Hargrave, Karl D. published the artcileNovel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones, Product Details of C6H7ClN2, the main research area is pyridobenzodiazepinone HIV1 reverse transcriptase inhibition; dipyridodiazepinone HIV1 reverse transcriptase inhibition; AIDS inhibitor pyridobenzodiazepinone dipyridodiazepinone.
Novel pyrido[2,3-b][1,4]benzodiazepinones, pyrido[2,3-b][1,5]benzodiazepinones, and dipyrido[3,2-b:2′,3′-e][1,4]diazepinones e.g., I (X = N, X1 = CH; X = CH; X1 = N) and II inhibited human immunodeficiency virus type 1 reverse transcriptase in vitro at concentrations as low as 35 nM. In all three series, small substituents (e.g., Me, Et, Ac) are preferred at the lactam nitrogen, whereas slightly larger alkyl moieties (e.g., Et, cyclopropyl) are favored at the other (N-11) diazepinone nitrogen. In general, lipophilic substituents are preferred on the A ring, whereas substitution on the C ring generally reduces potency relative to the corresponding compounds with no substituents on the aromatic ring. Maximum potency is achieved with Me substitution at the position ortho to the lactam nitrogen atom; however, in this case an unsubstituted lactam nitrogen is preferred. Addnl. substituents on the A ring can be readily tolerated. II (BI-RG-587) is a potent (IC50 = 84 nM) and selective non-nucleoside inhibitor of HIV-1 reverse transcriptase, and has been chosen for preclin. development. II is noncytotoxic except at high doses and effective against all clin. isolates of HIV-1, including those which are AZT-resistant. It is specific for HIV-1, ineffective against HIV-2, inactive against simian and feline reverse transcriptase, and does not inhibit DNA polymerases.
Journal of Medicinal Chemistry published new progress about AIDS (disease). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Product Details of C6H7ClN2.