Classes > rosiglitazone
Page last updated: 2024-06-07 21:15:02

rosiglitazone

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ChEBI ID: 50122

Members

There are 2 compounds belonging to this class, involving 2 studies.

MemberDefinitionRole
(-)-rosiglitazone
(+)-rosiglitazone

Research Growth

Pre-19901990-20002001-20102011-2020Post-2020
01010

Most Recent Studies

Article
Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6
    Peroxisome Proliferator-Activated Receptor γ (PPARγ) activators have drawn great recent attention in the clinical management of type 2 diabetes mellitus, prompting several attempts to discover and optimize new PPARγ activators. With this in mind, we explored the pharmacophoric space of PPARγ using seven diverse sets of activators. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select an optimal combination of pharmacophoric models and 2D physicochemical descriptors capable of accessing self-consistent and predictive quantitative structure-activity relationship (QSAR) (r2(71)=0.80, F=270.3, r2LOO=0.73, r2PRESS against 17 external test inhibitors=0.67). Three orthogonal pharmacophores emerged in the QSAR equation and were validated by receiver operating characteristic (ROC) curves analysis. The models were then used to screen the national cancer institute (NCI) list of compounds. The highest-ranking hits were tested in vitro. The most potent hits illustrated EC50 values of 15 and 224 nM.
Differential activity of rosiglitazone enantiomers at PPAR gamma.
    Bioorganic & medicinal chemistry letters, 1998, Dec-15, Volume: 8, Issue:24
    Analysis of the enantiomers of rosiglitazone in a PPAR gamma binding assay suggests that the (S)-(-)-isomer is responsible for the antidiabetic activity.