32314-39-9Relevant articles and documents
HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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, (2016/03/19)
The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
N1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
Luo, Wei,Liu, Yang,Wang, Jian,Guo, Chun,Lu, Wei-Qiang,Cui, Kun-Qiang
, p. 3073 - 3079,7 (2020/08/20)
A series of N1-{4-[(10S)-dihydroartemisinin- 10-oxyl]}phenylmethylene-N2-(2-methylquinoline-4-yl) hydrazine derivatives 9a-9n possessing 4-quinolylhydrazone and artemisinin cores were herein synthesized and evaluated for their activities against cysteine protease falcipain- 2 of Plasmodium falciparum. The structures were clearly confirmed by elemental analysis, 1H NMR, and mass spectra. The pharmacological results indicated that all compounds showed excellent activity against recombinant falcipain-2 (IC50 = 0.15-2.28 μM). The best one of this series was compound 9d (IC50 = 0.15 μM). The molecular docking results showed that the compound 9d made close contact with the key active site of cysteine protease falcipain-2.
Synthesis, antimicrobial activities and cytogenetic studies of newer diazepino quinoline derivatives via Vilsmeier-Haack reaction
Nandhakumar,Suresh,Jude, A.L. Calistus,Rajesh kannan,Mohan
, p. 1128 - 1136 (2008/03/12)
The study of the Vilsmeier-Haack reagent on 4-hydroxyquinaldines resulted in a new versatile intermediate 4-chloro-3-formyl-2-(2-hydroxy-ethene-1-yl)quinolines, which on further treatment with hydrazine hydrate yielded the desired diazepino quinoline derivatives. All the synthesized diazepino quinoline derivatives are screened for their antibacterial and antifungal activities. Cytogenetic analysis of the samples is also reported.