title: Microbial N-demethylation: biotransformation and recovery of a drug metabolite.
abstract: A total of 39 microbes were screened for the ability to selectively N-demethylate (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)aminopyrimidin-5-yl)-3,5-dihydroxy-hept-6-enoic acid (I), a potential drug for lowering blood cholesterol levels. Two Streptomyces species were found to carry out the desired N-demethylation. Bioconversion by Streptomyces griseus A.T.C.C. 13273 and product recovery were scaled up to the multi-gram level.
authors.affiliation: Process Research and Development, Bristol-Myers Squibb Co., New Brunswick, NJ 08903, USA.
authors.forename: Brian L
authors.initials: BL
authors.lastname: Davis
authors.forename: Mark S
authors.initials: MS
authors.lastname: Liu
authors.forename: Ronald L
authors.initials: RL
authors.lastname: Hanson
authors.forename: William L
authors.initials: WL
authors.lastname: Parker
authors.forename: Ramesh N
authors.initials: RN
authors.lastname: Patel
mesh_terms: D001419:Bacteria / Q000378:metabolism*; D001711:Biotransformation; D005658:Fungi / Q000378:metabolism*; D008745:Methylation; D011743:Pyrimidines / Q000378:metabolism*; D013302:Streptomyces / Q000378:metabolism; D014230:Triazoles / Q000378:metabolism*
chemical_list: C529816:7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid; D011743:Pyrimidines; D014230:Triazoles