129865-59-4Relevant academic research and scientific papers
Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors
Park, Hwangseo,Lee, Soyoung,Hong, Sungwoo
, p. 3784 - 3787 (2015/08/24)
Abstract p38 mitogen-activated protein kinase (MAPK) is a promising target for the development of therapeutics for various immunological diseases. We designed and synthesized aminothiazole-based p38 MAPK inhibitors of with IC50 values ranging from 0.1 to 2 μM by means of the structure-based de novo design of phenyl-(2-phenylamino-thiazol-5-yl)-methanone scaffold. Because these newly identified inhibitors were also screened for having desirable physicochemical properties as a drug candidate, they deserve consideration for further investigation as anti-inflammatory drugs. Structural features relevant to the stabilization of the newly identified inhibitors in the ATP-binding site of p38 MAPK are discussed in detail.
Practical synthesis of a highly functionalized thiazole ketone
Frey, Lisa F.,Marcantonio, Karen M.,Chen, Cheng-Yi,Wallace, Debra J.,Murry, Jerry A.,Tan, Lushi,Chen, Weirong,Dolling, Ulf H.,Grabowski, Edward J. J.
, p. 6363 - 6373 (2007/10/03)
Compound 1 is a uniquely substituted ketone prepared via addition of a thiazole anion to an aromatic nitrile in good overall yield. An exploration into the generality of the addition of thiazole anions to nitriles allowed us to make a variety of thiazole ketones in good to excellent yields. The non-odorous thiolate-mediated demethylation reaction used in the synthesis of 1 is also presented.
A practical preparation of 5-(ketoaryl)thiazoles
Marcantonio, Karen M.,Frey, Lisa F.,Murry, Jerry A.,Chen, Cheng-Yi
, p. 8845 - 8848 (2007/10/03)
This article describes a facile synthesis of 2-substituted-5-(ketoaryl)thiazoles, which are important intermediates for the synthesis of biologically active compounds. A variety of 2-substituted thiazole anions were added to aryl nitriles to provide the desired ketones after aqueous hydrolysis.
An Easy General Synthesis of 2-(N,N-Dialkylamino)thiazol-5-yl Aldehydes and Ketones
Sawhney, Indu,Wilson, John R. H.
, p. 329 - 331 (2007/10/02)
Reaction between 2-chloro-5-thiazolyl-lithium and N,N-dialkylformamides or amides gave 2-N,N-dialkylaminothiazol-5-yl aldehydes or ketones on quenching with water.Quenching with acid gave 2-chlorothiazole-5-yl aldehydes or ketones, from which chloride was easily displaced by free amines.
