Taiping Hou

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Organization: Sichuan University
Department: Key Laboratory of Bio-Resource and Eco-Environment of Ministry of Education, College of Life Sciences
Title:
Co-reporter:Hui Deng;Zhi-Yi Yu;Guan-Ying Shi;Ming-Jing Chen;Ke Tao;Tai-Ping Hou
Chemical Biology & Drug Design 2012 Volume 79( Issue 3) pp:279-289
Publication Date(Web):
DOI:10.1111/j.1747-0285.2011.01308.x

Pyrazolines, the well-known five-membered nitrogen-containing heterocyclic compounds, have received considerable interests in the fields of medicinal and agricultural chemistry because of their broad spectrum of biological activities. To discover more potent antifungal compounds, a series of structurally related 1,3,5-trisubstituted-2-pyrazoline derivatives have been synthesized by introducing furan rings regarded as bioactive substructure into the scaffold of pyrazolines and tested for their activities against six plant pathogenic fungi in vitro. The preliminary bioassays indicated that almost all synthesized compounds had displayed variable growth inhibitory effects on the tested pathogenic fungi. In particular, compounds 4, 7, 9, 12, 18, 19, and 38 displayed excellent antifungal activities against Rhizoctonia solani and their inhibition of growth reached 100% at the concentration of 20 mg/L. Additionally, compounds 9 and 19 bearing two furan rings, respectively, at site 3 and site 5 of the pyrazoline cycle showed the strongest activities against R. solani (the EC50 were 3.46 mg/L and 3.20 mg/L). The bioactivity results provide good starting templates for further structural optimization of pyrazoline derivatives.

Co-reporter:Hong Zhang;Hong Jin;Lan-zhu Ji;Ke Tao;Wei Liu;Hao-yu Zhao;Tai-ping Hou
Chemical Biology & Drug Design 2011 Volume 78( Issue 1) pp:94-100
Publication Date(Web):
DOI:10.1111/j.1747-0285.2011.01082.x

Three natural products, 1,5-diphenylpentan-1-one, 1,5-diphenylpent-2-en-1-one, and 3-hydroxy-1,5-diphenylpentan-1-one, with good insecticidal activities were extracted from Stellera chamaejasme L. Based on their shared diaryl ketone moiety as ‘pharmacophores’, a series of diaryl ketones were synthesized and tested for insecticidal activity, acetylcholinesterase inhibitory activity, and antifungal activity. All synthesized compounds showed poor insecticidal and acetylcholinesterase inhibitory activities. Compound III with a furyl ring showed strong activities against plant pathogenic fungi. The IC50 of compound (E)-1-(2,4-dichlorophenyl)-3-(furan-2-yl)- -prop-2-en-1-one (III2) was 1.20 mg/L against Rhizoctonia solani, suggesting its strong potential as a novel antifungal drug.

Co-reporter:Zhiyi Yu, Guanying Shi, Qiu Sun, Hong Jin, Yun Teng, Ke Tao, Guoping Zhou, Wei Liu, Fang Wen, Taiping Hou
European Journal of Medicinal Chemistry 2009 Volume 44(Issue 11) pp:4726-4733
Publication Date(Web):November 2009
DOI:10.1016/j.ejmech.2009.05.028
A series of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid (norfloxacin) derivatives were prepared according to the principle of combinating bioactive substructures and tested for their activities against five plant pathogenic bacteria and three fungi in vitro. The preliminary bioassays indicated that almost all synthesized target compounds retained the antibacterial activities of norfloxacin and had some antifungal activities as carboxylic acid amide compounds. The activities of compounds 1 and 22 against Xanthomonas oryzae were better than norfloxacin and all tested compounds had better antibacterial activities as compared to the agricultural streptomycin sulfate (a commercial bactericide) against X. oryzae, Xanthomonas axonopodis and Erwinia aroideae. Additionally, compounds 2 and 20 displayed good antifungal activities against Rhizoctonia solani and their inhibition of growth reached 83% and 94% respectively at the concentration of 200 mg/L.A series of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid (norfloxacin) derivatives were designed and synthesized according to the principle of combinating bioactive substructures, and their activities against five bacteria and three fungi were evaluated successively.
Co-reporter:Fang Wen, Hong Zhang, Zhiyi Yu, Hong Jin, Qian Yang, Taiping Hou
Pesticide Biochemistry and Physiology (October 2010) Volume 98(Issue 2) pp:248-253
Publication Date(Web):1 October 2010
DOI:10.1016/j.pestbp.2010.06.015
A series of nicotinamide derivatives based on Boscalid were prepared and tested for their activities against seven plant pathogenic fungi and two insects. The preliminary bioassays indicated that almost all of the synthesized target compounds displayed the antifungal activities and some of them also had certain insecticidal activities. And, compound 12 showed the strongest activity of all against Rhizoctonia solani (EC50 = 0.010 mg L−1) and Sphaceloma ampelimum (EC50 = 0.040 mg L−1), even stronger than Boscalid, a new nicotinamide fungicide. Additionally, both compounds 1 and 2 showed strong activities against Plutella xylostella (90% and 80%, respectively, at 1000 mg L−1).
3-Furancarboxamide, N-[2-[(4-methoxyphenyl)amino]phenyl]-2-methyl-
2,4-Difluoro-2'-Nitrodiphenylamine
2-(4-Methoxyphenoxy)aniline
N1-(4-bromophenyl)benzene-1,2-diamine
1,2-Benzenediamine, N1-(4-methylphenyl)-
Benzenamine, 2,4-dichloro-N-(2-nitrophenyl)-
BENZENAMINE, N-(3-CHLOROPHENYL)-2-NITRO-
3-Furancarboxylic acid, 2,4,5-trimethyl-, ethyl ester
2-(m-Tolyloxy)aniline