- Synthesis and Luminescent Properties of Eu3+, Gd3+, and Tb3+ Complexes with Quinoline-4-carboxylic Acids
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New complex compounds LnL3·nH2O (n = 5–10) have been synthesized on the basis of Eu3+, Gd3+, and Tb3+ salts and quinoline-4-carboxylic acid derivatives obtained via the Pfitzinger reaction. Compositio
- Aksenov, N. A.,Aksenova, I. V.,Dotsenko, V. V.,Kolokolov, F. A.,Kotlova, I. A.
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- A diboronic acid fluorescent sensor for selective recognition of d-ribose via fluorescence quenching
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Boronic acids have been widely developed as fluorescent sensors for recognition of carbohydrates, especially d-glucose, ions, catechol compounds and so on. However, few d-ribose selective boronic acid sensors have been reported, and their poor water solub
- Wang, Hao,Fang, Guiqian,Wang, Hongxiao,Dou, Jindi,Bian, Zhancun,Li, Ying,Chai, Huining,Wu, Zhongyu,Yao, Qingqiang
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- A highly selective and sensitive boronic acid-based sensor for detecting Pd2+ ion under mild conditions
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Herein, a boronic acid-based sensor was reported selectively to recognize Pd2+ ion. The fluorescence intensity increased 36-fold after sensor binding with 2.47 × 10?5 M of Pd2+ ion. It was carried out in the 99% aqueous so
- Bian, Zhancun,Fang, Guiqian,Wang, Ran,Wu, Zhongyu,Yao, Qingqiang,Zhan, Dongxue,Zhang, Guimin
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- New quinoline-based heterocycles as anticancer agents targeting Bcl-2
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The Bcl-2 protein has been studied as an anticancer drug target in recent years, due to its gatekeeper role in resisting programmed cancer cell death (apoptosis), and the design of BH3 domain mimetics has led to the clinical approval of Venetoclax (ABT-19
- Hamdy, Rania,Elseginy, Samia A.,Ziedan, Noha I.,Jones, Arwyn T.,Westwell, Andrew D.
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- Synthesis of Novel Quinoline–Benzoxazolinone Ester Hybrids: In Vitro Anti-Inflammatory Activity and Antibacterial Activity
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Abstract: A series of novel quinoline-benzoxazolinone ester hybrids were synthesized characterized and assessed for their in vitro anti-inflammatory and antibacterial activity. The in vitro anti-inflammatory activity was executed using protein denaturation assay, proteinase inhibitory assay and human red blood cell membrane stabilization assay. Most of the compounds exhibited potential anti-inflammatory activity. Compound (2-oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(thiophen-2-yl)quinoline-4-carboxylate showed a better anti-inflammatory activity than the standard drugs diclofenac sodium and indomethacin. Furthermore, antibacterial activities of the synthesized compounds were evaluated using resazurin microtiter assay (REMA) and were compared with a positive drug standard chloramphenicol. The compounds demonstrated moderate to potent antibacterial activity. (2-Oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(3,4-dimethoxyphenyl)quinoline-4-carboxylate and (2-oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(2-chlorophenyl)quinoline-4-carboxylate displayed excellent activity against all bacterial strains in comparison to standard chloramphenicol. Moreover, cytotoxicity was performed on MDCK cells using MTT assay and it was found that none of the synthesized derivatives possessed any cytotoxicity.
