Antagonists of slow-reacting substance of anaphylaxis. 1. Pyrido[2,1-b]quinazolinecarboxylic acid derivatives.
Members of a series of basic amide and ester derivatives of 2-substituted pyrido[2,1-b]quinazoline-8-carboxylic acids were prepared and evaluated for their ability to prevent slow-reacting substance of anaphylaxis (SRS-A) induced contractions of guinea pig ilea. The results indicate that the presence of a branched-chain alkyl group in the 2-position and a sterically demanding substituted aminoethyl carboxylate or carboxamide in the 8-position give optimal in vitro activity. The phenylpiperazine 25 was further found to block SRS-A-related symptomatology after intravenous administration in two animal models.
D000818:Animals; D001681:Biological Assay; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007202:Indicators and Reagents; D017999:Leukotriene E4; D009119:Muscle Contraction / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013189:SRS-A / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D011799:Quinazolines; D013189:SRS-A; D017999:Leukotriene E4