- 2 -trifluoromethyl -4 - amino - quinoline derivative and application thereof
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The invention discloses 2 -trifluoromethyl -4 - amino - quinoline derivatives and application thereof, and comprises a compound represented by the following general formula I. The prepared compound is used for preparing an anti-tumor active drug, has a go
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Paragraph 0032-0036; 0120-0124
(2021/11/10)
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- Nucleoside analogs useful as PRMT5 inhibitors
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The invention relates to the technical field of biological medicines, and particularly discloses a nucleoside analogue used as a PRMT5 inhibitor. According to the nucleoside analogue as shown in the formula (I) or the pharmaceutically acceptable salt of the nucleoside analogue, the nucleoside analogue or the pharmaceutically acceptable salt of the nucleoside analogue shows relatively high inhibition on the activity of PRMT5 and can be used for preventing and/or treating PRMT5-mediated diseases, and the PRMT5-mediated diseases comprise cell abnormal proliferative diseases.
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Paragraph 0219; 0221; 0222; 0223; 0224
(2021/08/11)
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- Antibacterial activity of new substituted 4-N-alkylated-2-trifluoromethyl-quinoline analogues against sensitive and resistant Mycobacterium tuberculosis strains
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Objectives: The emergence of resistant strain has aggravated the tuberculosis situation in the world, running out of control and hard to fight. We evaluate forty new quinoline analogues against sensitive and resistant Mycobacterium tuberculosis (Mtb). Methods: The compounds were obtained via synthesis and evaluated against sensitive strain ATCC 27294. Selected compounds were evaluated against resistant strains SR 2571/0215 and T113/09, using the MABA method. The more active compounds were selected for their potential cytotoxic activity against human macrophage cells. Results: Twenty-nine compounds displayed activity against sensitive strain, and thirteen were active against resistant strains. Against sensitive strain, the most promising compounds were 4c and 4d (MIC = 9 and 12 μM, respectively). Against resistant strains, the compounds 4a, 4d displayed the best results (MIC = 4 and 5 μM, respectively). The active compounds 4a, 4d, 6d, 7c, 8d, and 10d were non-cytotoxic to the host cells at concentrations near to the MIC. The non-cytotoxic compound 4d was the most potent against resistant and sensitive Mtb. Conclusion: These findings contribute to relevant information and perspectives in search of new bioactive compounds against sensitive and resistant TB. Resistant strains have turned tuberculosis a severe disease in the world.
- da Silva, Emerson Teixeira,de Andrade, Gabriel Fernandes,Araújo, Adriele da Silva,Louren?o, Maria Cristina Silva,de Souza, Marcus Vinícius Nora
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- Preparation of quinoline 4-position hydroxyethyl ester compound and application thereof in controlling plant diseases
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The invention discloses application of a compound of quinoline 4-position hydroxyethyl ester compound Ba-Bp in controlling or resisting agricultural plant fungal diseases. An antibacterial activity test results show that the compound exhibits high inhibitory activity against four fungal diseases of sclerotinia sclerotiorum, rhizoctonia solani, fusarium graminearum and magnaporthe oryzae, the inhibitory activity of some compounds to pathogens is superior to that of azoxystrobin, and the compound can be developed as a fungicide.
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Paragraph 0015; 0018-0019
(2019/11/20)
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- 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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- Investigations into the flexibility of the 3D structure and rigid backbone of quinoline by fluorine addition to enhance its blue emission
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Achieving the desired structures of organic molecules for targeted applications is vital. Folding caused by weak intermolecular forces plays an important part in their 3D structure. Powerful tools which enable us to do this are currently under investigation by researchers across the globe. On this account, quinoline was chosen as a model scaffold because of its rigid 3D structure. Addition of fluorine was found to result in increased flexibility of the structure with a decrease in the number of intermolecular interactions. This resulted in improvement of their photophysics and blue emission. A total of 19 novel fluoroquinoline molecules were synthesised in order to carry out this study. Of these, grown crystals of 10 compounds were successfully achieved and used. In addition, characterisation techniques such as NMR, HRMS, UV-vis and computational techniques were used to explore the 3D structure of these molecules.
- Alapour,Zamisa,Silva,Alves,Omondi,Ramjugernath,Koorbanally
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p. 2316 - 2323
(2018/04/30)
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- ANTIBIOTIC COMPOSITIONS
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The present disclosure relates to compounds having antimicrobial activity, compositions comprising said compounds in combination with β-lactam antibiotics, and methods of using the compounds and compositions.
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Page/Page column 0139; 0141
(2017/09/02)
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- Pesticides
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Compound of the formula (I) are disclosed or a salt thereof, wherein Ar is an optionally substituted polycyclic ring system containing n rings, where n is the integer 2 or 3, at least n-1 rings being aromatic and containing one to three ring nitrogen atoms and optionally containing one or more additional heteroatoms; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing a sulphur or one or two oxygen atoms; Q1 is a group (C(R2)=C(R3))a --(C(R4)=C(R5)) wherein a is 0 or 1, R2, R3, R4 and R5 are the same or different, at least two being hydrogen and the other two being independently selected from hydrogen, halo, C1-4 haloalkyl; X is oxygen or sulphur; and R1 is selected from hydrogen and C1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C1-6 alkoxy are described which have activity particularly against arthropod pests. Pesticidal formulations containing the compounds of the formula (1), their use in the control of pests and method for their preparation are also disclosed.
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