antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs, chloroquine (cq) and amodiaquine (aq), have been used to prevent and treat malaria for many years. the importance of these drugs is related to their simple usage, high efficacy, affordability, and cost-effectiveness of their synthesis. in recent years, with the spread of parasite resistance to cq and cross-resist...

objective(s) in recent years highly selective cox-2inhibitors were withdrawn from the market because of an increased risk of cardiovascular complications. in this study we were looking for potent compounds with moderate selectivity for cox-2. so, four analogues of 4, 5-diaryl-2-(2-alkylthio-5-imidazolyl) imidazole derivatives were synthesized and their anti-inflammatory and anti-nociceptive act...

In this work, the optimization calculations were carried out on quetiapine hemifumarat, 4, and its analogues, 1-5. These calculations were carried out using the B3LYP/6-31G(d) level of theory. The DFT calculations clarified a boat structure for dibenzothiazepine moiety of the molecule which piperazine moiety has a chair conformation. Thermal energies (E), enthalpies (H), and free energies (G) o...

the effects of adenosine,5-n-ethylcarbox-amidoadenosine (neca), 2-chloroadenosine (2-ca), n6-phenyiisopropyladenos'tne (l-pia and d-pia) and n6 -cyclohexyladenos'tne (cha) were examined on the mouse isolated vas deferens. all the compounds in a concentration-dependent manner inhibited electrically induced contrac¬tions. ic of adenosine and its analogues were 13.68 ± 5.97 for ado, 0.736 ± 0.087 ...

An intramolecular palladium catalysed carbometalation followed by anion capture achieves construction of a model comprised of the A ring of Vitamin D oxygen analogues.

  Objective(s): Nowadays, COX- 2 inhibitors such as valdecoxib are removed from the market because of their cardiovascular toxicity and their potential to increase the risk of strokes. In response to this, medicinal chemists have attempted to synthesize new classes of COX-2 Inhibitors.   Materials and Methods: In this study, three novel analogues of thiazolidin-4-ones derivatives ...

Using a-tetralone, as starting material, a series of phencyclidine analogues were synthesized. This ketone was reacted separately with ethylmagnesium bromide, P-methoxyphenylmagnesium bromide and P-methylphenylmagnesium bromide. The resultant alcohols were treated with a suspension of NaN3 and CCl3COOH in CHCl3. The azides were subsequently...

in this work, the optimization calculations were carried out on quetiapine hemifumarat, 4, and its analogues, 1-5. these calculations were carried out using the b3lyp/6-31g(d) level of theory. the dft calculations clarified a boat structure for dibenzothiazepine moiety of the molecule which piperazine moiety has a chair conformation. thermal energies (e), enthalpies (h), and free energies (g) o...

Background: Resistance to chloroquine (CQ) in Plasmodium falciparum malaria has become a major health concern of the developing countries.This resistance has prompted a re-examination of the pharmacology of alternative antimalarials that may be effective against resistant strains. Amodiaquine (AQ) is a 4-aminoquinoline antimalarial which is effective against many chloroquine-resistant strains o...

an intramolecular palladium catalysed carbometalation followed by anion capture achieves construction of a model comprised of the a ring of vitamin d oxygen analogues.