Microbial transformation ofN-heptyl physostigmine,a semisynthetic alkaloid inhibitor of cholinesterase |
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| Authors: | L So R White B Arison B Petuch M S Schwartz H Cheng R Monaghan T S Chen PhD |
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| Institution: | (1) Department 807, Department of Fermentation Microbiology, Merck Research Laboratories, Building R80Y-205, 07065 Rahway, NJ, USA;(2) Department of Drug Metabolism, 19486 West Point, PA, USA |
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| Abstract: | The microbiological transformation ofN-heptyl physostigmine (L-693, 487) (1), a semisynthetic physostigmine cholinesterase inhibitor, was investigated usingVerticillium lecanii MF 5713 (ATCC 74148),Acremonium sp MF 5723 (ATCC 74164) andActinoplanes sp MA 6559 (ATCC 53771). Nine microbial metabolites (2–10) of 1 were isolated and purified using reversed-phase HPLC. The structures of the metabolites were established using spectroscopic techniques including MS and NMR. Some of the microbial metabolites were identical to metabolites present in urine of a dog treated with 1. |
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| Keywords: | biotransformation N-heptyl physostigmine cholinesterase inhibitors |
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