1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis

Authors :: Stephen Fienberg
Gregory S. Basarab
Anne J. Lenaerts
Virsinha Reddy
Sandeep R. Ghorpade
Mathew Njoroge
Grant A. Boyle
Charles J. Eyermann
Clifton E. Barry
Timothy G. Myers
Efrem Abay
Nina Lawrence
Alissa Myrick
Helena I. Boshoff
Vinayak Singh
Lutete Peguy Khonde
Lisa M. Massoudi
Paul D. van Helden
Frederick A. Sirgel
Gregory T. Robertson
Rudolf Müller
Kelly Chibale
Aloysius T. Nchinda
Qin Su
Source :: Journal of Medicinal Chemistry. 64:12790-12807
Publication Year :: 2021
Publisher :: American Chemical Society (ACS), 2021.
Abstract: Phenotypic whole cell high-throughput screening of a ∼150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide 1 as a moderately active hit. Structure-activity relationship (SAR) studies demonstrated a clear scope to improve whole cell potency to MIC values of

Subjects :: biology
Chemistry
INHA
biology.organism_classification
In vitro
Cell wall
Mycobacterium tuberculosis
Biochemistry
In vivo
Drug Discovery
Molecular Medicine
Potency
Pharmacophore
Drug metabolism

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