(E)-1-aryl-2,4-bis(trimethylsilyl)but-1-en-3-ynes readily undergo protodesilylation and subsequent aerobic, copper-free Sonogashira cross-coupling with aryl halides to form (E)-1,4-diaryl-2-(trimethylsilyl)but-1-en-3-ynes. The proposed one-pot, two-step approach allows access the isomers containing substituents in mutual syn positions. resulting 2-silyl enynes can be further converted by proto-...

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

The aryl-(Z)-N-[2-amino-1,2-dicyanovinyl]formamidine 2 cyclize in solvent-free conditions and in the presence of a base to give a 5-amino-1-aryl-4-cyanoimidazoles 3. Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 through reaction with aromatic amines at room temperature and in good to excellent yields. ...

Twenty-three new oxime ester derivatives of nafimidone were synthesized with the prospect of potential anticonvulsant activities. MES and ScM tests were employed for their anticonvulsant activities and rotorod test for neurological deficits. Eighteen compounds were found to be protective against MES seizures. Alkyl (1-8) and arylalkyl (9, 10) oxime ester derivatives were found to be more active...

a series of new 2-arylimino-3-aryl-5-[5?-(3,4-dichlorophenyl)-2?-furylidene]-4-thiazolidinones (3a-l) have been synthesised by the condensation of 5-(3,4-dichlorophenyl)-2-furaldehyde 1 with 2-arylimino-3-aryl-5h-4-thiazolidinones 2 in glacial acetic acid. the physical and spectral data of the synthesised compounds are determined. the synthesised compounds have been screened for their in vitro ...

N(1)-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT(6) receptors. Replacement of the aryl moiety with similarly hydrophobic alkyl substituents results in decreased affinity, as does replacement of a benzenesulfonyl moiety with a benzyl group. Current findings indicate that an aryl (or substituted aryl) sulfonyl (rather than alkylsulfonyl or benzyl) moiety is optimal for...

ABSTRACT The pseudo-Michael reaction of 1-aryl-4,5-dihydro-1H-imidazol-2-amines with ethyl 2-cyano-3-methoxyprop-2-enoate (ethyl ethoxymethylenecyanoacetate) is investigated. At -10 °C reaction takes place on the exocyclic nitrogen atom, giving exclusively ethyl esters of 2-cyano-3-[(1-phenyl-4,5-dihydro-1H-imidazol-2-yl)amino]prop-2-enoic acid. The formation of isomeric enamines which may be a...

Synthesis and anticonvulsant potential of certain new 6-aryl-9-substituted-6,9-diazaspiro[4.5]decane-8,10-diones (6a-l) and 1-aryl-4-substituted-1,4-diazaspiro[5.5] undecane-3,5-diones (6m-x) are reported. The intermediates 1-[(aryl)(cyanomethyl)amino] cycloalkanecarboxamides (3a-f) were prepared via adopting Strecker synthesis on the proper cycloalkanone followed by partial hydrolysis of the o...

3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimido[1,2-c][1,3]benzothiazin-6-imine were investigated for the development of mo...