Antimycobacterial Activity and Mechanism of Action of NAS-91.
The antimalarial agents NAS-91 and NAS-21 were found to express potent antimycobacterial activity, NAS-91 being more active than NAS-21. They partially inhibited mycolic acid biosynthesis and profoundly altered oleic acid production. The development of a cell-free assay for Delta 9-desaturase activity allowed direct demonstration of the inhibition of oleic acid biosynthesis by these compounds.
Gratraud
Paul
P
Laboratoire de Dynamique des Interactions Membranaires Normales et Pathologiques, Université de Montpellier II et I, CNRS, UMR 5235, case 107, Place Eugène Bataillon, 34095 Montpellier Cedex 05, France.
Surolia
Namita
N
Besra
Gurdyal S
GS
Surolia
Avadhesha
A
Kremer
Laurent
L
D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology; D002474:Cell-Free System; D003470:Culture Media; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D054889:Fatty Acid Synthase, Type II / Q000037:antagonists & inhibitors; D008826:Microbial Sensitivity Tests; D009163:Mycobacterium bovis / Q000187:drug effects* / Q000254:growth & development*; D009171:Mycolic Acids / Q000378:metabolism*; D019301:Oleic Acid / Q000096:biosynthesis*; D013230:Stearoyl-CoA Desaturase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000995:Antitubercular Agents; D003470:Culture Media; D004791:Enzyme Inhibitors; D009171:Mycolic Acids; D019301:Oleic Acid; D013230:Stearoyl-CoA Desaturase; D054889:Fatty Acid Synthase, Type II