| Autor: |
S, Ulhaq, M A, Naylor, E C, Chinje, M D, Threadgill, I J, Stratford |
| Rok vydání: |
1997 |
| Předmět: |
|
| Zdroj: |
Anti-cancer drug design. 12(1) |
| ISSN: |
0266-9536 |
| Popis: |
Treatment of 1,1-dimethylethyl S-(2-1,1-dimethylethoxycarbonylamino)-5-bromopentanoate with 1-potassio-2-nitroimidazole, followed by deprotection, afforded S-2-amino-5-(2-nitroimidazol-1-yl)pentanoic acid, which was reduced to S-2-amino-5-(2-aminoimidazol-1-yl)pentanoic acid. This aminoimadazole inhibited rat brain nitric oxide synthase (NOS) activity 3.2 times more potently than did the nitro analogue. Thus S-2-amino-5-(2-nitroimidazol-1-yl)pentanoic acid is a potent prodrug which may be bioreductively activated to a NOS inhibitor in hypoxic solid tumours. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
