Fungal, bacterial, and cancer cells can develop resistance against antifungal, antibacterial, or anticancer agents. Mechanisms of resistance are complex and often multifactorial. Mechanisms include: (1) Activation of ATP-binding cassette (ABC) transporters, such as P-gp, which pump out lipophilic compounds that have entered a cell, (2) Activation of cytochrome p450 oxidases which can oxidize li...

Heterocyclic compounds are widely prevalent in animal kingdom as well as in plant kingdom and they play various roles in metabolic processes. A large number of heterocyclic compounds are in clinical practice as a drug, while many of them find industrial utility and hence the syntheses of heterocyclic compounds and understanding of the biological importance of specific heterocyclic class will be...

Background: cinchona extract contains quinoline alkaloids, has telangiectatic activity, is practically insoluble in water so penetration into hair follicles low and requires a delivery system, namely cream. Objective: to determine the formula of cream with good physical stability safety. Methodology: bark extraction (soxhletation method), phytochemical screening, dosage determination, optimizat...

A novel seco-limonoid, rel-(1S,5R,9S,7R,8S,9R,10S,11R,13S,14R,15R,17R)-11,19-dihydroxy-7-acetoxy-7-deoxoichangin (raputiolide) (1), and two novel quinolone alkaloids N-methyl-2-phenoxyquinolin-4(1H)-one (heptaphyllone A) (2) and 6-methylbenzofuro[2,3-b]quinolin-4(1H)-one (heptaphyllone B) (3), along with the known seco-limonoid ichangin (4), were isolated from Raputia heptaphylla PITTIER (Rutac...

Quinoline is a hepatocarcinogen in rats and mice and a well-known mutagen in bacteria after incubation with rat liver microsomes. The specific cytochrome P450 enzymes involved in quinoline metabolism in human and rat liver microsomes were determined using cDNA-expressed cytochrome P450s, correlations with specific cytochrome P450-linked monooxygenase activities in human liver microsomes and inh...

Recent developments on antimicrobial quinoline chemistry were shortly reviewed covering six important topics: Historical aspects of the quinoline-based antimicrobial drug development; Increasing resistance problems and reasons for developing new antimicrobial agents; Molecular quinoline-based hybrids in the design and development of novel antimicrobial agents; Structural evolution of the quinol...