PMID: 9647603Jul 1, 1998Paper

Chemistry and structure--activity relationships of leukotriene receptor antagonists

American Journal of Respiratory and Critical Care Medicine
P R Bernstein

Abstract

Several strategies have been employed by medicinal chemists in the design of potent and selective leukotriene receptor antagonists-leukotriene structural analogs, FPL 55712 analogs, and random screening of corporate compound banks. Lead compounds were optimized, often through the exchange of ideas with groups working on other chemical series of leukotriene antagonists. Pranlukast can likely be traced to a lead compound identified by random screening that was initially modified by incorporating structural components present in FPL 55712. Montelukast originated from an early quinoline lead, which was modified with leukotriene structural elements. Zafirlukast is based on a lead compound that incorporated structural components from both FPL 55712 and the leukotrienes. Therefore, each medicinal chemistry strategy that was originally employed has successfully identified clinically effective leukotriene receptor antagonists.

Related Concepts

Related Feeds

American Thoracic Association Journals

Discover the latest respiratory research published by the journals from the American Thoracic Society.

Related Papers

American Journal of Respiratory and Critical Care Medicine
P R Bernstein
Mini Reviews in Medicinal Chemistry
Paolo Montuschi
Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology
Jeanne E LoughlinEric S Johnson
Tidsskrift for den Norske lægeforening : tidsskrift for praktisk medicin, ny række
Hilde Berner HammerStig S Frøland
© 2022 Meta ULC. All rights reserved