Antihistaminic and other biological activities of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine

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• 作者：M. Saeed Arayne^a ; ^{msarayne@gmail.com} ; Najma Sultana^b ; Hina Shehnaz^c ; ^{hinashehnaz@gmail.com} ; Saf-ur-Rehman Mandukhail^d ; Anwarul Hassan Gilani^d ; Amir Haider^a
• 关键词：Fexofenadine ; Anticholinergic activity ; Carboxyterfenadine
• 刊名：Arabian Journal of Chemistry
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：10
• 期：1
• 页码：114-120
• 全文大小：1303 K
• 卷排序：10

文摘

In the present study the 2-methylpropanamide and benzamide derivatives of carboxyterfenadine, have been synthesized by nucleophilic substitution at carboxylic acid moiety (C-33) of tertiary carbon C-19 substituted with benzene ring. The proficient and high yielding series was carried out in two steps by continuous monitoring with TLC. The carboxylic group was utilized in the formation of 2-methylpropanamide and benzamide derivatives of carboxyterfenadine. The derivatives were characterized by spectroscopic techniques including mass. The starting material (2-[4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidino]butyl]phenyl]-2-methylpropanoic acid) itself is H1 receptor antagonist. Hence, all these compounds A–E were biologically evaluated for antihistaminic and anticholinergic activity, using isolated guinea pig ileum tissues.