PMID: 7538590May 12, 1995Paper

Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase

Journal of Medicinal Chemistry
P G WyattD C Humber

Abstract

A series of benzophenone derivatives has been synthesized and evaluated as inhibitors of HIV-1 reverse transcriptase (RT) and the growth of HIV-1 in MT-4 cells. Through the use of the structure-activity relationships within this series of compounds and computational chemistry techniques, a binding conformation is proposed. The SAR also indicated that the major interactions of 1h with the RT enzyme are through hydrogen bonding of the amide and benzophenone carbonyls and pi-orbital interactions with the benzophenone nucleus and an aromatic function separated from the benzophenone by a suitable spacer group. The crystal structure of compound 1h has been determined. A number of compounds with potent inhibitory activity against HIV-1 RT and HIV in cellular assays at levels comparable with AZT and our efforts to identify a metabolically stable analogue are described.

Citations

Nov 16, 2002·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·M W Nader, F Oberdorfer
Apr 5, 2011·Expert Opinion on Therapeutic Patents·Peng Zhan, Xinyong Liu
May 6, 2006·Rapid Communications in Mass Spectrometry : RCM·Feng Wang
Dec 14, 2018·MedChemComm·Khemchand SuranaSatyasheel Sharma
Sep 30, 2004·Bioorganic & Medicinal Chemistry Letters·Elizabeth A JeffersonEric E Swayze
Jun 3, 2020·The Journal of Organic Chemistry·Zhou TongRenhua Qiu
Feb 20, 2004·Journal of Medicinal Chemistry·Joseph H ChanLawrence R Boone
Feb 3, 2006·Journal of Medicinal Chemistry·Santiago VilarEugenio Uriarte
May 1, 1996·Journal of Chemical Information and Computer Sciences·D BarnumP Sprague
Jul 28, 2009·Bioorganic & Medicinal Chemistry·Dhaval G PrajapatiRajani Giridhar
Oct 12, 2021·Journal of Biomolecular Structure & Dynamics·Shashank M PatilV Lakshmi Ranganatha

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