30458-68-5Relevant academic research and scientific papers
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase
Gritzalis, Dimitrios,Park, Jaeok,Chiu, Wei,Cho, Hyungjun,Lin, Yih-Shyan,De Schutter, Joris W.,Lacbay, Cyrus M.,Zielinski, Michal,Berghuis, Albert M.,Tsantrizos, Youla S.
supporting information, p. 1117 - 1123 (2015/02/19)
In order to explore the interactions of bisphosphonate ligands with the active site and an allosteric pocket of the human farnesyl pyrophosphate synthase (hFPPS), substituted indole and azabenzimidazole bisphosphonates were designed as chameleon ligands. NMR and crystallographic studies revealed that these compounds can occupy both sub-pockets of the active site cavity, as well as the allosteric pocket of hFPPS in the presence of the enzyme's Mg2+ ion cofactor. These results are consistent with the previously proposed hypothesis that the allosteric pocket of hFPPS, located near the active site, plays a feed-back regulatory role for this enzyme.
FUSED HETEROCYCLIC COMPOUNDS
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Page/Page column 79, (2012/01/13)
The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
Synthesis and coordination chemistry of 4-azabenzimidazole derivatives
Jahnke, Mareike C.,Brackemeyer, Dirk,Pape, Tania,Hahn, F. Ekkehardt
experimental part, p. 476 - 490 (2012/01/06)
A facile method for the preparation of N1- (1a-6a) and N3-alkylated (1b-6b) 4-azabenzimidazole derivatives is presented. Both isomers were obtained by alkylation of 4-azabenzimidazole. The isomers were separated, and the preferred formation of the N1-alky
Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones
Oguchi,Wada,Honma,Tanaka,Kaneko,Sakakibara,Ohsumi,Serizawa,Fujiwara,Horikoshi,Fujita
, p. 3052 - 3066 (2007/10/03)
A series of imidazopyridine thiazolidine-2,4-diones were designed and synthesized from their corresponding pyridines. These compounds represent conformationally restricted analogues of the novel hypoglycemic compound rosiglitazone (5). The series was evaluated for its effect on insulin-induced 3T3-L1 adipocyte differentiation in vitro and its hypoglycemic activity in the genetically diabetic KK mouse in vivo. The structure-activity relationships are discussed. On the basis of the in vivo potency, 5-[4-(5-methoxy-3-methyl-3H-imidazo[4,5-b]pyridin-2-ylmethoxy)ben zyl]thiazolidine-2,4-dione (19a) was selected as the candidate for further studies in a clinical setting.
