New N-(2-phenyl-4-oxo-1,3-thiazolidin-3-yl)-1,2-benzothiazole-3-carboxamides and acetamides as antimicrobial agents

被引：7

作者：

Incerti, Matteo ^{[1
]}

Vicini, Paola ^{[1
]}

Geronikaki, Athina ^{[2
]}

Eleftheriou, Phaedra ^{[3
]}

Tsagkadouras, Athanasios ^{[3
]}

Zoumpoulakis, Panagiotis ^{[4
]}

Fotakis, Charalmpos ^{[4
]}

Ciric, Ana ^{[5
]}

Glamoclija, Jasmina ^{[5
]}

Sokovic, Marina ^{[5
]}

机构：

[1] Univ Parma, Dipartimento Sci Alimenti & Farmaco, Parma, Italy

[2] Aristotle Univ Thessaloniki, Sch Pharm, Thessaloniki 54124, Greece

[3] Alexander Technol Educ Inst Thessaloniki, Sch Hlth & Med Care, Dept Med Lab Studies, Thessaloniki, Greece

[4] Natl Hellen Res Fdn, Inst Biol Med Chem & Biotechnol, 48 Vas Constantinou Ave, Athens 11635, Greece

[5] Univ Belgrade, Inst Biol Res, Dept Plant Physiol, Mycol Lab, Bulevar, Serbia

来源：

MEDCHEMCOMM | 2017年 / 8卷 / 11期

关键词：

BIOLOGICAL EVALUATION; ANTIFUNGAL ACTIVITY; DERIVATIVES; DOCKING; 4-THIAZOLIDINONES;

D O I：

10.1039/c7md00334j

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 21 novel N-[2-phenyl-4-oxo-1,3-thiazolidin-3-yl]-1,2-benzothiazole-3-carboxamides/acetamides (4a-4p) as well as a series of N'-(halophenylmethylidene)-1,2-benzothiazole-3-acetohydrazides (3h-3p) have been synthesized and evaluated for their antimicrobial activity against eight bacterial and eight fungal species, among them plant, animal and human pathogens and food contaminating species. All compounds appeared to be potent and the best activity was exhibited by compound 4d with MIC in the range of 10.7-21.4 mu mol mL(-1) x 10(-2) and MBC of 21.4-40.2 mu mol mL(-1) x 10(-2). The best antifungal activity was observed for compounds 4p and 3h. Elucidation of the relationship between the antimicrobial activity and molecular properties of the synthesized compounds was also performed. Synthetic intermediates were also tested with several exhibiting good antimicrobial activities. Docking studies for some compounds were performed.

引用

页码：2142 / 2154

页数：13

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