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1.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 10): o3030, 2012 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-23125797

RESUMEN

In the title compound, C(21)H(16)N(2)O(2), the 3-nitro-phenyl and two phenyl rings are twisted from the mean plane of the enimino fragment by 44.4 (1), 37.2 (1) and 74.1 (1)°, respectively. The crystal packing exhibits no classical inter-molecular contacts.

2.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 5): o1040, 2011 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-21754367

RESUMEN

In the title compound, C(10)H(13)NO(2)S, the thio-phene and isoxazoline rings are almost coplanar, the dihedral angle between their least-squares planes being 2.08 (1)°. The O-H atoms of the methyl hy-droxy group and the N atom of the isoxazole ring are orientated in the same direction to allow for the formation of inter-molecular O-H⋯N hydrogen bonds that lead to a supra-molecular chain along the a axis.

3.
Int J Antimicrob Agents ; 31(6): 567-71, 2008 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-18337064

RESUMEN

Sulfometuron methyl (SM) is an inhibitor of acetohydroxyacid synthase (AHAS), the first common enzyme in the branched-chain amino acid biosynthetic pathway, and shows activity against Mycobacterium tuberculosis both in vitro and in vivo. To develop AHAS inhibitor derivatives with more potent activity, 100 sulfonylurea analogues were screened for antimycobacterial activity against M. tuberculosis and non-tuberculous mycobacteria (NTM), and then evaluated for intracellular activity using mouse macrophages. Three new compounds with antimycobacterial activity comparable with that of SM were identified. These compounds exhibit significant activity against intracellular M. tuberculosis (including the drug-resistant M. tuberculosis strains), and NTM Mycobacterium abscessus and Mycobacterium kansasii, respectively.


Asunto(s)
Acetolactato Sintasa/antagonistas & inhibidores , Antibacterianos/farmacología , Antituberculosos/farmacología , Inhibidores Enzimáticos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Mycobacterium/efectos de los fármacos , Animales , Antibacterianos/química , Antituberculosos/química , Células de la Médula Ósea/efectos de los fármacos , Inhibidores Enzimáticos/química , Macrófagos/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Relación Estructura-Actividad , Compuestos de Sulfonilurea/farmacología
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