Issue 8, 2012
From the journal:

MedChemComm

Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection†

Steven J. Moss,a   Michael Bobardt,b   Pieter Leyssen,c   Nigel Coates,‡a   Udayan Chatterji,b   Xie Dejian,d   Teresa Foster,‡a   Jinlun Liu,d   Mohammad Nur-e-Alam,‡a   Dipen Suthar,‡a   Chen Yongsheng,d   Tony Warneck,‡a   Ming-Qiang Zhang,‡a   Johan Neyts,c   Philippe Gallay,b   Barrie Wilkinson‡a  and  Matthew A. Gregory‡*a  

* Corresponding authors

a Biotica Technology Ltd., Chesterford Research Park, Cambridge, UK
E-mail: matt.gregory@biotica.com
Fax: +01799 532921
Tel: +44 1799 532920

b Department of Immunology and Microbial Science, Scripps Research Institute, La Jolla, California, USA

c Rega Institute for Medical Research, K. U. Leuven, 3000 Leuven, Belgium

d Shanghai Chempartner Co., Zhangjiang Hi-tech Park, Pudong, Shanghai, China

Abstract

Sangamides are amide derivatives of sanglifehrin A, a cyclophilin-binding polyketide natural product which is structurally distinct from cyclosporine A. Cyclosporine A is the starting point for the synthesis of cyclophilin inhibitors such as alisporivir, currently in development for the treatment of HCV infection. We report here initial results of the optimisation program which led to identification of the sangamides, compounds that exhibit significantly improved potential for the treatment of chronic HCV infection.

Graphical abstract: Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection

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Article information

DOI
https://doi.org/10.1039/C1MD00227A
Article type
Concise Article
Submitted
06 Sep 2011
Accepted
02 Oct 2011
First published
21 Oct 2011

Med. Chem. Commun., 2012,3, 944-949

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Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection

S. J. Moss, M. Bobardt, P. Leyssen, N. Coates, U. Chatterji, X. Dejian, T. Foster, J. Liu, M. Nur-e-Alam, D. Suthar, C. Yongsheng, T. Warneck, M. Zhang, J. Neyts, P. Gallay, B. Wilkinson and M. A. Gregory, Med. Chem. Commun., 2012, 3, 944 DOI: 10.1039/C1MD00227A

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