- THIAZOLIDINE DERIVATIVES, THEIR PREPARATION AND USE
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Compounds of formula (I): (in which R1-R7 are hydrogen or various organic groups, n is 1-10, Ar is an aromatic group, U is CH2 or a carbon atom doubly bonded to either one of its adjacent carbons, and W is >CH2, >C=0 , >CHOH, >C=NOH or various derivatives thereof) have the ability to lower the levels of blood lipid peroxides and blood sugars and to inhibit the activity of aldose reductase; they may be used therapeutically for these purposes.
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- Studies on hindered phenols and analogues. 1. Hypolipidemic and hypoglycemic agents with ability to inhibit lipid peroxidation
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A series of hindered phenols were investigated as hypolipidemic and/or hypoglycemic agents with ability to inhibit lipid peroxidation. 1,3-Benzoxathioles (9 and 22), phenoxypentanoic acid (34), phenoxypentanol (35a), phenoxynonanol (35b), phenylchloropropionic acid having a chromanyl group (25), and a thiazolidine compound (27) derived from 25, all having a hindered phenol group, were prepared and examined. Compound 27 showed the expected biological properties in vivo and in vitro without any liver weight increase. Biological activities of the analogous thiazolidine compounds, 43-58, were compared. Thus, roxy-2,5,7,8-tetramethylchroman-2-yl(methoxy]-benzyl]-2,4-thiazolidinedione (27) (CS-045) was found to have all our expected properties and was selected as a candidate for further development as a hypoglycemic and hypolipidemic agent.
- Yoshioka,Fujita,Kanai,Aizawa,Kurumada,Hasegawa,Horikoshi
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p. 421 - 428
(2007/10/02)
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- Thiazolidine derivatives, their preparation and compositions containing them
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The compounds of formula (I): STR1 [in which: R1 and R2 are the same or different and each represents hydrogen or C1 -C5 alkyl; R3 represents hydrogen, an acyl group, a (C1 -C6 alkoxy)carbonyl group or an aralkyloxycarbonyl group; R4 and R5 are the same or different and each represents hydrogen, C1 -C5 alkyl or C1 -C5 alkoxy, or R4 and R5 together represent a C1 14 C4 alkylenedioxy group; n is 1, 2 or 3; W represents the --CH2 --, >CO or >CH--OR6 group (in which R6 represents any one of the atoms or groups defined for R3 and may be the same as or different from R3); and Y and Z are the same or different and each represents oxygen or imino] and pharmaceutically acceptable salts thereof have various valuable therapeutic effects on the blood system and may be prepared by a process which includes reacting a corresponding halopropionic acid derivative with thiourea.
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