Syntheses and Cytotoxic, Antimicrobial, Antifungal and Cardiovascular Activity of New Quinoline Derivatives

Abstract

New derivatives of quinoline (CAS 91-22-5, Z-1) were synthesized and their potential therapeutical significance and structure-activity relationship were tested. The brine shrimp bioassay was carried out to study their in vitro cytotoxicity, and besides, also their antimicrobial, antifungal and cardiovascular activities were investigated. Some structures showed a high degree of activity on the isolated rabbit jejunum. Extensive spectroscopic techniques such as EIMS, FABMS, peak matching MS, UV, IR and 1H NMR were employed to confirm the structure of the synthetic products.

Synthesis and antimicrobial activity of some new 1,3-thiazoles, 1,3,4-thiadiazoles, 1,2,4-triazoles and 1,3-thiazines incorporating acridine and 1,2,3,4-tetrahydroacridine moieties

“…The structures of the latter products 11 and 12 were established on the basis of their elemental analysis and spectral data (See experimental section). Agar-diffusion technique was used for the determination of the preliminary antibacterial and antifungal activities [40,41]. Cephalothin, Chloramphenicol and Cycloheximide were used as reference drugs for Gram positive bacteria, Gram negative bacteria and fungi, respectively.…”

Synthesis and antimicrobial activity of chromone-linked 2-pyridone fused with 1,2,4-triazoles, 1,2,4-triazines and 1,2,4-triazepines ring systems

“…The test was performed on medium potato dextrose agars (PDA) which contain infusion of 200 g potatoes, 6 g dextrose and 15 g agar. 26 Uniform size filter paper disks (3 disks per compound) were impregnated with equal volume (10 µL) from the specific concentration of dissolved tested compounds and carefully placed on inoculated agar surface. After incubation for 36 h at 27 °C in the case of bacteria and for 48 h at 24 °C in the case of fungi, inhibition of the organisms was measured and used to calculate mean of inhibition zones.…”

A new approach for the synthesis of bioactive heteroaryl thiazolidine-2,4-diones

“…The test was performed on medium potato dextrose agar (PDA) which contains infusion of 200 g potatoes, 6 g dextrose and 15 g agar. 27 Uniform size filter paper disks (3 disks per compound) were impregnated by equal volume (10 µL) from the specific concentration of dissolved tested compounds and carefully placed on the inoculated agar surface. After incubation for 36 h at 27 °C in the case of bacteria and for 48 h at 24 °C in the case of fungi, inhibition of the organisms was measured and used to calculate mean of inhibition zones.…”