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Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.

Abstract：

:A molecular hybridization approach is a powerful tool in the design of new molecules with improved affinity and efficacy. In this context, a series of diarylpyrimidine-quinolone hybrids were synthesized and evaluated against both wt HIV-1 and mutant viral strains. The most active hybrid 5a displayed an EC50 value of 0.28±0.07μM against HIV-1 IIIB. A couple of enzyme-based assays clearly pinpoint a RT-targeted mechanism of action. Docking studies revealed that these hybrids could be well located in the NNIBP of HIV-1 RT despite the bulky and polar properties of a quinolone 3-carboxylic acid moiety in the molecules.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Mao TQ,He QQ,Wan ZY,Chen WX,Chen FE,Tang GF,De Clercq E,Daelemans D,Pannecouque C

doi

10.1016/j.bmc.2015.03.037

subject

Has Abstract

pub_date

2015-07-01 00:00:00

pages

3860-8

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00221-7

journal_volume

23

pub_type

杂志文章

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