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Based on the multi-target strategy to treat type 2 diabetes mellitus (T2DM), glucokinase/peroxisome proliferator-activated receptor gamma (GK/PPARgamma) dual-target molecules were constructed by the rational combination of pharmacophores from known GK activators and PPARgamma agonists. A series of dual-target agents were designed and synthesized, and their capacities to induce GK and PPARgamma transcriptional activity were evaluated. Three of these compounds showed particularly high potency toward GK, moderate activity toward PPARgamma, and their structure-activity relationships were preliminarily analyzed. The putative binding modes of one of the most promising compounds were also explored by molecular docking simulations with GK and PPARgamma. Two birds, one stone: GK/PPARgamma dual-target ligands were constructed by rational combination of pharmacophores from known GK activators and PPARgamma agonists. Their ability to induce GK and PPARgamma transcriptional activity were evaluated, and the putative binding modes of one of the most promising compounds were also explored by molecular docking simulations with GK and PPARgamma.

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Reference:
Thiazole | C3H9844NS – PubChem,
Thiazole | chemical compound | Britannica

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Background: Glucokinase activators (GKAs) represent a promising opportunity for the treatment of type 2 diabetes due to the fact that glucokinase (GK) is a key regulator of glucose homeostasis. Method: Based on structure-based design strategies, a series of novel orotic acid amide derivatives have been synthesized. Lead optimization led to the discovery of several active compounds via in vitro enzyme assays. Compared to the positive control compound GKA22, compounds 10j, 11h and 11i exhibited identical or even higher activity. Furthermore, docking simulation of compound 11i further demonstrated that the hydrogen atom of amide and the nitrogen atom of pyrimidine both bound to Arg63 via hydrogen bonds. Results: Hydrogen bond interactions were also observed between the two oxygen atoms of 2-methoxy-1-methyl-ethoxy moiety and Thr65. Both ends of the molecule were fixed in allosteric pocket of glucokinase, which was in favour of keeping active conformation.

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Reference:
Thiazole | C3H9846NS – PubChem,
Thiazole | chemical compound | Britannica

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A group of ethyl 6-methylimidazo<2,1-b>thiazole-5-carboxylates and 2-methylimidazo<2,1-b>benzothiazole-3-carboxylates was prepared by reaction of ethyl 2-chloroacetoacetate with some 2-aminothiazoles and 2-aminobenzothiazoles, respectively.Such reactions may sometimes afford a side product which was isolated and characterized.The ethyl esters were then converted into the corresponding acids by hydrolysis.Three of these acids were evaluated for antiinflammatory, analgesic, and antipyretic activities, as well as for ulcerogenic potential.

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Reference:
Thiazole | C3H9928NS – PubChem,
Thiazole | chemical compound | Britannica

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This invention provides compounds of Formula (I), wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

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Reference:
Thiazole | C3H9593NS – PubChem,
Thiazole | chemical compound | Britannica

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Glucokinase (GK) is a glucose sensor that couples glucose metabolism to insulin release. The important role of GK in maintaining glucose homeostasis is illustrated in patients with GK mutations. In this publication, identification of the hit molecule 1 and its SAR development, which led to the discovery of potent allosteric GK activators 9a and 21a, is described. Compound 21a (RO0281675) was used to validate the clinical relevance of targeting GK to treat type 2 diabetes.

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Reference:
Thiazole | C3H9797NS – PubChem,
Thiazole | chemical compound | Britannica

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Development of SAR in an aryl ether series of mGlu5 NAMs leading to the identification of tool compound VU0409106 is described in this Letter. VU0409106 is a potent and selective negative allosteric modulator of mGlu 5 that binds at the known allosteric binding site and demonstrates good CNS exposure following intraperitoneal dosing in mice. VU0409106 also proved efficacious in a mouse marble burying model of anxiety, an assay known to be sensitive to mGlu5 antagonists as well as clinically efficacious anxiolytics.

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Reference:
Thiazole | C3H9815NS – PubChem,
Thiazole | chemical compound | Britannica

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An improved method for the preparation of ethyl 1-hydroxy-3-oxo-6,7- dihydro-3H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylate has been proposed and a series of hetarylamides has been synthesized from it. A comparative analysis has been carried out of the antitubercular activities of the synthesized compounds with the active structural analogs 4-hydroxy-2-oxo-1,2-dihydroquinoline-3 and 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxamides studied before.

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Reference:
Thiazole | C3H9856NS – PubChem,
Thiazole | chemical compound | Britannica

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A set of electrophilic 2-(trifluoroacetyl)-1,3-azoles demonstrated- excellent activity in the C-oxyalkylation of pyrrole, furan, thiophene, 1,3-thiazole, and 1,2-oxazole derivatives. The reaction conditions and the yields of the corresponding trifluoromethyl-substituted alcohols depend strongly on both the electronic and steric nature of the 1,3-azole unit. Georg Thieme Verlag Stuttgart ? New York.

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Reference:
Thiazole | C3H9880NS – PubChem,
Thiazole | chemical compound | Britannica

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A simple and efficient method has been developed for the synthesis of 2-aminothiazoles from alpha-bromo ketones in one-pot using a supported reagents system, KSCN/SiO2-RNH3OAc/Al2O3, in which alpha-bromo ketone reacts first with KSCN/SiO2 and the product, alpha-thiocyano ketone, reacts with RNH3OAc/Al2O3 to give the final product, 2-aminothiazole, in high yield.

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Reference:
Thiazole | C3H9879NS – PubChem,
Thiazole | chemical compound | Britannica

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1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic scaffold allowed to improve the physico-chemical parameters for optimization of the aqueous solubility while retaining high in vitro potency.

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Reference:
Thiazole | C3H9956NS – PubChem,
Thiazole | chemical compound | Britannica