187341-14-6Relevant articles and documents
Novel antidiabetic and hypolipidemic agents. 5. Hydroxyl versus benzyloxy containing chroman derivatives
Reddy, K. Anji,Lohray,Bhushan,Reddy, A. Sekar,Mamidi, N. V. S. Rao,Reddy, P. Papi,Saibaba,Reddy, N. Jaipal,Suryaprakash,Misra, Parimal,Vikramadithyan, Reeba K.,Rajagopalan
, p. 3265 - 3278 (2007/10/03)
Several thiazolidinediones having chroman moieties were synthesized and evaluated for their euglycemic and hypolipidemic activities. Some of the analogues having an aminoalkyl group as a linker between the chroman ring and 4-[5-(2,4-dioxo-1,3-thiazolidinyl)methyl]phenoxy moiety seem to be better than troglitazone. In vitro transactivation assays of PPARγ have been carried out with these glitazones to understand their molecular mechanism. For the first time we have found that some of the unsaturated thiazolidinediones are superior to their saturated counterpart in the in vivo assay. A more potent thiazolidinedione analogue than troglitazone is reported. Pharmacokinetic studies have shown that protection of the OH group in the chroman moiety leads to a decrease in metabolism, thereby resulting in a superior pharmacological profile.
Thiazolidinedione derivatives having antidiabetic, hypolipidaemic antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
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, (2008/06/13)
A compound of the general formula (I), where A represents, substituted or unsunstituted unsaturated aliphatic, alicyclic, aromatic, heterocyclic groups, B represents a substituted or unsubstituted divalent alkylene or alkenyl group having 1 to 10 carbon atoms, wherein substituents may be present in one or more of the divalent alkylene or alkenyl groups, D represents a substituted or insubstituted divalent alkenyl, alkynyl, aralkyl alkoxycarbonyl or aryloxycarbonyl groups, X represents CH2, C=O, CH-OH, sulphur, oxygen, N-Y, where Y represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl or acyl, Ar represents a divalent aromatic, single or fused ring system, with or without substituents, the ring may contain one or more hetero atoms selected from nitrogen, sulphur, or oxygen; R1and R2each represents hydrogen or together represent a bond either or both may be substituents or both together form a part of a ring. Methods for preparing the compound and pharmaceutical compositions containing a compound of formula (I).
