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Scientia Pharmaceutica, Autorenhinweise 2015
Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
Open AccessArticle

Search for Compounds with Hypoglycemic Activity in the Series of 1-(2-(1H-Tetrazol-5-yl)-R1-Phenyl)-3-R2-phenyl(ethyl)ureas and R1-Tetrazolo[1,5-c]quinazolin-5(6H)-ones

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Department of Organic and Bioorganic Chemistry, Zaporizhzhya State Medical University, Mayakovsky 26 ave., 69035, Zaporizhzhya, Ukraine
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Department of Pharmacognosy, Pharmacology and Botany, Zaporizhzhya State Medical University, Mayakovsky 26 ave., 69035, Zaporizhzhya, Ukraine
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2016, 84(2), 233-254; https://doi.org/10.3797/scipharm.1507-14
Received: 17 July 2015 / Accepted: 10 October 2015 / Published: 10 October 2015
Methods of 1-[2-(1H-tetrazol-5-yl)-R1-phenyl]-3-R2-phenyl(ethyl)ureas and R1-tetrazolo[1,5-c]quinazolin-5(6H)-ones synthesis were designed. IR, LC-MS, 1H NMR, and elemental analysis data evaluated the structure and purity of the obtained compounds. Different products, depending on the reaction conditions, were distinguished and discussed. The preliminary hypoglycemic activity of 36 synthesized compounds was revealed. Docking studies to 11β-hydroxysteroid dehydrogenase 1, γ-peroxisome proliferator-activated receptor, and dipeptidyl peptidase-4 were conducted. Eight of these substances were further tested on glucocorticoid-induced insulin resistance models, namely glucose tolerance, oral rapid insulin, and adrenalin tests. One of the most active compounds turned out to be tetrazolo[1,5-c]quinazolin-5(6H)-one 3.1, exceeding the reference drugs Metformin (50 and 200 mg/kg) and Gliclazide (50 mg/kg).
Keywords: 1-[2-(1H-Tetrazol-5-yl)-R1-phenyl]-3-R2-phenyl(ethyl)ureas; Cyclization; Hypoglycemic activity; Molecular docking; Synthesis 1-[2-(1H-Tetrazol-5-yl)-R1-phenyl]-3-R2-phenyl(ethyl)ureas; Cyclization; Hypoglycemic activity; Molecular docking; Synthesis
MDPI and ACS Style

ANTYPENKO, O.M.; KOVALENKO, S.I.; ZHERNOVA, G.О. Search for Compounds with Hypoglycemic Activity in the Series of 1-(2-(1H-Tetrazol-5-yl)-R1-Phenyl)-3-R2-phenyl(ethyl)ureas and R1-Tetrazolo[1,5-c]quinazolin-5(6H)-ones. Sci. Pharm. 2016, 84, 233-254.

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