Synthesis and antimicrobial, antiproliferative evaluation of novel quinolone and conazole analogues via conventional and microwave techniques
Yükleniyor...
Dosyalar
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
John Wiley and Sons Inc
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
1,2,4-Triazole-3-one (3), acquired from cinnamaldehyde was converted to the corresponding carbox(thio)amides via several steps (6 a–c). Their reaction with sodium hydroxide gave the 1,2,4-triazole derivatives (7 a–c). Compound 3 treatment with 2-bromo-1-(4-chlorophenyl) ethanone or 2-chloro-1-(2,4-dichlorophenyl)ethanone afforded the compounds 8 a,b and by reducing these compounds reduction products were obtained (9 a,b). The synthesis of (10 a–e) was carried out by the reaction compounds 9 a,b with different benzyl chlorides. Then oxadiazole derivative (12) was obtained by ring closure from hydrazide compound 5. Subsequently compounds 3, 7 a–c, and 12 were treated with various amines in the presence of formaldehyde to yield Mannich bases (11 a–e, 14 a–e, 13 a,b). Microwave-assisted and conventional techniques were utilized for the syntheses. The structures of newly synthesized compounds were illuminated by spectroscopic methods. Their antimicrobial (MIC method), and anticancer activities (Abay's method) were examined. Results showed that most of the compounds exhibited good antimicrobial activities. Especially compounds 14 a–e which is a mannich base showed very good antitubercular activity against Mycobacterium smegmatis compared with Streptomycin standard drug. Also compounds 8 a and 9 b have been found to have strong antiproliferative effects on the HeLa cervical cancer cells and also these compounds did not have a cytotoxic effects on a normal cells.
Açıklama
Anahtar Kelimeler
1,2,4-triazole, Anticancer, Antimicrobial activity, Mannich base, Quinolone
Kaynak
ChemistrySelect
WoS Q Değeri
Q3
Scopus Q Değeri
Q3
Cilt
6
Sayı
35
Künye
Ceylan, Ş., Cebeci, Y. U., Demirbaş, N., Karaoğlu, Ş. A., & Altun, M. (2021). Synthesis and Antimicrobial, Antiproliferative Evaluation of Novel Quinolone and Conazole Analogues via Conventional and Microwave Techniques, ChemistrySelect, 6(35), 9467-9476.
