Homoallenic alcohols are prepared from propargyl vinyl ethers using a trinuclear gold(I)-oxo complex, [(Ph3PAu)3O]BF4, as a catalyst for propargyl Claisen rearrangement at room temperature. The gold(I)-catalyzed reaction is effective for a diverse collection of propargyl vinyl ethers, including substrates containing aryl and alkyl groups at the propargylic position, and hydrogen, aryl, and alky...

Synthesis of an antagonist, SR141716A, that selectively binds to brain cannabinoid (CB(1)) receptors without producing cannabimimetic activity in vivo, suggests that recognition and activation of cannabinoid receptors are separable events. In the present study, a series of SR141716A analogs were synthesized and were tested for CB(1) binding affinity and in a battery of in vivo tests, including ...

The first synthesis of hydroxamic acids from alcohols has been developed. Both benzylic and aliphatic alcohols can be tolerated and applied in this reaction. The methodology is economical, environmentally benign and high yielding.

A series of novel water-soluble beta-carbolines bearing a flexible amino side chain was designed, synthesized and evaluated as potent cytotoxic and DNA intercatalating agents. The N(9)-arylated alkyl substituted beta-carbolines represented the most interesting cytotoxic activities. The results suggested that (1) the N(9)-arylated alkyl substituents of beta-carboline nucleus played a very import...

A series of iron complexes bearing a bis(imino)pyridine ligand were synthesised and examined as precatalysts for homopolymerisation of propylene. The alkyl substituents attached to the aryl group on the imine nitrogen atoms significantly affected the catalytic activity and molecular weight of the obtained polypropylenes. Copolymerisation of propylene and various allyl comonomers catalysed by ir...

Oxidation of azafulleroids with peracids regenerated C60 depending on the N-substituents. Alkyl-substituted azafulleroids preferred the oxidation of nitrogen to afford N-oxides as possible intermediates for C60 in moderate yields. Phenyl- and tosyl-substituted azafulleroids rather allowed the oxidation at the carbon cage. Theoretical calculations predicted the order of reactivity of azafulleroi...

The synthesis of a series of new 4-amino-5-alkyl-1,2,4-triazole(4H)-3-yl thioacetanilides and 4-pyrrolyl-5-alkyl-1,2,4-triazole(4H)-3-yl thioacetanilides has been described in the article. The key intermediates – 4-amino-5-alkyl-3-mercapto-1,2,4-triazoles(4H) 4a-c were synthesized started from the corresponding carboxylic acids (acetic, propanoic and butanoic) after their esterification followe...

Some alkyl and aryl derivatives of 9H-purine-6-thiol were synthesized and evaluated in vitro and in vivo for potential antithyroid effects. Spectrophotometric studies demonstrated 1:1 charge transfer complexation between iodine and these compounds with quite high values of the formation constants. The blood assays of rats treated with these compounds revealed significant antithyroid activity fo...

In the present work a new series of 3-alkyl-2,6-diarylpiperidin-4-one-2-thienoyl hydrazones have synthesized by the reaction of 3-alkyl-2, 6-diarylpiperidin-4-one with 2-thiophenecarboxylic acid hydrazide and characterized by spectral (IR, H NMR, C NMR, HSQC, HMBC, NOESY and COSY) techniques. The hydrazones were screened for their in vitro antibacterial and antifungal activities against some se...