Discovery and optimization of indole pyrrolothiazole paf antagonists

Abstract 3-(3-Pyridinyl)-7-(indol-3-ylcarbonyl)-1 H -3 H -pyrrolo[1,2-c]thiazoles represent a new class of platelet activating factor antagonists. This series was discovered by combining the indole portion of a previous thiazolidine series with the known 3-pyridinyl-pyrrolothiazole pharmacophore. Optimization of the indole substituents resulted in the identification of 8i as one of the most potent PAF antagonists yet described.