214894-89-0Relevant academic research and scientific papers
Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles
Sutherland, Hamish S.,Tong, Amy S.T.,Choi, Peter J.,Conole, Daniel,Blaser, Adrian,Franzblau, Scott G.,Cooper, Christopher B.,Upton, Anna M.,Lotlikar, Manisha U.,Denny, William A.,Palmer, Brian D.
, p. 1797 - 1809 (2018/02/28)
Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological results for these compounds indicate on average a lower clogP limit of about 5.0 in this series for retention of potent inhibitory activity (MIC90s) against M.tb in culture. Some of the compounds also showed a significant reduction in inhibition of hERG channel potassium current compared with bedaquiline, but there was no common structural feature that distinguished these.
ANTIBACTERIAL COMPOUNDS AND USES THEREOF
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Paragraph 0076, (2017/09/28)
The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.
Substituted oxygenated heterocycles and thio-analogues: Synthesis and biological evaluation as melatonin ligands
Charton, Isabelle,Mamai, Ahmed,Bennejean, Caroline,Renard, Pierre,Howell, Edward H.,Guardiola-Lemaitre, B.Eatrice,Delagrange, Philippe,Morgan, Peter J.,Viaud, Marie-Claude,Guillaumet, G.Erald
, p. 105 - 114 (2007/10/03)
A new series of substituted oxygenated heterocycles and thio-analogues were synthesized and evaluated as melatonin receptor ligands. The replacement of the indolic moiety of melatonin by heterocyclic skeleton such as 1,4- benzodioxin, 2,3-dihydro-1,4-benzodioxin, chroman, 2,3-dihydro-1,4- benzoxathiin, thiochroman, carrying the amidic chain on the aromatic ring, leads to compounds showing a weak affinity for melatonin receptors, except for the compounds 1cb and 1hb. (C) 2000 Elsevier Science Ltd.
Heterocyclic compounds
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, (2008/06/13)
The invention relates to compound of general formula (I): STR1 wherein: Z represents O or CH 2n is from 0 to 4R, X and Y are as defined in the description, andA represents STR2 wherein R 1, R 2, R 6, R 7 and T'' are as defined in the description,and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
