Delving into the Latest Updates on Nonpeptide cyclic ureas(DuPont Merck Pharmaceutical) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

HIV-1 protease

Action

inhibitors

Mechanism

HIV-1 protease inhibitors(HIV protease inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

HIV Infections

Inactive Indication-

Originator Organization

DuPont Merck Pharmaceutical Co.

Active Organization

DuPont Merck Pharmaceutical Co.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Jackson, David A. ; Otto, Michael J. ; Chang, Chong-Hwan ; Meek, James L. ; Rayner, Marlene M. ; Jadhav, Prabhakar K. ; Eyermann, Charles J. ; Hodge, C. Nicholas ; Ru, Yu ; Erickson-Viitanen, Susan ; Sharpe, Thomas R. ; Bacheler, Lee T. ; Lam, Patrick Y. S. ; Wong, Y. Nancy ; Weber, Patricia C.

Mechanistic information and structure-based design methods have been used to design a series of nonpeptide cyclic ureas that are potent inhibitors of human immunodeficiency virus (HIV) protease and HIV replication. A fundamental feature of these inhibitors is the cyclic urea carbonyl oxygen that mimics the hydrogen-bonding features of a key structural water molecule. The success of the design in both displacing and mimicking the structural water molecule was confirmed by x-ray crystallographic studies. Highly selective, preorganized inhibitors with relatively low molecular weight and high oral bioavailability were synthesized.

100 Deals associated with Nonpeptide cyclic ureas(DuPont Merck Pharmaceutical)

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