Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2

A Walser; T Flynn; C Mason; H Crowley; C Maresca; M O'Donnell

doi:10.1021/jm00108a031

Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2

J Med Chem. 1991 Apr;34(4):1440-6. doi: 10.1021/jm00108a031.

Authors

A Walser¹, T Flynn, C Mason, H Crowley, C Maresca, M O'Donnell

Affiliation

¹ Chemistry Research Department, Roche Research Center, Hoffmann-La Roche Inc., Nutley, New Jersey 07110.

PMID: 2016721
DOI: 10.1021/jm00108a031

Abstract

The preparations of thienotriazolodiazepines bearing a substituted ethynyl group at the 2-position, and the corresponding cis-olefins and fully saturated analogues are described. The compounds were evaluated as potential antagonists of platelet-activating factor (PAF) in in vitro and in vitro test models. The new thienotriazolodiazepines are compared with known related compounds such as WEB 2086 (compound 6) and the phenylethyl derivatives 27 and 28.

Publication types

Comparative Study

MeSH terms

Animals
Azepines / chemical synthesis*
Azepines / chemistry
Azepines / pharmacology
Guinea Pigs
Indicators and Reagents
Lung / drug effects
Lung / physiology
Magnetic Resonance Spectroscopy
Molecular Structure
Platelet Activating Factor / antagonists & inhibitors*
Structure-Activity Relationship
Thiophenes / chemical synthesis*
Thiophenes / chemistry
Thiophenes / pharmacology
Triazoles / chemical synthesis*
Triazoles / chemistry
Triazoles / pharmacology

Substances

Azepines
Indicators and Reagents
Platelet Activating Factor
Thiophenes
Triazoles
WEB 2086