An efficient and practical procedure for the synthesis of esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, has been developed. The intermediate, 2-methylene-4-(4-methylphenyl)-4-oxobutanoic acid (2), was prepared by Friedel-Crafts acylation of toluene with itaconic anhydride (3) in the presence of aluminum trichloride and nitrobenzene in ...

A series of six Bodipy derivatives, namely 4,4-difluoro-8-(4-amidophenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene (1), 4,4-difluoro-8-(4-methylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene (2), 4,4-difluoro-8-(4-nitrylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene (3), 4,4-difluoro-8-(4-amidophenyl)-3,5-dimethyl-4-bora-3a,4a-diaza-s-indacene (4), 4,4-difluoro-8-...

objective(s): recently, phthalimide derivatives were designed based on ameltolide and thalidomide as they possess a similar degree of anticonvulsant potency due to their phenytoin-like profile. the ability of phthalimide pharmacophore to interact with neuronal voltage-dependent sodium channels was studied in the batrachotoxin affinity assay. therefore, in the present study, a series of 19 compo...

  Objective(s): Recently, phthalimide derivatives were designed based on ameltolide and thalidomide as they possess a similar degree of anticonvulsant potency due to their phenytoin-like profile. The ability of phthalimide pharmacophore to interact with neuronal voltage-dependent sodium channels was studied in the batrachotoxin affinity assay. Therefore, in the present study, a series of 19 com...

Novel acyclic nucleoside phosphonates with a pyrimidine base preferentially containing an amino group at C-2 and C-4 and a 2-(phosphonomethoxy)ethoxy or (R)-2-(phosphonomethoxy)propoxy group at C-6 selectively inhibit the replication of wild-type and lamivudine-resistant hepatitis B viruses. The activity of the most potent compounds was comparable to that of adefovir.

Evaluation the antinociceptive and antiinflammatory effect, of new rigid, propoxy benzopyrane-3,4 Di-hydroxychalcone derivative by Hot-plate, Formaline and Plethysmography Payam Khazaeli, Mamoud Reza Heidari, Alireza Foroumadi, Mehdi Kalati From 1 International Congress on Neurobiology and Clinical Psychopharmacology and European Psychiatric Association Conference on Treatment Guidance Thessalo...

The occurrence of metabolites of many commonly used herbicides in streams has not been studied extensively in tile-drained watersheds. We collected water samples throughout the Upper Embarras River watershed [92% corn, Zea mays L., and soybean, Glycine max (L.) Merr.] in east-central Illinois from March 1999 through September 2000 to study the occurrence of atrazine (2-chloro-4-ethylamino-6-iso...

Background and Objective: Regarding the prevalence of epilepsy in human society and with respect to insufficiency of usual treatments, new strategies and methods for medical treatment of epileptic patients are necessary. As NMDA receptor antagonists are the most prominent anti-epileptic drugs, in the present study, we synthesized and investigated anti-epileptic effect of a new piperidine deriva...