Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles
Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay.
Lewis-acid Promoted Aromatic Cyclization of &α-Chlorosulfides: Synthesis of Ethyl Isothiochroman-1-carboxylate and Related Compounds
A variety of ethyl isothiochroman-1-carboxylates and related compounds were synthesized by treatment of 2-chloro-2-acetates with stannic chloride in methylene chloride.The same procedure was applied to the synthesis of ethyl 4-chloro-4-methyltetrahydrothiopyran-2-carboxylate.Some isothiochroman-1-carboxylic acids were prepared and evaluated for antiinflammatory activity.Among the compounds tested, 7-phenoxyisothiochroman-1-carboxylic acid showed weak activity.