Design, synthesis, and docking studies of telmisartan analogs for the treatment of metabolic syndrome was written by Mizuno, Cassia S.;Chittiboyina, Amar G.;Patny, Akshay;Kurtz, Theodore W.;Pershadsingh, Harrihar A.;Speth, Robert C.;Karamyan, Vardan T.;Avery, Mitchell A.. And the article was included in Medicinal Chemistry Research in 2009.Recommanded Product: 4887-83-6 This article mentions the following:
In our early studies, telmisartan was found to be a moderate peroxisome proliferator-activated receptor (PPAR) gamma activator in the human PPARγ-GAL-4 cell-based transactivation assay. Thus, novel analogs of telmisartan were designed, synthesized, and evaluated in the AT1 receptor binding assay and PPAR gamma transactivation assay. A total of 11 compounds were designed based on docking in both AT1 receptor model and PPAR gamma active pocket and synthesized. Introduction of an addnl. acidic group at the para position of the distal Ph ring of telmisartan decreased affinity towards AT1 receptor and PPARγ activity. In the present study, the mol. with best results was I, with weak PPARγ activity (8% of maximum PPARγ activation achieved by full agonist rosiglitazone at 10 μM) and good binding affinity (Ki = 650 ± 139 nM) towards the AT1 receptor. Docking of I into AT1 receptor model and PPAR gamma showed very similar interactions with the receptors as AT1 antagonist telmisartan and PPAR gamma agonist rosiglitazone. In the experiment, the researchers used many compounds, for example, 7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6Recommanded Product: 4887-83-6).
7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.Recommanded Product: 4887-83-6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem