Efficient synthesis and identification of novel propane-1, 3-diamino bridged CCR5 antagonists with variation on the basic center carrier

X Fan, HS Zhang, L Chen, YQ Long

Index: Fan, Xing; Zhang, Hu-Shan; Chen, Li; Long, Ya-Qiu European Journal of Medicinal Chemistry, 2010 , vol. 45, # 7 p. 2827 - 2840

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Citation Number: 10

Abstract

By employing pharmacophore-based design and the privileged fragments reassembly, a series of piperidine-/tropane-/piperazine-bridged CCR5 antagonists were designed and synthesized via an efficient convergent synthesis strategy, with focus on the optimal choice of the basic center carrier structure. Significantly, the 4-amino-4-methylpiperidine bridged 1- acyl-1, 3-propanediamine compounds were identified as a new class of nanomolar CCR5 ...

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