- Design, synthesis, insecticidal, and acaricidal activities of novel pyrimidinamine derivatives containing a biphenyl ether
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A series of original pyrimidinamine derivatives containing a biphenyl ether moiety were designed and synthesized. Their structures were confirmed by 1H NMR, MS, and elemental analyses. Their insecticidal activities against lepidopteran and hemiptera insects and acaricidal activities were tested. The results of bioassay demonstrated that 9k showed the best activity (LC50 = 2.08 mg/L) against Tetranychus urticae, which is comparable with the positive control, spirotetramat (LC50 = 2.27 mg/L), and 9g showed better activity (LC50 = 0.52 mg/L) against Aphis fabae than the positive control, imidacloprid (LC50 = 1.02 mg/L), and relatively good activity (LC50 = 2.49 mg/L) against T urticae. Their structure-activity relationships indicated that both an ethyl group on the 4-position of the pyrimidine ring and alkyl chain as a para-substituent group of the benzene ring showed good biological activity.
- Li, Lizhong,Zhou, Chunge,Liu, Minhua,Zhang, Ping,Zhang, Ning,Li, Jianming,Li, Tao,Liu, Xingping,Cheng, Shufen,Li, Qianhe,Liu, Aiping
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p. 3206 - 3214
(2019/11/13)
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- Optimization of N-benzyl-5-nitrofuran-2-carboxamide as an antitubercular agent
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The optimization campaign for a nitrofuran antitubercular hit (N-benzyl-5-nitrofuran-2-carboxamide; JSF-3449) led to the design, synthesis, and biological profiling of a family of analogs. These compounds exhibited potent in vitro antitubercular activity (MIC = 0.019–0.20 μM) against the Mycobacterium tuberculosis H37Rv strain and low in vitro cytotoxicity (CC50 = 40–>120 μM) towards Vero cells. Significant improvements in mouse liver microsomal stability and mouse pharmacokinetic profile were realized by introduction of an α α-dimethylbenzyl moiety. Among these compounds, JSF-4088 is highlighted due to its in vitro antitubercular potency (MIC = 0.019 μM) and Vero cell cytotoxicity (CC50 > 120 μM). The findings suggest a rationale for the continued evolution of this promising series of antitubercular small molecules.
- Gallardo-Macias, Ricardo,Kumar, Pradeep,Jaskowski, Mark,Richmann, Todd,Shrestha, Riju,Russo, Riccardo,Singleton, Eric,Zimmerman, Matthew D.,Ho, Hsin Pin,Dartois, Véronique,Connell, Nancy,Alland, David,Freundlich, Joel S.
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supporting information
p. 601 - 606
(2019/01/04)
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- 5,5-HETEROAROMATIC ANTI-INFECTIVE COMPOUNDS
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The invention provides a series of 5,5-heteroaromatic compounds, syntheses thereof, compositions thereof, and methods of using such compounds and compositions. Various embodiments provide methods of killing and/or inhibiting the growth of M. tuberculosis
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- 5,5-HETEROAROMATIC ANTI-INFECTIVE COMPOUNDS
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The invention provides a series of 5,5-heteroaromatic compounds, syntheses thereof, compositions thereof, and methods of using such compounds and compositions. Various embodiments provide methods of killing and/or inhibiting the growth of M. tuberculosis
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Paragraph 0183
(2015/08/04)
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