Molecular modeling study and synthesis of quinazolinone-arylpiperazine derivatives as α 1-adrenoreceptor antagonists

SM Abou-Seri, K Abouzid, DAA El Ella

Index: Abou-Seri, Sahar Mahmoud; Abouzid, Khaled; Abou El Ella, Dalal A. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 2 p. 647 - 658

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Citation Number: 30

Abstract

Three series of new 2-[(4-substituted piperazin-1-yl) methyl] quinazolin-4 (3H)-ones 4a–c, Ethyl 6, 7-dimethoxy-4-oxo-3-[2-(4-substituted piperazin-1-yl) acetamido/propanamido]-3, 4- dihydroquinazoline-2-carboxylates 9a–f and their 2-methyl analogues 13a–l were designed and synthesized as promising α1-adrenoceptor antagonists. The final compounds were evaluated for their in vivo hypotensive activity in normotensive cats. The most potent ...