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异吲哚酮噻唑啉杂化物作为HIV-1逆转录酶的双重抑制剂

Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase.

作者信息

Meleddu Rita, Distinto Simona, Corona Angela, Tramontano Enzo, Bianco Giulia, Melis Claudia, Cottiglia Filippo, Maccioni Elias

机构信息

a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.

b Department of Life and Environmental Sciences , University of Cagliari, Cittadella Universitaria di Monserrato , Cagliari , Italy.

出版信息

J Enzyme Inhib Med Chem. 2017 Dec;32(1):130-136. doi: 10.1080/14756366.2016.1238366. Epub 2016 Oct 21.

DOI:10.1080/14756366.2016.1238366
PMID:27766892
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6010014/
Abstract

A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse Transcriptase) associated functions. These derivatives are analogs of previously reported series whose biological activity and mode of action have been investigated. In this work we investigated the influence of the introduction of a methyl group in the position 3 of the dihydrothiazole ring and of a chlorine atom in the position 5 of the isatin nucleus. The new synthesized compounds are active towards both DNA polymerase and ribonuclease H in the µM range. The nature of the aromatic group in the position 4 of the thiazole was relevant in determining the biological activity.

摘要

设计并合成了一系列3-3-{2-[2-(3-甲基-4-苯基-2,3-二氢-1,3-噻唑-2-亚基)肼基-1-亚基]-2,3-二氢-1H-吲哚-2-酮衍生物，以研究它们对HIV-1（人类免疫缺陷病毒1型）逆转录酶（RT）相关功能的活性。这些衍生物是先前报道系列的类似物，其生物活性和作用方式已得到研究。在这项工作中，我们研究了在二氢噻唑环的3位引入甲基和在异吲哚酮核的5位引入氯原子的影响。新合成的化合物在微摩尔范围内对DNA聚合酶和核糖核酸酶H均具有活性。噻唑4位芳香基团的性质对确定生物活性至关重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/f60d49cd6e7a/IENZ_A_1238366_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/6bafe7d5bf62/IENZ_A_1238366_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/f5abf07a3a60/IENZ_A_1238366_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/f60d49cd6e7a/IENZ_A_1238366_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/6bafe7d5bf62/IENZ_A_1238366_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/f5abf07a3a60/IENZ_A_1238366_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/014a/6010014/f60d49cd6e7a/IENZ_A_1238366_F0003_C.jpg

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