Synthesis and three-dimensional quantitative structure-activity relationship study of quinazoline derivatives containing a 1,3,4-oxadiazole moiety as efficient inhibitors against Xanthomonas axonopodis pv. citri.
Mol Divers
; 22(4): 791-802, 2018 Nov.
Article
em En
| MEDLINE
| ID: mdl-29808346
ABSTRACT
A series of quinazoline derivatives containing a 1,3,4-oxadiazole moiety were synthesized and evaluated for their antibacterial activities against Xanthomonas axonopodis pv. citri (Xac) and Ralstonia solanacearum (Rs). Antibacterial bioassays indicated that most of target compounds exhibited significant antibacterial activities against Xac and Rs in vitro. Strikingly, compounds 6d-6i, 6m-6r and 6u-6x showed antibacterial activity against Xac, with [Formula see text] values ranging from 14.42 to 38.91 [Formula see text]g/mL, which are better than that of bismerthiazol (39.86 [Formula see text]g/mL). Based on the antibacterial activity against Xac, comparative molecular filed analysis and comparative molecular similarity index analysis models were generated to investigate the structure-activity relationship of title compounds against Xac. The analytical results indicated that the above models exhibited good predictive accuracy and could be used as practical tools for guiding the design and synthesis of more potent quinazoline derivatives containing a 1,3,4-oxadiazole moiety.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Oxidiazóis
/
Quinazolinas
/
Relação Quantitativa Estrutura-Atividade
/
Xanthomonas axonopodis
/
Antibacterianos
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Mol Divers
Assunto da revista:
BIOLOGIA MOLECULAR
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
China