Synthesis and Structure-Activity relationship of 1-(5-isoquinolinesulfonyl)piperazine analogues as inhibitors of Mycobacterium tuberculosis IMPDH
Vinayak Singh, Angela Pacitto, Stefano Donini, Davide M Ferraris, Sandor Boros, Eszter Illyes, Balint Szokol, Menico Rizzi, Tom L Blundell, David B Ascher, Janos Pato, Valerie Mizrahi
European Journal of Medicinal Chemistry | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | Published : 2019
Awarded by European Community's Seventh Framework Programme
Awarded by Jack Brockhoff Foundation
Awarded by C.J. Martin Research Fellowship from the National Health and Medical Research Council of Australia
Awarded by Fundacao de Amparo a Pesquisa do Estado de Minas Gerais
This work was supported by the European Community's Seventh Framework Programme (Grant 260872, More Medicines for Tuberculosis); the Howard Hughes Medical Institute (Senior International Research Scholar's grant to V.M.); the National Research Foundation of South Africa (to V.M.); and the South African Medical Research Council (to V.M.). D.B.A was funded by the Jack Brockhoff Foundation (JBF 4186, 2016), a C.J. Martin Research Fellowship from the National Health and Medical Research Council of Australia (APP1072476), and the Department of Biochemistry, University of Melbourne. D.B.A. and T.L.B received funding from the Newton Fund RCUK-CONFAP Grant awarded by The Medical Research Council and Fundacao de Amparo a Pesquisa do Estado de Minas Gerais (MR/M026302/1). A.P and T.L.B were funded by the Bill and Melinda Gates Foundation. Special thanks to Gyorgyi Farkas (Vichem) for the technical assistance. We also thank medicinal chemists of Drug Discovery & Development Centre (H3D), University of Cape Town for the discussions.