生物活性 | |||
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描述 | 4-Quinolinecarboxylic acid was identified as Microbacterium sp. Mutants were induced with N-methyl-N'-nitro-N-nitrosoguanidine[1]. The highest antimicrobial effects were found with substituted quinoline-4-carboxylic acid derivatives. Quinoline-4-carboxamides only weakly influenced the growth of the tested microorganisms. Some derivatives of quinoline-4-carboxylic acid elicited profound changes in the morphology of hyphal tips of Botrytis cinerea, mainly their branching and the release of the cytoplasmic content. Quinoline derivatives, which elicited morphological changes, increased also the permeability of the plasmalemma of plant cells[2]. A very potent lead compound 6-fluoro-2- (5-isopropyl-2-methyl-4-phenoxyphenyl) quinoline-4-carboxylic acid (C44) that inhibits human dihydroorotate dehydrogenase (DHODH) with an IC50 of 1 nM, and viral replication of VSV and WSN-Influenza with an EC50 of 2 nM and 41 nM[3]. 6-bromo-2-[1-(2,5-dimethylphenyl)-5-methyl-1H-pyrazol-4-yl] quinoline-4-carboxylic acid (BPR-3P0128) exhibits excellent antiviral activity against EV71 (EC50 = 0.0029 μM). BPR-3P0128 inhibits viral replication during the early post infection stage, targets EV71 RNA-dependent RNA polymerase and VPg uridylylation, and also reduces viral RNA accumulation levels and inhibits viral replication of EV71[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.77mL 1.15mL 0.58mL |
28.87mL 5.77mL 2.89mL |
57.75mL 11.55mL 5.77mL |
参考文献 |
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