- Efficient synthesis of nevirapine analogs to study its metabolic profile by click fishing
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Knowledge of the biotransformation and pharmacokinetics of the antiretroviral agent nevirapine is still insufficient. In order to trace rash inducing metabolites of nevirapine, we devised a short and efficient multi-gram synthesis of a nevirapine analog that can be coupled to azide containing compounds by click chemistry.
- Bernard, Sylvain,Defoy, Daniel,Dory, Yves L.,Klarskov, Klaus
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supporting information; experimental part
p. 6127 - 6130
(2010/06/13)
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- PREPARATION AND UTILITY OF NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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Disclosed herein are non-nucleoside reverse transcriptase inhibitors having structural Formula ( I ), processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof. Formula ( I )
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Page/Page column 67
(2008/12/08)
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- AN IMPROVED PROCESS FOR INDUSTRIAL MANUFACTURE OF NEVIRAPINE
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An improved cost-effective, environmental friendly, industrial method for manufacture of Nevirapine.Formula (I):
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Page/Page column 18
(2008/06/13)
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- 5,11-dihydro-6H-dipyrido(3,2-B:2',3'-E)(1,4)diazepines and their use in the prevention or treatment of HIV infection
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Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.
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- Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 1. Tricyclic Pyridobenzo- and Dipyridodiazepinones
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Novel pyridobenzodiazepinones (I), pyridobenzodiazepinones (II), and dipyridodiazepinones (III) were found to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase in vitro at concentrations as low as 35 nM.In all three series, small substituents (e.g., methyl, ethyl, acetyl) are preferred at the lactam nitrogen, whereas slightly larger alkyl moieties (e.g., ethyl, cyclopropyl) are favored at the other (N-11) diazepinone nitrogen.In general, lipophilic substituents are preferred on the A ring, whereassubstitution on the C ring generally reduces potency relative to the corresponding compounds with no substituents on the aromatic rings.Maximum potency is achieved with methyl substitution at the position ortho to the lactam nitrogen atom; however, in this case an unsubstituted lactam nitrogen is preferred.Additional substituents on the A ring can be readily tolerated.The dipyridodiazepinone derivative 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyridodiazepin-6-one (96, nevirapine) is a potent (IC50 = 84 nM) and selective non-nucleoside inhibitor of HIV-1 reverse transcriptase, and has been chosen for clinical evaluation.
- Hargrave, Karl D.,Proudfoot, John R.,Grozinger, Karl G.,Cullen, Ernest,Kapadia, Suresh R.,et al.
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p. 2231 - 2241
(2007/10/02)
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