- HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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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.
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- HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be 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.
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- N1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
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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.
- Luo, Wei,Liu, Yang,Wang, Jian,Guo, Chun,Lu, Wei-Qiang,Cui, Kun-Qiang
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p. 3073 - 3079,7
(2020/08/20)
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- 4,5-bis(dimethylamino)quinolines: Proton sponge versus azine behavior
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Two first representatives, 5 and 6, of the still unknown 4,5-bis(dimethylamino)quinoline have been synthesized and studied. While the former, being protonated either at the peri-NMe2 groups or at the ring nitrogen, has been shown to display pro
- Dyablo, Olga V.,Shmoilova, Elena A.,Pozharskii, Alexander F.,Ozeryanskii, Valery A.,Burov, Oleg N.,Starikova, Zoya A.
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p. 4134 - 4137
(2012/09/22)
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- Synthesis, antimicrobial activities and cytogenetic studies of newer diazepino quinoline derivatives via Vilsmeier-Haack reaction
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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.
- Nandhakumar,Suresh,Jude, A.L. Calistus,Rajesh kannan,Mohan
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p. 1128 - 1136
(2008/03/12)
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- A novel approach to 12-chloro-3-thio-4H-quino[3,2-e][1,3]diazocines via Vilsmeier Haack reaction
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The Vilsmeier Haack reaction on 4-hydroxyquinaldines lead to potential intermediate 4-chloro-3-formyl-2-(2-hydroxyethene-1-yl)quinolines. The intermediate is further utilized to prepare quino[3,2-e][1,3]diazocines on treatment with thiourea. The structures of the new compounds are determined by the analytical and spectroscopic data.
- Kumar, R. Nandha,Suresh,Dhanabal,Mohan
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p. 995 - 1000
(2008/09/18)
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- Synthesis of 6-methylbenzo-[b]pyrido[3,2-f][1,6]naphthyridines from 4-chloro-2-methylquinoline
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4-Chloro-2-methylquinolines in reaction with 3-aminopyridine yielded 4-quinolinamines, which upon cyclisation under Vilsmeier-Haak conditions afforded the title compounds. 2005 Springer Science+Business Media, Inc.
- Suresh,Nandha Kumar,Mohan
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p. 778 - 781
(2007/10/03)
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- Synthesis of 12-ethoxy-3-oxo-4-phenylquino[3,2-c][1,3]diazocines via Vilsmeier-Haack reaction
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Application of Vilsmeier condition on 4-hydroxyquinaldines give potentially useful intermediates 4-chloro-3-formyl-2-(2-hydroxyethene-1-yl)quinolines, which are utilized to prepare quino[3,2-c][1,3]diazocines on treatment with N-phenylurea.
- Kumar, Nandha,Suresh,Dhanabal,Mohan
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p. 598 - 601
(2007/10/03)
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- Utility of Vilsmeier Haack reagent in the synthesis of 3-amino-12-chloroquino[3,2-e][1,3]diazocines
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Application of Vilsmeier condition on 4-hydroxyquinaldines gives a potential intermediate 4-chloro-3-formyl-2-(2-hydroxy-ethene-1-yl)quinolines which is utilized to prepare quino[3,2-e][1,3]diazocines on treatment with guanidine nitrate. All the synthesized compounds are characterized by the analytical and spectroscopic data.
- Kumar, R. Nandha,Suresh,Dhanabal,Mohan
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p. 846 - 851
(2007/10/03)
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- Vilsmeier-Haack reaction on quinaldines
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The study of the Vilsmeier-Haack reaction on 4-hydroxyquinaldines resulted with the preparation of rarely existing 4-chloro-3-formyl-2(vinyl-1-ol)-quinolines.
- Nandha Kumar,Suresh,Mohan
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p. 2069 - 2073
(2007/10/03)
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- Quinoline derivatives as antitubercular/antibacterial agents
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A number of quinoline derivatives of known antibacterial agents have been prepared and tested against the micro-organisms S. coli, S. paratyphi B, S. aureus and in particular against Mycobacterium tuberculosis H37-Rv. It has not been possibfe to establish correlation between antibacterial and antitubercular activities of these compounds. However, the antitubercular effect at MIC of 5 μg/mL against H37Rv shows that many modified compounds are more inhibitory than the parent agents such as 3-aminophenol, sulphamethoxazole, sulphaphenazole, sulphathiazole and monoacetyldapsone; among these the most effective are those with substituents such as 6-methyl, 6-chloro, 6-ethoxy-, or 8-methoxy functions in quinoline moiety.
- Desai,Desai, Pratibha,Machhi, Dilip,Desai,Patel, Dinesh
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p. 871 - 873
(2007/10/03)
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