| Autor: |
Hoffman JM; Department of Medicinal Chemistry, Merck Reserch Laboratories, West Point, Pennsylvania 19486-0004., Smith AM, Rooney CS, Fisher TE, Wai JS, Thomas CM, Bamberger DL, Barnes JL, Williams TM, Jones JH, et. al. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1993 Apr 16; Vol. 36 (8), pp. 953-66. |
| DOI: |
10.1021/jm00060a002 |
| Abstrakt: |
A new series of potent specific 2-pyridinone reverse transcriptase (RT) inhibitors was developed based on the preliminary development lead 3-[(phthalmido)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (3), a non-nucleoside derivative which exhibited weak antiviral activity in cell culture against HIV-1 strain IIIB. One compound, 3-[(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (9,L-696,229), which was a highly selective antagonist of the RT enzyme (IC50 = 23 nM) and which inhibited the spread of HIV-1 IIIB infection by > 95% in MT4 human T-lymphoid cell culture (CIC95 = 50-100 nM), was selected for clinical evaluation as an antiviral agent. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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