Synthesis, antileishmanial activity and docking study of N′-substitutedbenzylidene-2-(6,7-dihydrothieno[3,2-c] pyridin-5(4H)-yl) acetohydrazides

被引：28
作者：
Sangshetti, Jaiprakash N. [1 ]
Shaikh, Rehan I. [1 ]
Khan, Firoz A. Kalam [1 ]
Patil, Rajendra H. [2 ]
Marathe, Sayali D. [2 ]
Gade, Wasudev N. [2 ]
Shinde, Devanand B. [3 ]
机构：
[1] YB Chavan Coll Pharm, Aurangabad 431001, MS, India
[2] Univ Pune, Dept Biotechnol, Pune 411007, MS, India
[3] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem Technol, Aurangabad 431004, MS, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 06期
关键词：
Thieno[3,2-c] pyridine; Antileishmanial activity; L. donovani promastigotes; Antimicrobial activity; Docking study; ADME properties; ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; VISCERAL LEISHMANIASIS; DERIVATIVES; CHEMOTHERAPY; DISCOVERY; ANALOGS; DESIGN; ASSAY;
D O I：
10.1016/j.bmcl.2014.01.035
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of N '-substitutedbenzylidene-2-(6,7-dihydrothieno[ 3,2-c] pyridin-5(4H)-yl) acetohydrazide derivatives is synthesized and evaluated for antileishmanial activity against Leishmania donovani promastigotes. Compounds 9a and 9i were shown significant antileishmanial when compared with standard sodium stilbogluconate. Antimicrobial study revealed that compound 9b has potent as well as broad spectrum antibacterial activity when compared with ampicillin and compound 9e showed promising antifungal activity when compared with miconazole. Also, none of the synthesized compounds showed cytotoxicity up to tested concentration. Further, docking study against pteridine reductase 1 enzyme of L. donovani showed good binding interactions. ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates. (C) 2014 Elsevier Ltd. All rights reserved.
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收藏
页码：1605 / 1610
页数：6
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