Synthesis and Biological Activities of 1-Acetyl-5-substituted Indoline Compounds

Chem. J. Chinese Universities ›› 2010, Vol. 31 ›› Issue (5): 970.

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Synthesis and Biological Activities of 1-Acetyl-5-substituted Indoline Compounds

CHEN Guo-Hua^1*, LUO Xiao-Chuan¹, ZHANG Jiang-Bo¹, HUANG Wen-Long²

1. Department of Medicinal Chemistry,
2. Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China

Received:2009-06-30 Online:2010-05-10 Published:2010-05-10
Contact: CHEN Guo-Hua. E-mail: cgh63@163.com

Abstract

Abstract:

As benign prostate hyperplasia(BPH) is a common disease in elderly men, it is urgent to find new α₁-adrenoceptor(AR) antagonists, the first choice for the therapy of BPH. On the basis of hybridization principle with 1-acetylindoline as the starting compound, two series of indoline derivatives 1-acetyl-5-{2-[4-(substituted phenoxy)ethyl]piperazin-1-yl}alkyl indoline and 1-acetyl-5-{2-[4-(substituted phenyl)piperazin-1-yl]alkyl} indoline were designed and synthesized. The structures of the target compounds were confirmed by ¹H NMR, elemental analysis, IR and MS. Preliminary pharmacological test show all the target compounds exhibit certain antagonism of α₁-AR. Compounds 9h and 12l perform better than piperazine, and are worth of further research.

Key words: Indoline; 1-(Substituted phenyl)piperazine; 1-[2-(Substituted phenoxy)ethyl]piperazine; Benign prostatic hyperplasia; α1-Adrenoceptor

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CHEN Guo-Hua*, LUO Xiao-Chuan, ZHANG Jiang-Bo, HUANG Wen-Long. Synthesis and Biological Activities of 1-Acetyl-5-substituted Indoline Compounds[J]. Chem. J. Chinese Universities, 2010, 31(5): 970.

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Synthesis and Biological Activities of 1-Acetyl-5-substituted Indoline Compounds

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