staphylococcus aureus causes a wide variety of infections worldwide. methicillin-resistant s. aureus is one of most common causes of nosocomial and community acquired infections. the fluoroquinolones are an important class of antibiotics that used to treat infections caused by s. aureus. today, a significant increase in the rate of ciprofloxacin resistance in methicillin-resistant s. aureus str...

Staphylococcus aureus causes a wide variety of infections worldwide. Methicillin-resistant S. aureus is one of most common causes of nosocomial and community acquired infections. The fluoroquinolones are an important class of antibiotics that used to treat infections caused by S. aureus. Today, a significant increase in the rate of ciprofloxacin resistance in methicillin-resistant S. aureus str...

This article describes one-pot synthesis of new fluorinated hexahydroquinoline derivatives via unsymmetric Hantzsch reaction involving 5-trifluoromethyl-1,3cyclohexanedione, aldehydes, acetoacetate ester, and ammonium acetate in trifluoroethanol (TFE). The reaction is simple and rapid with high yield.

a series of new hexahydroquinoline and 1,4-dihydropyrimidine derivatives were synthesized. condensation of 2-methyl- thiazole-4-carboxaldehyde (1) with 1,3-cyclohexanedione and alkyl 3- aminocrotonate afforded 4-(2-methyl-thiazol-4-yl)-hexahydroquinoline while condensation of aldehyde (1) with benzoyl acetone and thiourea gave 1,4-dihydropyrimidine derivatives. the stereochemistry of 1,4-dihydr...

A series of new hexahydroquinoline and 1,4-dihydropyrimidine derivatives were synthesized. Condensation of 2-methyl- thiazole-4-carboxaldehyde (1) with 1,3-cyclohexanedione and alkyl 3- aminocrotonate afforded 4-(2-methyl-thiazol-4-yl)-hexahydroquinoline while condensation of aldehyde (1) with benzoyl acetone and thiourea gave 1,4-dihydropyrimidine derivatives. The stereochemistry of 1,4-dihydr...

The reaction of cyanothioacetamide with aromatic aldehydes and 1,3-dicarbonyl compounds followed by aminomethylation or S-alkylation gave a series heterocyclic derivatives 1,2,3,4-tetrahydropyridine 1,4,5,6,7,8-hexahydroquinoline fragment. resulting were tested for analgesic activity in vivo. Some the prepared showed an antinociceptive effect superior to that ketorolac dynamics.

2-Oxo-4-phenyl-1,2,5,6,7,8-hexahydroquinoline-3-carbonitrile (10) reacted with hydrazine hydrate, phenylisothiocyanate or benzoyl chloride to give derivatives 12, 13 and 15, respectively. The latter two products were treated with hydrazine hydrate to afford pyrozole[3,4-b]quinolines derivatives 14 and 16, respectively. Compound 10 also reacted with acetonitrile dimer or malononitrile dimer to y...

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...