349576-90-5

Upstream product

• 5856-79-1 iso-butyl chloroformate 
• 63-74-1 sulfanilamide 

Relevant academic research and scientific papers

Syntheses and evaluation of anticonvulsant profile and teratogenicity of novel amide derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide

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.

SULFANYLAMIDE DERIVATIVES, USES THEREOF AND COMPOSITIONS COMPRISING THEM

The present invention concerns a family of sulfanilamide derivatives of formula (I) as anticonvulsant agents, where R1 is selected from optionally substituted C4-C9 alkyl, optionally substituted C6-C10 aryl, optionally substituted C6-C10 alkylenearyl and optionally substituted C5-C10 heteroaryl; R2 is selected from -H and optionally substituted C1-C6 alkyl; each of R3 and R4, independently of each other, is selected from -H, optionally substituted C1-C6 alkyl, optionally substituted C6-C10 aryl and optionally substituted C5-C10 heteroaryl; n is 0, 1, 2, 3 or 4. The derivatives have been prepared and their anticonvulsant profile was evaluated for the control of epileptic seizures.