126534-13-2Relevant academic research and scientific papers
Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4
Cheng, Xinlai,Yoshida, Hiroki,Raoofi, Dena,Saleh, Sawsan,Alborzinia, Hamed,Wenke, Frank,G?hring, Axel,Reuter, Stefanie,Mah, Nancy,Fuchs, Heiko,Andrade-Navarro, Miguel A.,Adjaye, James,Gul, Sheraz,Utikal, Jochen,Mrowka, Ralf,W?lfl, Stefan
, p. 5742 - 5750 (2015)
The octamer-binding transcription factor 4 (Oct3/4) is a master gene in the transcriptional regulatory network of pluripotent cells. Repression of Oct3/4 in embryonic stem cells (ESCs) is associated with cell differentiation and loss of pluripotency, wher
Discovery of 2-aminothiazole-4-carboxamides, a novel class of muscarinic M3 selective antagonists, through solution-phase parallel synthesis
Sagara, Yufu,Mitsuya, Morihiro,Uchiyama, Minaho,Ogino, Yoshio,Kjmura, Toshifumi,Ohtake, Norikazu,Mase, Toshiaki
, p. 437 - 440 (2007/10/03)
Synthesis and structure-activity relationship of a new class of muscarinic M3 selective antagonists were described. In the course of searching for a muscarinic M3 antagonist with a structure distinct from those of the 2-(4,4-difluorocyclopentyl)-2-phenylacetamide derivatives, we identified a thiazole-4-carboxamide derivative (1) as a lead compound in our in-house chemical collection. Since this compound (1) showed relatively low binding affinity (K1 = 140 nM) for M3 receptors in the human binding assays, we tried to improve its potency and selectivity for M 3 over M1 and M2 receptors by derivatization of 1 through a combinatorial approach. A solution-phase parallel synthesis effectively contributed to the optimization of each segment of 1. Thus, we have identified a cyclooctenylmethyl derivative (3e) and a cyclononenylmethyl derivative (3f) as representative M3 selective antagonists in this class.
Thiazole derivatives, their preparation and their use in the treatment of diabetes complications
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, (2008/06/13)
Compounds of formula (I): STR1 in which: R1 and R2 are independently hydrogen, alkyl, aliphatic hydrocarbon groups having one or two carbon-carbon double or treble bonds, cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, alkanoyl, alkenyol, cycloalkylcarbonyol, arylcarbonyl, substituted arylcarbonyl, arylalkanoyl, substituted arylalkanoyl, arylalkenoyl, substituted arylalkenoyl, alkoxycarbonyl, aryloxycarbonyl, substituted aryloxycarbonyl, aralkyloxycarbonyl, substituted aralkyloxycarbonyl, optionally substituted carbamoyl or thiocarbamoyol, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, alkylthio, arylthio and substituted arylthio, or R1 and R2, together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group; one of Ra and Rb is hydrogen, alkyl or halogen, and the other of Ra and Rb is a group of formula (II): STR2 R4 is hydrogen, carboxy, protected carboxy or optionally substituted carbamoyl; R5 is hydrogen, or carboxyalkyl or protected carboxyalkyl in which the alkyl part is C1 -C6 ; n=0, 1 or 2; X is oxygen or sulfur; are useful in the treatment of the complications attendant upon diabetes and may be prepared by condensation of a thiazolidine or rhodanine compound with a compound corresponding to the remainder of the molecule of the compound of formula (I).
