- Synthesis and nematicidal activity of piperazinedione derivatives based on the natural product Barettin
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Nematodes are serious constraints of crop production worldwide. However, the traditional nematicides suffer from the side-effects, including environmental and human toxicity. Herein, more than 70 novel piperazinedione derivatives based on the natural product Barettin were synthesized and evaluated against the root-knot nematode Meloidogyne incognita (M. incognita). While most of synthesized compounds exhibited certain nematicidal activity at high concentration, the best one showed a nematicidal activity of 75% at 2.4 μmol/L.
- Sun, Haiyang,Li, Hui,Wang, Jiayi,Song, Gonghua
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p. 977 - 980
(2017/11/16)
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- Pyrazolopyrimidines: Potent Inhibitors Targeting the Capsid of Rhino- and Enteroviruses
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There are currently no drugs available for the treatment of enterovirus (EV)-induced acute and chronic diseases such as the common cold, meningitis, encephalitis, pneumonia, and myocarditis with or without consecutive dilated cardiomyopathy. Here, we report the discovery and characterization of pyrazolopyrimidines, a well-tolerated and potent class of novel EV inhibitors. The compounds inhibit the replication of a broad spectrum of EV in vitro with IC50 values between 0.04 and 0.64 μM for viruses resistant to pleconaril, a known capsid-binding inhibitor, without affecting cytochrome P450 enzyme activity. Using virological and genetics methods, the viral capsid was identified as the target of the most promising, orally bioavailable compound 3-(4-trifluoromethylphenyl)amino-6-phenylpyrazolo[3,4-d]pyrimidine-4-amine (OBR-5-340). Its prophylactic as well as therapeutic application was proved for coxsackievirus B3-induced chronic myocarditis in mice. The favorable pharmacokinetic, toxicological, and pharmacodynamics profile in mice renders OBR-5-340 a highly promising drug candidate, and the regulatory nonclinical program is ongoing. Curing the common cold! A cluster of pyrazolopyrimidines with potent broad-spectrum activity against enteroviruses was discovered. Extensive structure-property relationship analyses led to the identification of 3-(4-trifluoromethyl-phenyl)amino-6-phenylpyrazolo[3,4-d]pyrimidine-4-amine, shown to be a blocker of the viral capsid protein, as a lead compound for drug development with favorable physicochemical, pharmacokinetic, and toxicological properties.
- Makarov, Vadim A.,Braun, Heike,Richter, Martina,Riabova, Olga B.,Kirchmair, Johannes,Kazakova, Elena S.,Seidel, Nora,Wutzler, Peter,Schmidtke, Michaela
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supporting information
p. 1629 - 1634
(2015/10/06)
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- Synthesis and herbicidal activities of fluorine-containing 3-pyridylmethyl-2-phenyliminothiazolidine derivatives
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A series of fluorine-containing 2-phenyliminothiazolidine derivatives were synthesized by a facile and mild method in high yields. The structures of all the title compounds were characterized by 1H NMR, IR and HRMS. The results of bioassay showed that most of target compounds exhibited efficient herbicidal activities against Echinochloa crusgalli, Sorghum vulgare, Digitaria sanguinalis, Eclipta prostrasta, Cucumis sativus and Brassica campestris at 50 mg L-1.
- Li, Gangyue,Qian, Xuhong,Cui, Jingnan,Huang, Qingchun,Cui, Dawei,Zhang, Rong,Liu, Fengyu
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p. 182 - 186
(2007/10/03)
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- Thiazole-4-carboxyamide derivatives
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The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
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Page/Page column 29
(2008/06/13)
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- Antihypertensive (2-Aminoethyl)thiourea Derivatives. 1
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Structure-activity studies were carried out on a series of antihypertensive 1-(2-aminoethyl)-3-(substituted phenyl)thioureas.From this class of compounds, the 2,6-dichlorophenyl analogue 2 was found to have potent oral antihypertensive activity in two hypertensive rat models and the renal hypertensive dog.In addition to its effect on blood pressure, 2 displayed sedative effects which had a marked species specificity.
- Tilley. Jefferson W.,Levitan, Paul,Kierstead, Richard W.,Cohen, Michael
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p. 1387 - 1392
(2007/10/02)
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- Thiourea derivatives
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Antihypertensively active thiourea derivatives of the formulas STR1 wherein R, R1, R2, R3 and X are as hereinafter described, as well as a method of using a compound of the formula STR2 wherein R1 ', R2 ', R3 and X are as previously described, or a compound of formula II as an anti-hypertensive agent, is described.
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