory of Organic Synthesis, Institute of Chemistry, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil;1. Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Str. 2+4, Berlin, 14195, Germany;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, S?hhiye, Ankara, 06100, Turkey;3. Department of Physiology & Pharmacology, Hotchkiss Brain Institute, University of Calgary, 3330 Hospital Drive NW, Calgary, T2N 4N1, Canada;1. Grupo de Pesquisa em Fotoquímica Orgânica Aplicada, Universidade Federal do Rio Grande do Sul – Instituto de Química, Av. Bento Gonçalves 9500, CEP 91501-970, Porto Alegre, RS, Brazil;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 S?hhiye, Ankara, Turkey;3. Grupo de Química Teórica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves 9500, CEP 91501-970, Porto Alegre, RS, Brazil;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ba?kent University, 06790 Ba?l?ca, Ankara, Turkey;1. Chemistry Department, Production Technology Research Institute -ACECR, Ahvaz, Iran;2. Young Researchers and Elites Club, Science and Research Branch, Islamic Azad University, Tehran, Iran;3. Chemistry Department, Omidiyeh Branch of Islamic Azad University, Omidiyeh, Iran |
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| Abstract: | 11-Beta-Hydroxysteroid dehydrogenase-1(11β-HSD1) inhibitors are one of the emerging classes of molecules to fight against diabetic complications. A novel series of 4-(1-substituted-1H-1,2,3-triazol-4-yl)-1,4-dihydropyridine derivatives were synthesized and evaluated for their anti-diabetic activity. Two compounds showed anti-diabetic activity very effectively. To clarify the mechanism of action of these compounds, the most potent compounds (5g and 5h) of the synthesized analogs were further studied by testing its 11-Beta Hydroxysteroid dehydrogenase-1 inhibitory activity through in vitro enzymatic experiments. The results showed that the 11β-HSD1 inhibitory activity of compounds 5g and 5h was stable and efficient. Molecular docking studies revealed compounds 5g (?9.758) and 5h (?8.495) to have a stable binding patterns to the human 11-Beta-Hydroxysteroid dehydrogenase-1. |
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| Keywords: | 11-BetaHydroxysteroid dehydrogenase-1(11β-HSD1) inhibitors 1 4-dihydropyridine 1 2 3–Triazole Diabetic agents and molecular docking studies |
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