Synthesis and antimicrobial studies of new thiadiazoline based symmetrical bisheterocyclics

Mohamad Yusuf; Payal Jain

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Synthesis and antimicrobial studies of new thiadiazoline based symmetrical bisheterocyclics

机译：基于新型噻二唑啉的对称双环杂环化合物的合成与抗菌研究

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The bisheterocyclic compounds 4a-4h have been prepared in good yields from the cyclization of bisthiosemicarbazones 3a-3h with acetic anhydride. The condensation reaction of bisacetophenones 2a-2h with thiosemicarbazide in alcoholic medium provided 3a-3h and the former were obtained from the O-alkylation of 4- hydroxyacetophenone with suitable 1,ω-dibromoalkanes under alkaline conditions in the presence of dry EtOH/DMF. The intermediates 3a-3h and bisthiadiazolines 4a-4h were also screened for their in vitro antimicrobial activities. Most of the compounds showed significant activity against the tested microorganisms.

机译：从双硫代半氨基甲酮3a-3h与乙酸酐的环化反应已经以高收率制备了双环化合物4a-4h。双苯乙酮2a-2h与硫代氨基脲在酒精介质中的缩合反应提供3a-3h，前者是在碱性条件下，在干燥的EtOH / DMF存在下，由4-羟基苯乙酮与合适的1，ω-二溴链烷烃进行O-烷基化反应而获得的。还对中间体3a-3h和双噻二唑啉4a-4h的体外抗菌活性进行了筛选。大多数化合物对被测微生物表现出显着的活性。

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《Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry》 |2012年第4期|共9页
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Mohamad Yusuf; Payal Jain;
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Synthesis and antimicrobial studies of new thiadiazoline based symmetrical bisheterocyclics

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