So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Bromidge, Steven M.; Dabbs, Steven; Davies, David T.; Davies, Susannah; Duckworth, D. Malcolm; Forbes, Ian T.; Gaster, Laramie M.; Ham, Peter; Jones, Graham E.; King, Frank D.; Mulholland, Keith R.; Saunders, Damian V.; Wyman, Paul A.; Blaney, Frank E.; Clarke, Stephen E.; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Lightowler, Sean; Middlemiss, Derek N.; Trail, Brenda; Riley, Graham J.; Wood, Martyn D. researched the compound: 3-Bromo-4-chloronitrobenzene( cas:16588-26-4 ).Formula: C6H3BrClNO2.They published the article 《Biarylcarbamoylindolines Are Novel and Selective 5-HT2C Receptor Inverse Agonists: Identification of 5-Methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant/Anxiolytic Agent》 about this compound( cas:16588-26-4 ) in Journal of Medicinal Chemistry. Keywords: biarylcarbamoyl indoline preparation structure 5HT2C agonist; antidepressant anxiolytic biarylcarbamoylindoline serotoninergic agonist. We’ll tell you more about this compound (cas:16588-26-4).
The evolution, synthesis, and biol. activity of a novel series of 5-HT2C receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT2C affinity and selectivity over 5-HT2A receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with addnl. selectivity over the closely related 5-HT2B receptor. Compounds from this series are inverse agonists at the human cloned 5-HT2C receptor, completely abolishing basal activity in a functional assay. The new series have reduced P 450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biol. profile, SB-228357 and SB-243213 have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.
As far as I know, this compound(16588-26-4)Formula: C6H3BrClNO2 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
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