N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Mitchell ML, Son JC, Lee IY, Lee CK, Kim HS, Guo H, Wang J, Hayes J, Wang M, Paul A, Lansdon EB, Chen JM, Eisenberg G, Geleziunas R, Xu L, Kim CU
Bioorganic & medicinal chemistry letters (2010), Volume 20, Page 1585
PubMed entry Publisher's site

Abstract:

A series of N1-heterocyclic pyrimidinediones were extensively ...
A series of N1-heterocyclic pyrimidinediones were extensively evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Inhibitor 1 is active against NNRTI-resistant viruses including RT mutant K103N. The co-crystal structure of inhibitor 1 with HIV-1 RT revealed that H-bonds are formed with K101 and K103. Efforts to improve the suboptimal pharmacokinetic profile of 1 resulted in the discovery of compound 13, which represents the lead compound in this series with improved pharmacokinetics and similar potency as inhibitor 1.

Polymerases:

HIV RT,HIV RT K103N

Topics:

Structure and Structure/Function, Reverse Transcriptase

Status:

new topics/pols set partial results complete validated

Results:

Polymerase Reference Property Result Context
HIV RT K103N N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. Reverse Transcriptase Activity Yes
HIV RT N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. Reverse Transcriptase Activity Yes
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Structures:

3LAK

Version:20241007

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