331274-56-7Relevant articles and documents
Cytotoxic effect of a family of peroxisome proliferator-activated receptor antagonists in colorectal and pancreatic cancer cell lines
Ammazzalorso, Alessandra,De Lellis, Laura,Florio, Rosalba,Bruno, Isabella,De Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Maccallini, Cristina,Perconti, Silvia,Verginelli, Fabio,Cama, Alessandro,Amoroso, Rosa
, p. 1029 - 1035 (2017)
Recent studies report an interesting role of peroxisome proliferator-activated receptor (PPAR) antagonists in different tumor models, being these compounds able to perturb metabolism and viability in cancer cells. In this work, the identification of a nov
SULFANYLAMIDE DERIVATIVES, USES THEREOF AND COMPOSITIONS COMPRISING THEM
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Page/Page column 30, (2011/04/19)
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.
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.
Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB
Guezel, Oezlen,Innocenti, Alessio,Scozzafava, Andrea,Salman, Aydin,Supuran, Claudiu T.
experimental part, p. 4894 - 4899 (2009/12/04)
A series of aromatic/heterocyclic sulfonamides incorporating phenyl(alkyl), halogenosubstituted-phenyl- or 1,3,4-thiadiazole-sulfonamide moieties and thienylacetamido; phenacetamido and pyridinylacetamido tails were prepared and assayed as inhibitors of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the cytosolic human (h) hCA I and hCA II, and the mitochondrial hCA VA and hCA VB. The new compounds showed moderate inhibition of the two cytosolic isoforms (KIs of 50-390 nM) and excellent inhibitory activity against the two mitochondrial enzymes, with many low nanomolar inhibitors detected (KIs in the range of 5.9-10.2 nM). All substitution patterns explored here lead to effective hCA VA/VB inhibitors. Some hCA VA/VB selective inhibitors were also detected, with selectivity ratios for inhibiting the mitochondrial over the cytosolic isozymes of around 55.5-56.9. As hCA VA/VB are involved in several biosynthetic processes catalyzed by pyruvate carboxylase, acetyl CoA carboxylase, and carbamoyl phosphate synthetases I and II, providing the bicarbonate substrate to these carboxylating enzymes involved in fatty acid biosynthesis, their selective inhibition may lead to the development of antiobesity agents possessing a new mechanism of action.
Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors
Guezel, Oezlen,Innocenti, Alessio,Scozzafava, Andrea,Salman, Aydin,Supuran, Claudiu T.
experimental part, p. 3170 - 3173 (2010/03/24)
A series of aromatic/heterocyclic sulfonamides incorporating phenyl(alkyl), halogenosubstituted-phenyl- or 1,3,4-thiadiazole-sulfonamide moieties and thienylacetamido; phenacetamido- and pyridinylacetamido tails were prepared and assayed as inhibitors of cytosolic human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms hCA I, II and VII. The new compounds showed moderate inhibition of the two ubiquitous isoforms I and II (KIs of 50-390 nM) and excellent inhibitory activity against the brain associated hCA VII (KIs in the range of 4.7-8.5 nM). Isoform VII highly selective inhibitors are being detected for the first time, with selectivity ratios for inhibiting CA VII over CA II of 11-75, and for inhibiting CA VII over CA I of 10-49, which may be useful for understanding the role of CA VII in epileptogenesis and other physiologic processes.
