Naslov
Synthesis, antiproliferative, antibacterial activity and DNA/RNA binding of novel amidino- substituted benzimidazoles and benzothiazoles

Autori
Rep, Valentina ; Glavaš-Obrovac, Ljubica ; Ivo Crnolatac, Ivo ; Radić Stojković, Marijana ; Čipčić Paljetak, Hana ; Matijašić, Mario ; Perić, Mihaela ; Raić-Malić, Silvana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, ostalo, znanstveni

Skup
37th National Medicinal Chemistry Symposium, American Chemical Society Division of Medicinal Chemistry

Mjesto i datum
New York City (NY), Sjedinjene Američke Države, 26.06.2022. - 29.06.2022

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
benzimidazoles ; benzothiazoles ; antiproliferative activity ; antibacterial activity ; DNA/RNA binding

Sažetak
In recent years, the number of treatment failures associated with the development of drug resistant cancer cells and pathogens has increased with an alarming rate. In addition, the growing prevalence of hospital and community-acquired infections caused by multidrug-resistant (MDR) bacterial pathogens is limiting the options for effective antibiotic therapy. Therefore, new agents are needed to overcome emerging resistance problems. This has prompted the search of azole pharmacophores, among which benzimidazole and benzothiazole derivatives have found to be efficacious for combating these fatal diseases [1, 2]. In continuation of our recent work on the development of aromatic amidines as cytostatic and antibacterial agents [3-6], herein we have designed and synthesized the tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles with a range of cyclic, aromatic and aliphatic substituents at phenoxy central core (Figure). Their antiproliferative and antibacterial activity will be presented. Compounds with most potent activity were further investigated on their DNA binding affinities by UV-Vis and CD spectroscopy, as well as thermal denaturation experiments to elucidate type of interactions with DNA.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA