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ChemInform Abstract: Novel, Highly Potent Aldose Reductase Inhibitors: (R)-(-)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo [1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (AS-3201) and Its Congeners.

✍ Scribed by T. NEGORO; M. MURATA; S. UEDA; B. FUJITANI; Y. ONO; A. KUROMIYA; M. KOMIYA; K. SUZUKI; J. MATSUMOTO

Publisher
John Wiley and Sons
Year
2010
Weight
38 KB
Volume
30
Category
Article
ISSN
0931-7597

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✦ Synopsis

Novel, Highly Potent Aldose Reductase Inhibitors: (R)-(-)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo [1,2-a]pyrazine-4spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and Its Congeners.

-Investigation of the structure-activity relationship of a series of novel tetrahydropyrrolopyrazine derivatives, e.g. (X)-(XIII), shows that the racemate of (VII) possesses the best oral activity. Therefore, its enantiomers are synthesized. The (R)-(-)-enantiomer is responsible for the activity and is about 2 times more potent than the racemate in both the aldose reductase inhibitory activity and in vivo activity, and 10, respectively, 500 times more potent in vitro and in vivo than the (S)-(+)-enantiomer. Thus, evaluation of its clinical efficiency in the prevention of diabetic complications is of interest.

-(NEGORO,

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## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v