European Journal of Medicinal Chemistry p. 539 - 550 (2018)
Update date:2022-08-04
Topics:
Poce, Giovanna
Cocozza, Martina
Alfonso, Salvatore
Consalvi, Sara
Venditti, Giulia
Fernandez-Menendez, Raquel
Bates, Robert H.
Barros Aguirre, David
Ballell, Lluis
De Logu, Alessandro
Vistoli, Giulio
Biava, Mariangela
BM635 is the hit compound of a promising anti-TB compound class. Herein we report systematic variations around the central pyrrole core of BM635 and we describe the design, synthesis, biological evaluation, pharmacokinetic analysis, as well as in vivo TB mouse efficacy studies of novel BM635 analogues that show improved physicochemical properties. This hit-to-lead campaign led to the identification of a new analogue, 4-((1-isopropyl-5-(4-isopropylphenyl)-2-methyl-1H-pyrrol-3-yl)methyl)morpholine (17), that shows excellent activity (MIC = 0.15 μM; SI = 133) against drug-sensitive Mycobacterium tuberculosis strains, as well as efficacy in a murine model of TB infection.
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Doi:10.1002/cmdc.201402186
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