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均三唑并[3,4-b]-1,3,4-噻二唑和 4-噻唑烷二酮衍生物的合成及抑菌活性。

Synthesis and antibacterial activity of some novel bis-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and bis-4-thiazolidinone derivatives from terephthalic dihydrazide.

机构信息

Department of Fibres and Textile Processing Technology, Institute of Chemical Technology (Autonomous), University of Mumbai, N. Parekh Marg, Matunga, Mumbai 400019, Maharashtra, India.

出版信息

Eur J Med Chem. 2009 Dec;44(12):5112-6. doi: 10.1016/j.ejmech.2009.07.023. Epub 2009 Jul 30.

Abstract

A novel series of 1,4-bis(6-(substituted phenyl)-[1,2,4]-triazolo[3,4-b]-1,3,4-thiadiazoles (5a-b) and 4-bis(substituted phenyl)-4-thiazolidinone derivatives (7a-c) have been synthesized from terephthalic dihydrazide (1) through multistep reaction sequence. 1,4-Bis(5-aryl-1,3,4-oxadiazole-2yl) benzene derivatives (2a-f) and bis-substituted terephthalohydrazide (6a-e) were also synthesized from terephthalic dihydrazide by cyclization with various aromatic acids and aldehydes. Terephthalic dihydrazide (1) was obtained from poly(ethylene terephthalate) waste from reaction with hydrazine hydrate in good yield (86%). All the synthesized compounds were screened for their antibacterial activities against various bacteria and fungi strains. Several of these compounds showed potential antibacterial activity.

摘要

从对苯二甲酸二酰肼(1)出发,通过多步反应序列,合成了一系列新型的 1,4-双(6-(取代苯基)-[1,2,4]三唑并[3,4-b]-1,3,4-噻二唑(5a-b)和 4-双(取代苯基)-4-噻唑啉酮衍生物(7a-c)。还通过与各种芳香酸和醛的环化反应,从对苯二甲酸二酰肼(1)合成了 1,4-双(5-芳基-1,3,4-恶二唑-2-基)苯衍生物(2a-f)和双取代对苯二甲酰肼(6a-e)。对苯二甲酸二酰肼(1)是通过聚对苯二甲酸乙二醇酯(PET)与水合肼反应,以良好的收率(86%)得到的。所有合成的化合物都进行了抗菌活性筛选,以评估它们对各种细菌和真菌菌株的抑制作用。其中一些化合物表现出潜在的抗菌活性。

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