3302-11-2Relevant articles and documents
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Newman,M.S.,Fukunaga,T.
, p. 1176 - 1178 (1963)
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Syntheses and evaluation of anticonvulsant profile and teratogenicity of novel amide derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide
Hen, Naama,Bialer, Meir,Wlodarczyk, Bogdan,Finnell, Richard H.,Yagen, Boris
experimental part, p. 4177 - 4186 (2010/09/04)
Despite the availability of 14 new antiepileptic drugs (AEDs), about 30% of epileptic patients are not seizure-free. Consequently there is substantial need to develop new effective AEDs. A novel class of aromatic amides composed of phenylacetic acid or branched aliphatic carboxylic acids, with five to nine carbons in their carboxylic moiety, and aminobenzenesulfonamide were synthesized and evaluated in the anticonvulsant rat-maximal electroshock (MES) and subcutaneous metrazol seizure (scMet) tests. Fourteen of the synthesized amides had an anticonvulsant ED50 of 50 values of 7.6, 9.9, and 9.4 mg/kg and remarkable protective index (PI = TD 50/ED50) values of 65.7, 50.5, and 53.2, respectively. These potent sulfanylamides caused neural tube defects only at doses markedly exceeding their effective dose. The anticonvulsant properties of these compounds make them potential candidates for further development as new, potent, and safe AEDs.
Thioketene Syntheses, VI. Stable Thioketenes via Thionation of Sterically Hindered Acyl Chlorides
Schaumann, Ernst
, p. 2755 - 2765 (2007/10/02)
Sterically hindered acyl chlorides 11 are accessible via alkylation of the ester 1 or via chain elongation of the ketones 4 by one carbon atom in practicable, though multi-step reaction sequences.Action of phosphorus pentasulfide/pyridine on 11 leads to t
