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New N-(2-phenyl-4-oxo-1,3-thiazolidin-3-yl)-1,2-benzothiazole-3-carboxamides and acetamides as antimicrobial agents
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-11-03 00:00:00 , DOI: 10.1039/c7md00334j Matteo Incerti 1 , Paola Vicini 1 , Athina Geronikaki 2 , Phaedra Eleftheriou 3 , Athanasios Tsagkadouras 3 , Panagiotis Zoumpoulakis 4 , Charalmpos Fotakis 4 , Ana Ćirić 5 , Jasmina Glamočlija 5 , Marina Soković 5
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-11-03 00:00:00 , DOI: 10.1039/c7md00334j Matteo Incerti 1 , Paola Vicini 1 , Athina Geronikaki 2 , Phaedra Eleftheriou 3 , Athanasios Tsagkadouras 3 , Panagiotis Zoumpoulakis 4 , Charalmpos Fotakis 4 , Ana Ćirić 5 , Jasmina Glamočlija 5 , Marina Soković 5
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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 μmol mL−1 × 10−2 and MBC of 21.4–40.2 μmol mL−1 × 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.
中文翻译：
新型 N-(2-phenyl-4-oxo-1,3-thiazolidin-3-yl)-1,2-benzothiazole-3-carboxamides 和 acetamides 作为抗菌剂
一系列 21 种新型N- [2-phenyl-4-oxo-1,3-thiazolidin-3-yl]-1,2-benzothiazole-3-carboxamides/acetamides ( 4a–4p ) 以及一系列N '-(halophenylmethylidene)-1,2-benzothiazole-3-acetohydrazides ( 3h-3p ) 已经合成并评估了它们对八种细菌和八种真菌物种的抗菌活性，其中包括植物、动物和人类病原体以及食品污染物种。所有化合物似乎都是有效的，化合物4d表现出最佳活性，MIC 在 10.7-21.4 μmol mL -1 × 10 -2范围内，MBC 为 21.4-40.2 μmol mL -1 × 10 -2. 化合物4p和3h的抗真菌活性最好。还对合成化合物的抗微生物活性和分子性质之间的关系进行了阐明。还测试了合成中间体，其中几种表现出良好的抗微生物活性。对一些化合物进行了对接研究。
更新日期：2017-11-05
中文翻译：
新型 N-(2-phenyl-4-oxo-1,3-thiazolidin-3-yl)-1,2-benzothiazole-3-carboxamides 和 acetamides 作为抗菌剂
一系列 21 种新型N- [2-phenyl-4-oxo-1,3-thiazolidin-3-yl]-1,2-benzothiazole-3-carboxamides/acetamides ( 4a–4p ) 以及一系列N '-(halophenylmethylidene)-1,2-benzothiazole-3-acetohydrazides ( 3h-3p ) 已经合成并评估了它们对八种细菌和八种真菌物种的抗菌活性，其中包括植物、动物和人类病原体以及食品污染物种。所有化合物似乎都是有效的，化合物4d表现出最佳活性，MIC 在 10.7-21.4 μmol mL -1 × 10 -2范围内，MBC 为 21.4-40.2 μmol mL -1 × 10 -2. 化合物4p和3h的抗真菌活性最好。还对合成化合物的抗微生物活性和分子性质之间的关系进行了阐明。还测试了合成中间体，其中几种表现出良好的抗微生物活性。对一些化合物进行了对接研究。
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