A series of quinazoline derivatives containing a 1,3,4-oxadiazole moiety were synthesized and evaluated for their antibac- terial 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 EC values ranging from 14.42 to 38.91 µg/mL, which are better than that of bismerthiazol (39.86 µg/mL). Based on the antibacterial activity against Xac, comparative molecular ﬁled analysis and comparative molecular similarity index analysis models were generated to investi- gate 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. Keywords Quinazoline · 1,3,4-Oxadiazole · Antibacterial activity · 3D-QSAR · Xanthomonas axonopodis pv. citri Introduction their pervasive application was greatly limited due to poor efﬁciency, negative impact on the environment, rapid emer- Xanthomonas axonopodis pv. citri (Xac), a destructive gency of pathogen resistance and high residue level . Gram-negative bacterium that can infect many important Thus, searching for novel
Molecular Diversity – Springer Journals
Published: May 28, 2018
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