- Design, Synthesis, and Antifungal Evaluation of Novel Quinoline Derivatives Inspired from Natural Quinine Alkaloids
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Inspired by quinine and its analogues, we designed, synthesized, and evaluated two series of quinoline small molecular compounds (a and 2a) and six series of quinoline derivatives (3a-f) for their antifungal activities. The results showed that compounds 3e and 3f series exhibited significant fungicidal activities. Significantly, compounds 3f-4 (EC50 = 0.41 μg/mL) and 3f-28 (EC50 = 0.55 μg/mL) displayed the superior in vitro fungicidal activity and the potent in vivo curative effect against Sclerotinia sclerotiorum. Preliminary mechanism studies showed that compounds 3f-4 and 3f-28 could cause changes in the cell membrane permeability, accumulation of reactive oxygen species, loss of mitochondrial membrane potential, and effective inhibition of germination and formation of S. sclerotiorum sclerotia. These results indicate that compounds 3f-4 and 3f-28 are novel potential fungicidal candidates against S. sclerotiorum derived from natural products.
- Yang, Guan-Zhou,Zhu, Jia-Kai,Yin, Xiao-Dan,Yan, Yin-Fang,Wang, Yu-Ling,Shang, Xiao-Fei,Liu, Ying-Qian,Zhao, Zhong-Min,Peng, Jing-Wen,Liu, Hua
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p. 11340 - 11353
(2019/10/14)
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- Synthesis and cytotoxicity of new quinoline derivatives
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New 2,8-bis(trifluoromethyl)-4-substituted quinolines have been synthesized from 4-haloquinoline following the Suzuki protocol and N-arylation. The cytotoxicity of the synthesized compounds has been evaluated against human cancer cell lines, and among them, compounds 5a and 5g are found to be the more potent antiproliferative agents.
- Meshram, H. M.,Chennakesava Reddy, B.,Aravind Kumar, D.,Kalyan, M.,Ramesh, P.,Kavitha, P.,Venkateswara Rao, J.
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p. 1411 - 1416,6
(2020/08/31)
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- PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.
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Page/Page column 75
(2010/04/25)
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- PYRAZOLONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyrazolone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1,R2: C1-6 alkyl; R3,R4: H, X, C1-6 alkoxy; Z:O, S; A:AA, BB, wherein AA represents wherein BB represents wherein R5: H, C1-6 alkyl ; R6,R7: C1-6 alkyl.
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Page/Page column 59
(2010/04/25)
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- THIAZOLIDINE DERIVATIVE AND MEDICINAL USE THEREOF
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A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.
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- 8-Methoxyquinolines as PDE4 inhibitors.
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The synthesis and pharmacological profile of a novel series of 2-substituted 8-methoxyquinolines is described. The 2-trifluoromethyl compound was found to be a potent inhibitor of phosphodiesterase type 4 (PDE4).
- Billah, Motasim,Buckley, George M,Cooper, Nicola,Dyke, Hazel J,Egan, Robert,Ganguly, Ashit,Gowers, Lewis,Haughan, Alan F,Kendall, Hannah J,Lowe, Christopher,Minnicozzi, Michael,Montana, John G,Oxford, Janet,Peake, Joanna C,Picken, C Louise,Piwinski, John J,Naylor, Robert,Sabin, Verity,Shih, Neng-Yang,Warneck, Julie B H
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p. 1617 - 1619
(2007/10/03)
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- 8-hydroxy-7-substituted quinolines as anti-viral agents
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The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula III These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
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