- New potential antimalarial agents: Design, synthesis and biological evaluation of some novel quinoline derivatives as antimalarial agents
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A novel series of dihydropyrimidines (DHPMs) 4a-j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC50 values ranging from 0.014-5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).
- Radini, Ibrahim Ali M.,Elsheikh, Tarek M. Y.,El-Telbani, Emad M.,Khidre, Rizk E.
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- Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H-1,2,4-triazol-3-one, by Fragment-Based Drug Design
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This publication details the successful use of FBDD (fragment-based drug discovery) principles in the invention of a novel covalent Bruton's tyrosine kinase inhibitor, which ultimately became the Takeda Pharmaceuticals clinical candidate TAK-020. Describe
- Sabat, Mark,Dougan, Douglas R.,Knight, Beverly,Lawson, J. David,Scorah, Nicholas,Smith, Christopher R.,Taylor, Ewan R.,Vu, Phong,Wyrick, Corey,Wang, Haixia,Balakrishna, Deepika,Hixon, Mark,Madakamutil, Loui,McConn, Donavon
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p. 12893 - 12902
(2021/09/13)
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- 2-Anilino-3-Aroylquinolines as Potent Tubulin Polymerization Inhibitors
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Several 2-anilino-3-aroylquinolines were designed, synthesized, and screened for their cytotoxic activity against five human cancer cell lines: HeLa, DU-145, A549, MDA-MB-231, and MCF-7. Their IC50values ranged from 0.77 to 23.6 μm. Among the s
- Srikanth,Nayak, V. Lakshma,Suresh Babu, Korrapati,Kumar, G. Bharath,Ravikumar,Kamal, Ahmed
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p. 2050 - 2062
(2016/10/22)
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- GLYCINE B ANTAGONISTS
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The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.
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Page/Page column 48
(2010/04/27)
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- Vilsmeier-Haack reagent: A facile synthesis of 2-chloro-3-formylquinolines from N-arylacetamides and transformation into different functionalities
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A simple and regioselective synthesis of 2-chloro-3-formylquinolines through Vilsmeier-Haack cyclisation of N-arylacetamides has been reported. The cyclisation is facilitated by N-arylacetamides bearing electron donating groups at m-position. However, yields of quinolines having electron donating groups are good in all cases. Further, the nucleophilic substitution reaction of the quinolines is also investigated. Similarly, the formyl group in the quinolines is subjected to further transformation into cyano (CAN-NH3) and alkoxycarbonyl (NIS-K2CO3/alcohols) groups to afford corresponding 3-cyano and 3-alkoxycarbonylquinolines, respectively.
- Srivastava, Ambika,Singh
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p. 1868 - 1875
(2007/10/03)
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- Novel Extension of Meyers' Methodology: Stereoselective Construction of Axially Chiral 7,5-Fused Bicyclic Lactams
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A novel extension of Meyer's lactamization is reported for the preparation of seven-membered ring lactams 1a-d incorporating a biaryl unit. The required keto-esters 2a-c were readily accessible via the Suzuki coupling reaction. A borylation-Suzuki couplin
- Penhoat, Mael,Levacher, Vincent,Dupas, Georges
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p. 9517 - 9520
(2007/10/03)
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