title: Design, synthesis and structure-activity relationships of 3,5-diaryl-1H-pyrazoles as inhibitors of arylamine N-acetyltransferase.
abstract: The synthesis and inhibitory potencies of a novel series of 3,5-diaryl-1H-pyrazoles as specific inhibitors of prokaryotic arylamine N-acetyltransferase enzymes is described. The series is based on hit compound 1 3,5-diaryl-1H-pyrazole identified from a high-throughout screen that has been carried out previously and found to inhibit the growth of Mycobacterium tuberculosis.
authors.affiliation: Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK. e.fullam@warwick.ac.uk
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Fullam
authors.forename: James
authors.initials: J
authors.lastname: Talbot
authors.forename: Areej
authors.initials: A
authors.lastname: Abuhammed
authors.forename: Isaac
authors.initials: I
authors.lastname: Westwood
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Davies
authors.forename: Angela J
authors.initials: AJ
authors.lastname: Russell
authors.forename: Edith
authors.initials: E
authors.lastname: Sim
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001665:Binding Sites; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D062105:Molecular Docking Simulation; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D017434:Protein Structure, Tertiary; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000995:Antitubercular Agents; D004791:Enzyme Inhibitors; D011720:Pyrazoles; C031280:pyrazole; D001191:Arylamine N-Acetyltransferase