Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
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.
Walser
A
A
Chemistry Research Department, Roche Research Center, Hoffmann-La Roche Inc., Nutley, New Jersey 07110.
Flynn
T
T
Mason
C
C
Crowley
H
H
Maresca
C
C
O'Donnell
M
M
D000818:Animals; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D007202:Indicators and Reagents; D008168:Lung / Q000187:drug effects / Q000502:physiology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D001381:Azepines; D007202:Indicators and Reagents; D010972:Platelet Activating Factor; D013876:Thiophenes; D014230:Triazoles; C052518:WEB 2086