- Shaikh, Sarfaraz F.,Dhavan, Pratik P.,Singh, Pinky R.,Vaidya,Jadhav,Ramana
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p. 572 - 583
(2021/05/03)
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- Synthesis, characterization, and antileishmanial activity of certain quinoline-4-carboxylic acids
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Leishmaniasis is a fatal neglected parasitic disease caused by protozoa of the genus Leishmania and transmitted to humans by different species of phlebotomine sandflies. The disease incidence continues to increase due to lack of vaccines and prophylactic drugs. Drugs commonly used for the treatment are frequently toxic and highly expensive. The problem of these drugs is further complicated by the development of resistance. Thus, there is an urgent need to develop new antileishmanial drug candidates. The aim of this study was to synthesize certain quinoline-4-carboxylic acids, confirm their chemical structures, and evaluate their antileishmanial activity. Pfitzinger reaction was employed to synthesize fifteen quinoline-4-carboxylic acids (Q1-Q15) by reacting equimolar mixtures of isatin derivatives and appropriate α-methyl ketone. The products were purified, and their respective chemical structures were deduced using various spectral tools (IR, MS, 1H NMR, and 13C NMR). Then, they were investigated against L. donovani promastigote (clinical isolate) in different concentration levels (200 μg/mL to 1.56 μg/mL) against sodium stibogluconate and amphotericin B as positive controls. The IC50 for each compound was determined and manipulated statistically. Among these compounds, Q1 (2-methylquinoline-4-carboxylic acid) was found to be the most active in terms of IC50.
- Abdelwahid, Mazin A. S.,Elsaman, Tilal,Mohamed, Malik S.,Latif, Sara A.,Mukhtar, Moawia M.,Mohamed, Magdi A.
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- COMPOUNDS FOR TREATMENT OF GLIOBLASTOMA
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The present invention relates to compounds and methods for the treatment of glioblastoma, as well as to a pharmaceutical composition comprising said compounds. More specifically the invention relates to substituted quinoline derivatives having the formula (I), (II) or (III), and a pharmaceutical composition comprising said compounds for the treatment of cancer. (Formulae (I), (II), (III))
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Paragraph 00258; 00330-00333; 00336-00337
(2018/09/08)
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- Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase
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We pursued a structure-guided approach toward the development of improved dihydroorotate dehydrogenase (DHODH) inhibitors with the goal of forming new interactions between DHODH and the brequinar class of inhibitors. Two potential residues, T63 and Y356, suitable for novel H-bonding interactions, were identified in the brequinar-binding pocket. Analogues were designed to maintain the essential pharmacophore and form new electrostatic interactions through strategically positioned H-bond accepting groups. This effort led to the discovery of potent quinoline-based analogues 41 (DHODH IC50 = 9.71 ± 1.4 nM) and 43 (DHODH IC50 = 26.2 ± 1.8 nM). A cocrystal structure between 43 and DHODH depicts a novel water mediated H-bond interaction with T63. Additional optimization led to the 1,7-naphthyridine 46 (DHODH IC50 = 28.3 ± 3.3 nM) that forms a novel H-bond with Y356. Importantly, compound 41 possesses significant oral bioavailability (F = 56%) and an elimination t1/2 = 2.78 h (PO dosing). In conclusion, the data supports further preclinical studies of our lead compounds toward selection of a candidate for early-stage clinical development.
- Madak, Joseph T.,Cuthbertson, Christine R.,Miyata, Yoshinari,Tamura, Shuzo,Petrunak, Elyse M.,Stuckey, Jeanne A.,Han, Yanyan,He, Miao,Sun, Duxin,Showalter, Hollis D.,Neamati, Nouri
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p. 5162 - 5186
(2018/05/15)
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- Energy efficient Pfitzinger reaction: A novel strategy using a surfactant catalyst
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A novel energy efficient method for the Pfitzinger reaction is demonstrated, which is catalysed using a surfactant, cetyltrimethylammonium hydroxide. The surfactant nature of the catalyst caused the substrate to be soluble in aqueous media, which enhanced the interaction of the catalyst with the substrate. An increase in the rate of reaction and more than 78% of energy saving were observed under ultrasonic irradiation.
- More, Priyanka A.,Shankarling, Ganapati S.
