Bioorganic & Medicinal Chemistry Letters 2012-01-01

Inhibition of noroviruses by piperazine derivatives.

Dengfeng Dou, Guijia He, Sivakoteswara Rao Mandadapu, Sridhar Aravapalli, Yunjeong Kim, Kyeong-Ok Chang, William C Groutas

Index: Bioorg. Med. Chem. Lett. 22(1) , 377-9, (2012)

Full Text: HTML

Abstract

There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to the identification of two promising compounds (6a and 9l) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.Copyright © 2011 Elsevier Ltd. All rights reserved.

Related Compounds

  • N-Boc-piperazine

Related Articles:

Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.

2014-04-01

[J. Enzyme Inhib. Med. Chem. , (2013)]

Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.

2004-06-07

[Bioorg. Med. Chem. Lett. 14 , 2857-2862, (2004)]

Molecular iodine-catalyzed facile procedure for N-Boc protection of amines.

2006-10-13

[J. Org. Chem. 71 , 8283, (2006)]

1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.

2004-05-20

[J. Med. Chem. 47 , 2833-2838, (2004)]

Efficient copper-catalyzed cross-coupling of 1-Boc-piperazine with aryl iodides and its application in the synthesis of trazodone. Yong FF, et al.

[Tetrahedron Lett. 54(39) , 5332-34, (2013)]

More Articles...