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Design, synthesis and molecular docking of pyrazolo [3,4d] thiazole hybrids as potential anti-HIV-1 NNRT inhibitors.

Abstract：

:A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via the formation of 2-imino-3-(4-substituted-arylthiazol-2-yl)-thiazolidin-4-ones 3 using substituted aldehydes 4. The 5-acrylidene derivative 5 on cyclisation with phenyl hydrazine give the pyrazolo [3, 4, d] thiazole derivatives 6. The obtained pyrazolo [3.4, d]thiazole derivatives were studied as anti-HIV-1 NNRT inhibitors. It was found that these compounds might have potent RT inhibition activity.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Kasralikar HM,Jadhavar SC,Goswami SV,Kaminwar NS,Bhusare SR

doi

10.1016/j.bioorg.2019.02.006

subject

Has Abstract

pub_date

2019-05-01 00:00:00

pages

437-444

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30978-7

journal_volume

86

pub_type

杂志文章

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