New Cyclohexylamine-dithiocarbamate Derivatives as Potential Anti-microbial Agents

被引：1

作者：

Yurttas, Leyla ^{[1
]}

Kaya, Betul ^{[1
]}

Cankilic, Meral Yilmaz ^{[2
]}

Levent, Serkan ^{[1
]}

机构：

[1] Anadolu Univ, Dept Pharmaceut Chem, Fac Pharm, TR-26470 Eskisehir, Turkey

[2] Anadolu Univ, Dept Biol, Fac Sci, TR-26470 Eskisehir, Turkey

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2017年 / 14卷 / 11期

关键词：

Dithiocarbamate; lipophilicity; antifungal activity; antibacterial activity; ADME; agents; ANTIBACTERIAL ACTIVITY; LIPOPHILICITY; DISCOVERY;

D O I：

10.2174/1570180814666170412121402

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: In this study, 2-(substituted-sulfanyl)-N, N-dicyclohexylacetamide derivatives (2a-2g) and 2-(dicyclohexylamino)-2-oxoethyl-1-substituted carbodithioate derivatives (2h-2m) were synthesized and screened for their antimicrobial activity. Methods: Newly synthesized compounds were screened against two gram negative bacteria (S. typhimurium and E. coli), three gram positive bacteria (S. aureus, B. cereus and L. monocytogenes), four Candida species, four Aspergillus spp. and three Penicillium spp. Among them (2a-2m), compounds 2i (2-(dicyclohexylamino)-2-oxoethyl-thiomorpholine-4-carbodithioate) and 2k (2( dicyclohexylamino)-2-oxoethyl-4-(4-methoxyphenyl) piperazine-1-carbodithioate) were detected to have higher inhibitory effect than other compounds. Results and Conclusion: Minumum inhibitor concentrations (MICs) of the compounds were determined between the range of 97.5-390 mu g/mL. Additionally, parameters determined that some physicochemical and toxic properties were predicted using computational methods.

引用

页码：1308 / 1315

页数：8

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