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Published in Canadian Journal of Chemistry - 01 Jan 2016

Stéphanie Petrella, Alexandra Aubry, Geneviève Janvier, Eloi Paul Coutant, Alex Cartier, Thuy-Ha Dao, Frédéric Bonhomme, Laurence Motreff, Cédric Pissis, Chantal Bizet, Dominique Clermont, Evelyne Begaud, Pascal Retailleau, Hélène Munier-Lehmann, Estelle Capton, Claudine Mayer, Yves Janin

Can. J. Chem. 2016, 94 , 240-250

A recently discovered series of inhibitors of the ATPase function of bacterial type IIA topoisomerases featuring a carboxypyrrole component led us to attempt to replace this group with a potentially bioisosteric carboxypyrazole. Accordingly, synthetic pathways to 2-(4-(1H-pyrazole-5-carboxamido)piperidin-1-yl)thiazole-5-carboxylic acids or 2-(4-(N-methyl-1H-pyrazole-5-carboxamido)piperidin-1-yl)thiazole-5-carboxylic acids featuring an array of substituents on the pyrazole ring were explored. Unfortunately, none of the analogues made were effective on the ATPase function of Mycobacterium tuberculosis gyrase, as well on the DNA supercoiling activity of the whole gyrase of M. tuberculosis and Escherichia coli. However, this work is still providing original insights in chemistry as well as in the structure-activity relationships of this series of inhibitors.

http://www.nrcresearchpress.com/doi/abs/10.1139/cjc-2015-0475