Delving into the Latest Updates on BMS-183920 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

AT1R

Action

antagonists

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Hypertension

Originator Organization

Bristol Myers Squibb Co.

Active Organization-

Inactive Organization

Bristol Myers Squibb Co.

License Organization-

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC26H19N5O3

InChIKeyUVTFLTXWSSGYFE-UHFFFAOYSA-N

CAS Registry153072-33-4

Prodrug derivatization of a potent quinoline-4-carboxylic acid angiotensin II receptor antagonist was undertaken as an approach to achieve improved oral activity.A dioxolenone carboxylic ester and an alkylated tetrazole prodrug both showed greater oral antihypertensive activity in the salt-depleted spontaneously hypertensive rat and increased oral bioavailability relative to the parent compound

01 Jan 1994·BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Quinoline-4-carboxylic acids as angiotensin II receptor antagonists

Author: J.E. Bird ; S. Skwish ; T.L. Waldron ; D.E. Normandin ; S. Moreland ; E.R. Spitzmiller ; J. Buote ; T. Dejneka ; K.E.J. Dickinson ; C.L. Delaney ; D.E. Ryono ; J. Lloyd

The authors have synthesized a series of quinoline-4-carboxylic acids that are potent antagonists of the angiotensin II receptor.They show high binding affinities and functional antagonism in rabbit aortic strips.They are also effective in blocking the hypertensive effects of AII in vivo.

100 Deals associated with BMS-183920

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