256950-42-2Relevant academic research and scientific papers
Computer-Assisted Selective Optimization of Side-Activities—from Cinalukast to a PPARα Modulator
Pollinger, Julius,Schierle, Simone,Neumann, Sebastian,Ohrndorf, Julia,Kaiser, Astrid,Merk, Daniel
, p. 1343 - 1348 (2019)
Automated computational analogue design and scoring can speed up hit-to-lead optimization and appears particularly promising in selective optimization of side-activities (SOSA) where possible analogue diversity is confined. Probing this concept, we employ
Discovery of inhibitors of Escherichia coli methionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity
Wang, Wen-Long,Chai, Sergio C.,Huang, Min,He, Hong-Zhen,Hurley, Thomas D.,Ye, Qi-Zhuang
experimental part, p. 6110 - 6120 (2009/10/23)
Methionine aminopeptidase (MetAP) is a promising target to develop novel antibiotics, because all bacteria express MetAP from a single gene that carries out the essential function of removing N-terminal methionine from nascent proteins. Divalent metal ion
A simple route to new phenanthro- and phenanthroid-fused thiazoles by a PIFA-mediated (hetero)biaryl coupling reaction
Moreno, Isabel,Tellitu, Imanol,Dominguez, Esther,SanMartin, Raul
, p. 2126 - 2135 (2007/10/03)
An application of the PIFA-mediated [PIFA: phenyliodine(III) bis(trifluoroacetate) biaryl coupling reaction is presented and extended to the formation of heterobiaryl connections. A preliminary study of the scope and limitations of this procedure was carried out in the synthesis of phenanthroids 11 from a series of phenethyl-substituted heterocycles 10, It was observed that in some cases a competitive dimerization process took place. It was also found that the coupling step could be efficiently extended to a larger number of examples if an aromatic ring were situated fused to the 1,2-diarylethane skeleton, as in 23 and 30. The synthesis of a series of 4,5-diarylthiazoles 23a-g was therefore carried out to explore the electronic requirements and the regioselectivity of the PIFA-mediated non-phenolic coupling reaction. When the same procedure was applied to aryl-heteroarylthiazoles 30, a series of phenanthroid-fused thiazoles 31 was obtained in good overall yields. To the best of our knowledge, no oxidative aryl-heteroaryl coupling reaction of this type had previously been reported. Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
