ABSTRACT
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 44.4â (1), 37.2â (1) and 74.1â (1)°, respectively. The crystal packing exhibits no classical inter-molecular contacts.
ABSTRACT
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 2.08â (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-Hâ¯N hydrogen bonds that lead to a supra-molecular chain along the a axis.
ABSTRACT
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.
