Structure-activity relationship studies of CNS agents. Part 29. N-Methylpiperazino-substituted derivatives of quinazoline, phthalazine and quinoline as novel α 1, 5-HT …

…, B Duszyńska, S Charakchieva-Minol…

Index: Mokrosz; Duszynska; Charakchieva-Minol; Bojarski; Wydra; Janda; Strekowski European Journal of Medicinal Chemistry, 1996 , vol. 31, # 12 p. 973 - 980

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Citation Number: 21

Abstract

New N-methylpiperazino-substituted quinazolines 8 and 9, phthalazine 13, and quinoline 19 have been synthesized. The receptor binding profiles (α1, 5-HT1A, 5-HT2A) of these compounds and their analogs (7–22) have been determined. It has been demonstrated that orientation of a local dipole moment of the heteroaromatic ring system affects both the α1 and 5-HT2A affinity of the investigated class of ligands. Distortion of the coplanar unfused ...