Synthesis and Analgesic Activity of Some Side-Chain Modified Anpirtoline Derivatives

Abstract

New derivatives of anpirtoline and deazaanpirtoline modified in the side chain have been synthesized. The series includes compounds3with side‐chains containing piperidine or pyrrolidine rings, compounds4containing 8‐azabicyclo[3.2.1]octane moiety, and compounds5having piperazine ring in their side‐chains. Their receptor binding profiles (5‐HT1A, 5‐HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Optimized structures (PM3‐MOPAC, Alchemy 2000, Tripos Inc.) of the synthesized compounds3—5were compared with that of anpirtoline