- Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles
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Two series of oxazolidinone derivatives having substituted isoxazoles were synthesized and tested for antibacterial activities against several Gram-positive strains including the resistant strains of Staphylococcus and Enterococcus, such as MRSA, CRSA, MSSA and VRE. Some of them showed in vitro activities (MIC) comparable or superior to the reference compound vancomycin.
- Pae, Ae Nim,Kim, Hye Yeon,Joo, Hyun Jin,Kim, Bo Hyung,Cho, Yong Seo,Choi, Kyung Il,Choi, Jung Hoon,Koh, Hun Yeong
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p. 2679 - 2684
(2007/10/03)
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- Synthesis and structure-activity relationships of fused imidazopyridines: A new series of benzodiazepine receptor ligands
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2-Arylimidazo[4,5-c]quinolines and analogous fused imidazopyridines were synthesized and evaluated as benzodiazepine receptor ligands. Affinity to the receptors was greatly affected by the bulkiness of the aryl group at the 2- position, compared to the pyrazoloquinolines such as CGS-9896. Derivatives with an isoxazole moiety at the 2-position showed high binding affinity and in vivo activity. In the imidazo[4,5-c]quinoline series, substitution at the 6-position decreased or abolished activity. Most derivatives with an unsubstituted isoxazolyl group showed antagonist or inverse agonist activity except for the 7-halo analogues, which exhibited agonist activity. On the other hand, 5-methylisoxazol-3-yl or 3-methylisoxazol-5-yl derivatives generally exhibited agonist activity. A similar substitution effect on the isoxazole moiety was observed in the imidazopyridines fused with a nonaromatic ring. From the detailed pharmacological evaluation, S-8510, 2- (3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine monophosphate, possessing weak inverse agonist activity was selected as a therapeutic candidate for the treatment of some symptoms of senile dementia.
- Takada, Susumu,Sasatani, Takashi,Chomei, Nobuo,Adachi, Makoto,Fujishita, Toshio,Eigyo, Masami,Murata, Shunji,Kawasaki, Kazuo,Matsushita, Akira
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p. 2844 - 2851
(2007/10/03)
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