68523-22-8Relevant academic research and scientific papers
Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors
Song, Lijun,Merceron, Romain,Hulpia, Fabian,Lucía, Ainhoa,Gracia, Bego?a,Jian, Yanlin,Risseeuw, Martijn D.P.,Verstraelen, Toon,Cos, Paul,Aínsa, José A.,Boshoff, Helena I.,Munier-Lehmann, Hélène,Savvides, Savvas N.,Van Calenbergh, Serge
, (2021/08/27)
Mycobacterium tuberculosis thymidylate kinase (MtTMPK) has emerged as an attractive target for rational drug design. We recently investigated new families of non-nucleoside MtTMPK inhibitors in an effort to diversify MtTMPK inhibitor chemical space. We here report a new series of MtTMPK inhibitors by combining the Topliss scheme with rational drug design approaches, fueled by two co-crystal structures of MtTMPK in complex with developed inhibitors. These efforts furnished the most potent MtTMPK inhibitors in our assay, with two analogues displaying low micromolar MIC values against H37Rv Mtb. Prepared inhibitors address new sub-sites in the MtTMPK nucleotide binding pocket, thereby offering new insights into its druggability. We studied the role of efflux pumps as well as the impact of cell wall permeabilizers for selected compounds to potentially provide an explanation for the lack of correlation between potent enzyme inhibition and whole-cell activity.
A CONVENIENT METHOD FOR THE PREPARATION OF 6-PHENOXY-2-PYRIDINECARBALDEHYDE
Ozawa, Kiyomi,Ishii, Shigeru,Hatanaka, Masataka
, p. 1803 - 1804 (2007/10/02)
6-Phenoxy-2-pyridinecarbaldehyde was prepared in good yields through a few reaction steps utilizing Grignard reaction which has been regarded disadvantageous for preparation of pyridinecarbaldehydes.
6-(Substituted phenoxy)-2-di-(substituted phenoxy)methyl pyridines
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, (2008/06/13)
Compounds are prepared corresponding to the formula STR1 wherein Y represents chloro or R'; R represents STR2 wherein X independently represents alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, alkyl sulfonyl
Phenoxypyridinemethyl esters of 4-alkenoic acids
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, (2008/06/13)
Novel phenoxypyridinemethyl esters of 4-alkenoic acid compounds having pesticidal activity and methods of their preparation.
