Journal ArticleDOI
Synthesis and bioactivity evaluation of novel arylimines containing a 3-aminoethyl-2-[(p-trifluoromethoxy)anilino]-4(3H)-quinazolinone moiety.
TLDR
Results indicate that novel arylimine derivatives containing the 4(3H)-quinazolinone moiety can effectively control tobacco bacterial wilt, tomato bacterial wilts, and X. oryzae.Abstract:
Twenty-seven novel (E)-3-[2-arylideneaminoethyl]-2-[4-(trifluoromethoxy)anilino]-4(3H)-quinazolinone derivatives were synthesized by reacting various aromatic aldehydes with intermediate 6. The target compounds were characterized by 1H NMR, 3C NMR, IR, and elemental analysis. Bioassay results revealed that some of the compounds have strong antifungal activities against six fungi (Gibberella zeae, Fusarium oxysporum, Clematis mandshurica, Paralepetopsis sasakii, Phytophthora infestans, and Sclerotinia sclerotiorum) and three bacteria (Xanthomonas oryzae, tomato bacterial wilt, and tobacco bacterial wilt). Notably, these compounds exhibited the highest activity against tomato bacterial wilt and X. oryzae, with 50% effective concentration (EC50) values ranging from 45.96 to 93.31 μg/mL and from 20.09 to 21.33 μg/mL, respectively, which are superior to those of the commercial antibacterial agents thiodiazole-copper (99.80 μg/mL) and bismerthiazol (92.61 μg/mL). These results indicate that novel arylimine deri...read more
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Journal ArticleDOI
Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: synthetic approaches and multifarious applications.
TL;DR: This article is an effort to summarize recent developments in the environmentally benign synthetic methods providing access to quinazoline andQuinazolinone scaffolds with promising biological potential and discuss potential future directions on the development of more potent and specific analogues for various biological targets.
Journal ArticleDOI
Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: The advances continue
TL;DR: Recent developments in the eco-friendly and green procedures for the construction of highly challenging and potentially bioactive quinazoline and quinzolinone compounds are recapitulate in order to help medicinal chemists in designing and synthesizing novel and potent compounds for the treatment of different disorders.
Journal ArticleDOI
Quinazoline Synthesis via Rh(III)-Catalyzed Intermolecular C–H Functionalization of Benzimidates with Dioxazolones
TL;DR: An efficient double C-N bond formation sequence to prepare highly substituted quinazolines utilizing benzimidates and dioxazolones under the catalytic redox-neutral [Cp*RhCl2]2/AgBF4 system is reported.
Journal ArticleDOI
Design, synthesis, and antibacterial activity of novel Schiff base derivatives of quinazolin-4(3H)-one.
TL;DR: Results indicated that novel Schiff base derivatives containing the 4(3H)-quinazolinone moiety can effectively control tobacco and tomato bacterial wilts.
Journal ArticleDOI
Pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety as potential antiviral agents
Wang Yanyan,Xu Fangzhou,Yun-Ying Zhu,Baoan Song,Luo Dexia,Gang Yu,Shunhong Chen,Wei Xue,Jian Wu +8 more
TL;DR: Findings indicate that pyrazolo[3,4-d-d]pyrimidine derivatives containing a Schiff base may be potential antiviral agents.
References
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Journal ArticleDOI
Biological Properties of Schiff Bases and Azo Derivatives of Phenols
Journal ArticleDOI
Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains
TL;DR: A series of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells, and Piperazine-1-carbodithioate 8q exhibited significant inhibitory activity.
Journal ArticleDOI
Synthesis and antimicrobial activities of Schiff bases derived from 5-chloro-salicylaldehyde.
TL;DR: Among the compounds tested, (E)-4-chloro-2-((4-fluorobenzylimino)methyl)phenol showed the most favorable antimicrobial activity with MICs of 45.5 microg/mL against B. subtilis, E. coli, P. aureus and A. niger, respectively.
Journal ArticleDOI
Inhibition of tobacco bacterial wilt with sulfone derivatives containing an 1,3,4-oxadiazole moiety.
TL;DR: It is demonstrated that sulfone derivatives containing 1,3,4-oxadiazole can be used to develop potential bactericides for plants and the control effect of compound 5'j against tobacco bacterial wilt was better than that of the commercial bactericide Saisentong.
Journal ArticleDOI
Structure−Activity Relationships of Novel 2-Substituted Quinazoline Antibacterial Agents
P P Kung,M D Casper,K L Cook,Laura Wilson-Lingardo,Lisa M. Risen,Timothy A. Vickers,Raymond Ranken,Lawrence B. Blyn,Jacqueline R. Wyatt,Phillip Dan Cook,David J. Ecker +10 more
TL;DR: High-throughput screening of in-house compound libraries led to the discovery of a novel antibacterial agent, compound 1 (MIC: 12-25 microM against S. pyogenes), which displayed improved broad-spectrum antibacterial activity against a variety of bacterial strains.