Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[( N -cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors

Crystal structure and Hirshfeld surface analysis of hexyl 1-hexyl-2-oxo-1,2-dihydroquinoline-4-carboxylate

“…Quinoline derivatives represent an important class of heterocyclic compounds utilized as pharmaceuticals (Chu et al, 2019). They possess various biological properties such as antibacterial (Panda et al, 2015), anticancer (Tang et al, 2018), antitubercular (Xu et al, 2017), antiviral (Sekgota et al, 2017), anti-HCV (Cannalire et al, 2016), antimalarial (Hu et al, 2017), anti-Alzheimer's (Bolognesi et al, 2007), antileishmanial (Palit et al, 2009) and anti-inflammatory (Pinz et al, 2016) activities.…”

Quinolone derivatives: Potential anti‐HIV agent—development and application

“…Integrase (IN) represents a clinically validated target for the development of anti‐HIV agents, so it is worth to search for new lead compounds with HIV‐1 IN inhibition potential. A series of 3‐[( N ‐cycloalkylamino)methyl]‐2‐quinolones ( 2 and 3 ) were screened as potential HIV‐1 IN inhibitors by Sekgota et al, and nearly all the compounds exhibited a measure of HIV‐1 IN inhibition at 20 µM. None of the compounds showed significant inhibition to either HIV‐1 protease (PR) or reverse transcriptase (RT), suggesting that these derivatives could selectively inhibit HIV‐1 IN.…”

Quinolone derivatives and their antifungal activities: An overview

“…2‐Quinolone (carbostyrils or 1‐aza coumarins) derivatives GSK945237 and AZD9742 (Figure ) are under clinical trials for the treatment of infections caused by various bacteria, and 2‐quinolone derivatives as potent and selective antimicrobial agents have stimulated remarkable interest in medicinal chemistry.…”

“…Quinolones which can be divided into 2‐quinolones and 4‐quinolones (Figure ) possess a variety of pharmacological properties such as antibacterial, anticancer, antitubercular, antimalarial, anti‐HIV and antifungal properties, and occupy an important place in the development of new drugs. Combined application of available antifungal drugs (such as fluconazole and amphotericin B) and quinolone antibiotics (such as trovafloxacin) has additive‐to‐synergistic activities over the use of antifungal drugs alone, suggesting that this may be a viable avenue to pursue the pending development of specific antifungal quinolones …”