Davis Brian L, Liu Mark S, Hanson Ronald L, Parker William L, Patel Ramesh N
Process Research and Development, Bristol-Myers Squibb Co., New Brunswick, NJ 08903, USA.
Biotechnol Appl Biochem. 2009 Jun;53(Pt 2):133-7. doi: 10.1042/BA20080079.
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.
总共筛选了39种微生物，以检测其对（3R,5S,E）-7-（4-（4-氟苯基）-6-异丙基-2-（甲基（1-甲基-1H-1,2,4-三唑-5-基）氨基嘧啶-5-基）-3,5-二羟基-庚-6-烯酸（I）进行选择性N-去甲基化的能力，（I）是一种潜在的降低血液胆固醇水平的药物。发现两种链霉菌属物种能够进行所需的N-去甲基化反应。灰色链霉菌A.T.C.C. 13273的生物转化及产物回收已扩大到克级规模。
