21647-13-2Relevant academic research and scientific papers
Novel benzimidazole-based MCH R1 antagonists
Carpenter, Andrew J.,Al-Barazanji, Kamal A.,Barvian, Kevin K.,Bishop, Michael J.,Britt, Christy S.,Cooper, Joel P.,Goetz, Aaron S.,Grizzle, Mary K.,Hertzog, Donald L.,Ignar, Diane M.,Morgan, Ronda O.,Peckham, Gregory E.,Speake, Jason D.,Swain, Will R.
, p. 4994 - 5000 (2007/10/03)
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
2,3(1H,4H)quinoxalinedione
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, (2008/06/13)
2,3(1H,4H)-quinoxalinediones of the formula I STR1 where R1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R3, --CO--O--R3 or --CO--NH--R3, where R3 is hydrogen, C1 -C4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R1 can have up to three of the following substituents: C1 -C4 -alkyl, C1 -C4 -haloalkyl, C1 -C4 -alkoxy, C1 -C4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R3 and --CO--NH--R3 ; R2 is 1-pyrrolyl which can have up to two of the following substituents: C1 -C4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R3, --CO--NH--R3, --CH2 --O--R3, --O--R3 and --CH=NO--R3 R radicals are identical or different and are the following: C1 -C4 -alkyl, C1 -C4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R3 and --CO--NH--R3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' STR2 where R1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.
