214282-14-1Relevant academic research and scientific papers
5-MEMBERED N-HETEROCYCLIC COMPOUNDS WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY
-
Page 66, (2010/02/07)
Use of a compound of the formula: wherein R represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -CO-, -CS-, -CR(OR)- or -NR- wherein each of R and R represents a hydrogen atom or a hydrocarbon group which may be substituted, R represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -NR-, -CONR- or -NRCO- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -O-SO2- or -NR- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; R represents a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; W represents a bond or a divalent hydrocarbon residue having 1 to 20 carbon atoms; R represents a group of the formula: -OR (R represents a hydrogen atom or a hydrocarbon group which may be substituted) or -NRR (each of R and R, whether identical or not, represents a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; R and R may bind together to form a ring); or a salt thereof, for the manufacture of a pharmaceutical preparation for preventing or treating syndrome X.
Novel phthalazinone and benzoxazinone containing thiazolidinediones as antidiabetic and hypolipidemic agents
Madhavan, Gurram R,Chakrabarti, Ranjan,Kumar, Sunil K.B,Misra, Parimal,Mamidi, Rao N.V.S,Balraju,Kasiram, Katneni,Babu, Ravi K,Suresh, Juluri,Lohray, Braj B,Lohray, Vidya B,Iqbal, Javed,Rajagopalan, Ramanujam
, p. 627 - 637 (2007/10/03)
We report here the synthesis of a series of 5-[4-[2-[substituted phthalazinones-2(or 4)yl]ethoxy]phenylmethyl]thiazolidine-2,4-diones and 5-[4-[2-[2,3-benzoxazine-4-one-2-yl]ethoxy]phenylmethyl]thiazolidine-2, 4-diones and their plasma glucose and plasma triglyceride lowering activity in db/db mice. In vitro PPARγ transactivation assay was performed in HEK 293T cells. In vitro and in vivo pharmacological studies showed that the phthalazinone analogue has better activity. PHT46 (compound 5a), the best compound in this series, showed better in vitro PPARγ transactivation potential than troglitazone and pioglitazone. In insulin resistant db/db mice, PHT46 showed better plasma glucose and triglyceride lowering activity than the standard drugs. Pharmacokinetic study in Wistar rats showed good systemic exposure of PHT46. Subchronic toxicity study in Wistar rats did not show any treatment-related adverse effect.
Alpha-Substituted phenylpropionic acid derivative and medicine containing the same
-
, (2008/06/13)
Disclosed herein are an α-substituted phenylpropionic acid derivative represented by the following general formula (1): wherein W is a (substituted) lactam ring, A is an alkylene or alkyleneoxy group or the like, X is O, S, NH or CH2, Y1/
