On October 24, 1997, Bromidge, Steven M.; Duckworth, Malcolm; Forbes, Ian T.; Ham, Peter; King, Frank D.; Thewlis, Kevin M.; Blaney, Frank E.; Naylor, Christopher B.; Blackburn, Thomas P.; Kennett, Guy A.; Wood, Martyn D.; Clarke, Stephen E. published an article.Computed Properties of 52537-00-5 The title of the article was 6-Chloro-5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]-5-pyridyl]carbamoyl]indoline (SB-242084): The First Selective and Brain Penetrant 5-HT2C Receptor Antagonist. And the article contained the following:
The synthesis and biol. activity of a number of substituted 1-(3-pyridylcarbamoyl)indolines is reported. These compounds are potent and selective 5-HT2C/2B receptor antagonists and illustrate the use of 5,6-disubstitution as a replacement for a fused 5-membered ring in this context. Unfortunately, some compounds were also found to be very potent inhibitors of a number of human cytochrome P 450 enzymes which precluded their development as potential anxiolytic agents. Elaboration of the left hand side pyridyl ring abolished the inhibitory activity, leading to bipyridylethers such as SB-242084 which is the first reported brain penetrant, 5-HT2C receptor antagonist with selectivity over both the 5-HT2A and 5-HT2B receptor subtypes. Furthermore, SB-242084 was found to exert marked anxiolytic-like responses in rat models, confirming that these responses are mediated by 5-HT2C receptor blockade. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5
The Article related to pyridylcarbamoyl indoline preparation structure 5ht2c antagonist, sb242084 serotoninergic s2c receptor antagonist, Pharmacology: Structure-Activity and other aspects.Computed Properties of 52537-00-5
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles