Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents

Synthesis and antileishmanial activity of novel pyridinium-hydrazone derivatives

“…These compounds comprising a diverse group of chemical structures have been reported as antileishmanial agents. Most of them include nitrogen heterocycle rings such as quinolines 9 , quinazolines 10 , acridines 11 , pyrimidines 12 , pyrazols 13 , pyridines 8 , benzothiazoles 14 , imidazoles 15 , thiadiazoles 16 and include functional structures such as alkyl phospholipids 17 , ether phospholipids 18 , chalcones 19 , amidines 20 , oximes 21 , amidoxime 22 , hydrazones 23 and hydrazides 24,25 . On the other hand, a number of quaternized amine derivatives such as thiadiazolium-phenylamine 26,27 , arylisoquinolinium 28 , imidazo-pyridinium 29 , alkylammonium-phenothiazines 30 , indolo-quinolinium 31 and naphthalimide-amonnium 32 were previously reported to exert antiprotozoal properties.…”

Synthesis of revised structure of klaivanolide (acetylmelodorinol)

“…The solution of 2-furanone (1 g, 11.9 mmol) in dry THF (10 mL) was added dropwise and stirring continued for another 30 minutes before addition of aldehyde 4 (2.11 g, 11.9 mmol) in 10 mL of dry THF. The reaction mixture stirred for 1.5 h at -78 ºC and quenched with 5 ml of saturated solution of NH 4 Cl and slowly warmed to room temperature, diluted with ether and washed with saturated solution of NH 4 Cl (10 mL). Solvent was removed under reduced pressure and crude product was dissolved in dry DCM, treated with triethylamine (1.5 mL), acetic anhydride (1.0 mL) and DMAP (catalytic) at room temperature for 2 h. diluted with water and washed with 1N HCl, saturated solution of NaHCO 3 , brine and dried over Na 2 SO 4 and purified by column chromatography gave 3 (1.7 g, 59% over two steps) as colorless oil.…”

“…[1][2][3][4][5][6][7] The available treatment for most parasitic diseases with the existing drugs suffer from several limitations such as toxicity, parenteral administration, emergence and spread of drug resistance. There is a need for the discovery of new drugs which address some of these issues.…”

Synthesis of Imidazole Derivatives and Their Biological Activities

“…The synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles were reported by Bhandari et al, (2010).Ketone (acetone, acetophenone or propiophenone) 98a-98c was reacted with pyrrolidine and paraformaldehydeunder asymmetric Mannich conditions in the presence of L-proline to give the corresponding Mannichproducts. Subsequent replacement of the pyrrolidine with imidazole (amine exchange reaction to give 99a and 99b, 99c) followed by sodium borohydridereduction gave the hydroxyl intermediates 100a-100c.…”