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supporting information
p. 12380 - 12383
(2017/11/06)
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- Hypoboric acid derivative based on 2-(4-dyhydroxy borane)pheoylquinoline-4-carboxylic acid and preparation method and application thereof
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The invention discloses a hypoboric acid derivative based on 2-(4-dyhydroxy borane)pheoylquinoline-4-carboxylic acid and a preparation method thereof. The hypoboric acid derivative is used for preparing catecholamine and carbohydrate fluorescent probes. T
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Paragraph 0024; 0025; 0026; 0027
(2017/07/19)
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- 2-(4-bromophenyl) quinoline-4-carboxylic acid compound and its preparation method and application
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The invention relates to a 2-(4-bromophenyl) quinoline-4-formic acid complex and a preparation method and application thereof. The structural formula of the complex is shown in the specification, wherein M is metal and can be Mn, Co, Cd or Zn. The 2-(4-br
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Paragraph 0032-0033
(2017/01/19)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 109-110
(2014/08/07)
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- Discovering novel chemical inhibitors of human cyclophilin A: Virtual screening, synthesis, and bioassay
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Cyclophilin A (CypA) is a member of cyclophilins, a family of the highly homologous peptidyl prolyl cis-trans isomerases (PPIases), which can bind to cyclosporin A (CsA). CypA plays critical roles in various biological processes, including protein folding, assembly, transportation, regulation of neuron growth, and HIV replication. The discovery of CypA inhibitor is now of a great special interest in the treatment of immunological disorders. In this study, a series of novel small molecular CypA inhibitors have been discovered by using structure-based virtual screening in conjunction with chemical synthesis and bioassay. The SPECS_1 database containing 85,000 small molecular compounds was searched by virtual screening against the crystal structure of human CypA. After SPR-based binding affinity assay, 15 compounds were found to show binding affinities to CypA at submicro-molar or micro-molar level (compounds 1-15). Seven compounds were selected as the starting point for the further structure modification in considering binding activity, synthesis difficulty, and structure similarity. We thus synthesized 40 new small molecular compounds (1-6, 15, 16a-q, 17a-d, and 18a-l), and four of which (compounds 16b, 16h, 16k, and 18g) showed high CypA PPIase inhibition activities with IC50s of 2.5-6.2 μM. Pharmacological assay indicated that these four compounds demonstrated somewhat inhibition activities against the proliferation of spleen cells.
- Li, Jian,Chen, Jing,Gui, Chunshan,Zhang, Li,Qin, Yu,Xu, Qiang,Zhang, Jian,Liu, Hong,Shen, Xu,Jiang, Hualiang
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p. 2209 - 2224
(2007/10/03)
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- A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase
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A series of quinoline inhibitors of C. albicans prolyl tRNA synthetase was identified. The most potent analogue, 2-(4bromo-phenyl)-6-chloro-8-methyl-4-quinolinecarboxylic acid, showed IC50=5 nM (Ca. ProRS) with high selectivity over the human enzyme.
- Yu, Xiang Y.,Hill, Jason M.,Yu, Guixue,Yang, Yifeng,Kluge, Arthur F.,Keith, Dennis,Finn, John,Gallant, Paul,Silverman, Jared,Lim, Audrey
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p. 541 - 544
(2007/10/03)
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- Synthesis and aldose reductase inhibitory activity of N-(quinolinyl thiocarbonyl) glycine derivatives
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The onset of diabetic complications may be prevented by the inhibition of aldose reductase.Derivatives of N-(quinolinyl thiocarbonyl) glycine were prepared and their in vitro and ex vivo aldose reductase inhibitory activities were tested on rat lens.The cincophen derivatives were the most potent in vitro with an enzyme inhibition value of 29percent at 10-8 M and 91percent at 10-7 for the N--N-methylglycine compound 10a.This activity was shown to be dependent on the nature of the substituents and seems to be optimal for the acids; esterswerefound to be inactive.No compound have shown ex vivo inhibitory activity.It is concluded that the lack of ex vivo activity is likely due to a poor bioavailability or a bad penetration of the compounds in target tissue (lens). aldose reductase inhibitors / diabetic complications / N-(quinolinyl thiocarbonyl) glycine
- Nicolaie, E,Guengoer, T,Goyard, J,Cure, G,Fouquet, A,et al.
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p. 977 - 984
(2007/10/02)
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- 4-Piperidino-2-phenylquinolines
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Disclosed are compounds of the formula STR1 wherein: R1 and R2 may be either the same or different and each is hydrogen or lower alkyl; and wherein R3 and R4 may be either the same or different and each is hydrogen, halogen, or lower alkyl, with the proviso that R3 and R4 cannot both be hydrogen. These compounds are useful as anticonvulsant or anxiolytic agents.
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