Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase

L M Tillekeratne; A Sherette; P Grossman; L Hupe; D Hupe; R A Hudson

doi:10.1016/s0960-894x(01)00577-7

Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7. doi: 10.1016/s0960-894x(01)00577-7.

Authors

L M Tillekeratne¹, A Sherette, P Grossman, L Hupe, D Hupe, R A Hudson

Affiliation

¹ Department of Medicinal and Biological Chemistry, College of Pharmacy, University of Toledo, Toledo, OH 43606, USA.

PMID: 11591519
DOI: 10.1016/s0960-894x(01)00577-7

Abstract

Systematic simplification of the molecular structures of epicatechin gallate and epigallocatechin gallate to determine the minimum structural characteristics necessary for HIV-1 reverse transcriptase inhibition in vitro resulted in several compounds that strongly inhibited the native as well as the A17 double mutant (K103N Y181C) enzyme, which is normally insensitive to most known nonnucleoside inhibitors.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Catechin / analogs & derivatives*
Catechin / chemistry
Catechin / pharmacology*
HIV Reverse Transcriptase / antagonists & inhibitors*
HIV Reverse Transcriptase / genetics
Mutation
Reverse Transcriptase Inhibitors / chemistry
Reverse Transcriptase Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Reverse Transcriptase Inhibitors
catechin gallate
Catechin
epicatechin gallate
epigallocatechin gallate
HIV Reverse Transcriptase