PubMed · 4717438
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1973-07-07. Riot control agent.. https://pubmed.ncbi.nlm.nih.gov/4717438/
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Dibenz[b,f][1,4]oxazepin-11(10H)-ones (III), pyrido[2,3-b][1,4]benzoxazepin-6(5H)-ones (IV), and pyrido[2,3-b]- [1,5]benzoxazepin-5(6H)-ones (V) were found to inhibit human immunodeficiency virus type 1 reverse transcriptase with IC50 values as low as 19 nM. A-ring substitution has a profound effect on activity, with appropriate substituents at the positions ortho and para to the lactam nitrogen providing dramatically enhanced potency. Substitution in the C-ring is generally neutral or detrimental to activity. Although a C-ring amino substituent at the position meta to the lactam carbonyl is generally beneficial to activity, it has essentially no effect when the A-ring is optimally substituted. Like the dipyridodiazepinone nevirapine, compounds III-V are specific for HIV-1 RT, exhibiting no inhibitory activity against HIV-2 RT or other virial reverse transcriptase enzymes.
1H-NMR and X-ray conformation studies of new muscarinergic dibenzodioxazocines have been carried out. It is suggested that EGYT-2347 (2-chloro-12-/2-piperidino-ethyl/-dibenzo [d,g] [1, 3, 6] dioxazocine hydrochloride) may exist in solution in at least two distinct conformations, unlike other tricyclic or non-tricyclic compounds having antimuscarinergic activity. One of these conformations possessing an asymmetric, twisted central hetero-ring confined between two phenyl rings is probably the energetically more stable form, while the other having a butterfly-like structure, with mirror symmetry-related phenyl rings as in phenothiazines seems to be more suitable for receptor binding. The importance of the hydrophobic pocket at the receptor site was revealed by the good correlation of the calculated and measured hydrophobic parameters to the muscarinic activity of these newly synthesized and other known muscarinergic compounds.
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