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  • Title: Antagonists of slow-reacting substance of anaphylaxis. 1. Pyrido[2,1-b]quinazolinecarboxylic acid derivatives.
    Author: Tilley JW, Levitan P, Welton AF, Crowley HJ.
    Journal: J Med Chem; 1983 Nov; 26(11):1638-42. PubMed ID: 6313920.
    Abstract:
    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.
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