- Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones
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Novel 6-aryl benzimidazolones and benzothiazolones were prepared and examined as bioisosteres of the recently reported 6-aryl dihydroquinolines (1) for progesterone receptor (PR) antagonist activities. PR antagonist activities increased when compounds 9c-f possessed a more lipophilic group at position-1 and pendent aryl moiety para to NH moiety. Furthermore, conversion of carbonyl moiety of 9e,f to the thio-carbonyl led to benzoimidazolethiones 15a,b with significantly improved potency and binding affinity.
- Zhang, Puwen,Terefenko, Eugene A.,Wrobel, Jay,Zhang, Zhiming,Zhu, Yuan,Cohen, Jeffrey,Marschke, Keith B.,Mais, Dale
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- Regiospecific functionalization of 1,3-dihydro-2H-benzimidazol-2-one and structurally related cyclic urea derivatives
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Methods for selectively protecting one of the degenerate nitrogen atoms of the cyclic urea derivatives 1,3-dihydro-2H-benzimidazol-2-one (6a), 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (11), 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones (20), 1,3-dihydro-
- Meanwell,Sit,Gao,Wong,Gao,St. Laurent,Balasubramanian
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p. 1565 - 1582
(2007/10/02)
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