1197342-24-7Relevant academic research and scientific papers
Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units
Choi, Peter J.,Sutherland, Hamish S.,Tong, Amy S.T.,Blaser, Adrian,Franzblau, Scott G.,Cooper, Christopher B.,Lotlikar, Manisha U.,Upton, Anna M.,Guillemont, Jerome,Motte, Magali,Queguiner, Laurence,Andries, Koen,Van den Broeck, Walter,Denny, William A.,Palmer, Brian D.
, p. 5190 - 5196 (2017)
Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and showed acceptable oral bioavailability, but there was only limited (and unpredictable) improvement in their hERG liability.
DIHYDROPYRAZOLE DERIVATIVES AS TYROSINE KINASE MODULATORS FOR THE TREATMENT OF TUMORS
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Page/Page column 23, (2011/04/18)
Compounds of the formula I, in which R1, R2, R3′, R3, R4 and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
