The apical sodium--dependent bile acid transporter (ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation. Inhibition of ASBT could increase the excretion of bile acids, thus increasing bile acid synthesis and consequently cholesterol consumption. Therefore, ASBT is an attractive target for developing new cholesterol-lo...

In the present work a series of novel coumarin-3-carboxamides and their hybrids with the alpha-lipoic acid were designed, synthesized and tested as potent antioxidant and anti-inflammatory agents. The new compounds were evaluated for their antioxidant activity, their activity to inhibit in vitro lipoxygenase and their in vivo anti-inflammatory activity. In general, the derivatives were generall...

12-Carboxamido- and 12-carboxyl-11-spirostenes were synthesized from the corresponding 12-iodo-11-ene derivative in palladium-catalyzed carbonylation reactions under mild reaction conditions. The synthesis of the iodo-alkene substrate is based on the transformation of the 12-keto derivative (hecogenin) to hydrazone, which was treated with iodine in the presence of a base (1,1,3,3-tetramethyl gu...

The well-known aminoazoles, 3-amino-5-methylisoxazole and 5-amino-N-aryl-1H-pyrazole-4-carboxamides, were studied as an amine component in Ugi and Groebke-Blackburn-Bienaymé multicomponent reactions. The first example of an application of aminoazoles in an Ugi four-component reaction was discovered and novel features of a Groebke-Blackburn-Bienaymé cyclocondensation are established and discusse...

2-Chloroquinoline-3-carbaldehyde 1 reacts with 2-cyanoacetohydrazide in ethanol to result in 1-[1-aza-2-(2-chloro(3quinolyl))vinyl]-2-cyanoacetamide 2. Phenyl isothiocyanate added to a stirred solution of compound 2, sulphur and triethylamine in a mixed solvent of dimethylformamide : ethanol to result in N-[1-aza-2-(2-chloro(3-quinolyl))vinyl](4amino-3-phenyl-2-thioxo(1,3-thiazoline-5-yl)) carb...

Overexpression of the efflux pump P-glycoprotein (P-gp) is one of the important mechanisms of multidrug resistance (MDR) in many tumor cells. In this study, 26 novel 5-oxo-hexahydroquinoline derivatives containing different nitrophenyl moieties at C4 and various carboxamide substituents at C3 were designed, synthesized and evaluated for their ability to inhibit P-gp by measuring the amount of r...

COX-2 inhibitory activities of some 1,4-dihydropyridine and 5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives were modeled by quantitative structure-activity relationship (QSAR) using stepwise-multiple linear regression (SW-MLR) method. The built model was robust and predictive with correlation coefficient (R2) of 0.972 and 0.531 for training and test groups, respectively. The quality of the mod...

2-Methylpyridinum p-toluenesulfonate ([2-MPy][p-TSA]) as a novel room temperature ionic liquidwas synthesized and evaluated as a recoverable catalyst for the one-pot synthesis ofhexahydroquinoline-3-carboxamide derivatives by four-component reaction of arylaldehydes,dimedone, acetoacetanilide and ammonium acetate in high to excellent yield in ethanol at 50 oC.The [2-MPy]...