Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2017 Dec 21

PMID 29259750

Citations 14

Authors

Christopher J Bungard

Peter D Williams

Jurgen Schulz

Catherine M Wiscount

M Katharine Holloway

H Marie Loughran

Jesse J Manikowski

Hua-Poo Su

David J Bennett

Lehua Chang

Xin-Jie Chu

Alejandro Crespo

Michael P Dwyer

Kartik Keertikar

Gregori J Morriello

Andrew W Stamford

Sherman T Waddell

Bin Zhong

Bin Hu

Tao Ji

Tracy L Diamond

Carolyn Bahnck-Teets

Steven S Carroll

John F Fay

Xu Min

William Morris

Jeanine E Ballard

Michael D Miller

John A McCauley

Affiliations

Soon will be listed here.

Abstract

Using the HIV-1 protease binding mode of and as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core showed an 60-fold increase in enzyme binding affinity and a 10-fold increase in antiviral activity relative to .

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