Bioorganic & medicinal chemistry letters.
Publisher:
Pergamon Press,. Oxford : Elsevier Science Ltd
Frequency: Semimonthly, 1994-
Country: England
Language: English
Start Year:1991 -
ISSN:
0960-894X (Print)
1464-3405 (Electronic)
0960-894X (Linking)
1464-3405 (Electronic)
0960-894X (Linking)
Impact Factor
2.7
2022
| NLM ID: | 9107377 |
| (DNLM): | SR0069668(s) |
| (OCoLC): | 23245011 |
| Coden: | BMCLE8 |
| Classification: | W1 BI876KE |
Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase. Conformationally restricted carbamate inhibitors, exo-2-norbornyl-N-butylcarbamate (1), endo-2-norbornyl-N-butylcarbamate (2), l-adamantyl-N-butylcarbamate (3), and 2-adamantyl-N-butylcarbamate (4) as active site-directed irreversible inhibitors of horse serum butyrylcholinesterase are investigated for values of the dissociation constant (KI), the carbamylation constant (k2), and the bimolecular rate constant (ki). Compound 1 is the most potent inhibitor of the enzyme and the values of KI and ki are 20 nM and 1.1 x 10(5) M-1sec-1, respectively.