Structure-activity relationship studies of central nervous system (CNS) agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl) …

…, M Pietrasiewicz, B Duszynska, MT Cegla

Index: Mokrosz; Pietrasiewicz; Duszynska; Cegla Journal of Medicinal Chemistry, 1992 , vol. 35, # 13 p. 2369 - 2374

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Citation Number: 28

Abstract

The effect of the hydrocarbon chain of the model Csubstituted 1-(3-~ hlorophenyl) piperazines 12-31 on their affiiity for 5-HT1~ receptor sites was investigated. It was found that elongation of the 4-n-alkyl chain strongly increases the 5-HTu affity of the inveatigated compounds. The affinity reaches the maximum (Ki= 2.67 nM) for the n-hexyl derivative 20. It was shown that hydrophobic interactions of N-4 substituents of 1-arylpiperazines ...