- Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase
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Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this class of molecules by variation of two parts of the molecule, the phenyl and triazolopyrimidine rings. SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action.
- Patil, Vikas,Kale, Manoj,Raichurkar, Anandkumar,Bhaskar, Brahatheeswaran,Prahlad, Dwarakanath,Balganesh, Meenakshi,Nandan, Santosh,Shahul Hameed
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supporting information
p. 2222 - 2225
(2014/05/06)
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- N-(phenylsulfonyl)picolinamide derivatives, process for producing the same, and herbicide
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A herbicide containing as the active ingredient an N-(henylsulfonyl)picolinamide derivative represented by general formula (I) wherein X reprcsents a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, a C1-4 haloalkoxy, a (C1-4 alkoxy)carbonyl, a [di(C1-4 alkyl)amino]sulfonyl, an [N—(C1-4 alkyl)-N—(C1-4 alkoxy)amino]sulfonyl, a (C1-4 alkylamino)sulfonyl, a C1-4 alkylthio, a C1-4 alkylsulfinyl, a C1-4 alkylsulfonyl, or nitro; n is an integer of 0 to 5; Y represets a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, C1-4 haloalkoxy, a C1-4 alkylthio, a C1-4 haloalkylthio, amino, a C1-4 alkylamino, a di(C1-4 alkyl)amino, a (C1-4 alkoxy) C1-4 alkyl, a (C1-4 alkylthio) C1-4 alkyl, or nitro; and m is an integer of 0 to 4. This active ingredient is synthesized by condensing a substituted picolinic acid with a substituted benzenesulfonamide under dehydration, or by reacting the phenyl ester of a substituted picolinic acid with a substituted benzenesulfonamide in the presence of a basic compound.
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- Method of preparing 2-trifluoromethoxy-benzenesulphonamide
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2-Trifluoromethoxy-benzenesulphonamide, of the formula (I), STR1 which can be used as intermediate for the preparation of certain herbicidally active compounds is obtained in very high yield and high purity by a process in which halogenated trifluorometho
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