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The search for potent, small molecule NNRTIs: A review.

Abstract：

:AIDS has become the leading pandemic disease, and is the cause of death worldwide. Presently, HAART treatment, a combination of reverse transcriptase (RT) and protease inhibitors is also unsuccessful due to the virus getting resistant to the drugs because of mutational changes. Two types of RT inhibitors exist namely nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). The NNRTIs which bind to an allosteric site on RT are an important arsenal of drugs against HIV-1. The specificity of NNRTIs towards HIV-1 has led to extensive structural and molecular modelling studies of enzyme complexes and chemical synthesis of second and third-generation NNRTIs. The major drawbacks of NNRTIs are generation of resistance and pharmacokinetic problems. By mutational studies of non-nucleoside inhibitor binding pocket (NNIBP) some amino acids which were found to play an important role in proper binding resulted less prone to mutation. In this review we present a chronological history of NNRTI development, also highlighting the need for small molecules belonging to the NNRTI class for the management of AIDS.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Prajapati DG,Ramajayam R,Yadav MR,Giridhar R

doi

10.1016/j.bmc.2009.06.060

subject

Has Abstract

pub_date

2009-08-15 00:00:00

pages

5744-62

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00613-0

journal_volume

17

pub_type

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