Results 141 to 150 of about 4,514 (173)

Pharmacologic actions of 4-aminoquinoline compounds

The American Journal of Medicine, 1983
The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye.
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Synthesis of 4‐aminoquinoline‐1,2,3‐triazole and 4‐aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine Hybrids as Potential Antimalarial Agents

Chemical Biology & Drug Design, 2011
We report herein synthesis of a series of 4‐aminoquinoline‐1,2,3‐triazole and 4‐aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine hybrids and evaluate their antimalarial activity against D6 and W2 strains of Plasmodium falciparum. To study the structure–activity relationship of substituted 4‐aminoquinoline–based hybrids, 34 structurally diverse compounds ...
Sunny, Manohar, Shabana I, Khan, Diwan S, Rawat   +2 more
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4-Aminoquinolines as AChE Inhibitors

1998
A systematic analysis of the tacrine-TcAChE complex X-ray structure2 has been carried out, in conjunction with other available crystallographic data, with the aim of identifying possible areas for selective inhibitor design.
P. D. Bentley, F. Earley, R. J. Fletcher, A. Kinkaid, T. Lewis, B. Pirard, J. Taylor, R. C. Viner   +7 more
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4-Aminoquinolines:  Novel Nociceptin Antagonists with Analgesic Activity

Journal of Medicinal Chemistry, 2000
Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL(1) receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated.
H, Shinkai, T, Ito, T, Iida, Y, Kitao, H, Yamada, I, Uchida   +5 more
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4-Aminoquinolines and Mannich Bases

1984
The antimalarial 4-aminoquinolines and Mannich bases have been compiled and/or discussed in a number of compendia and reviews. These reviews have, for the most part, considered only those drugs or compounds that have shown an activity sufficient to focus broad attention upon them.
T. R. Sweeney, R. O. Pick
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Antimalarial 4‐aminoquinolines: mode of action and pharmacokinetics

Fundamental & Clinical Pharmacology, 1994
Summary— In the last ten years, the widespread increase in Plasmodium falciparum resistance to chloroquine has prompted research into antimalarial 4‐aminoquinolines, empirically used up to now. The mechanism of action of 4‐aminoquinolines is characterized by the concentration of the drug in the digestive vacuole of the intraerythrocytic parasite ...
E, Pussard, F, Verdier
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7-(Trifluoromethyl)-4-aminoquinoline hypotensives: novel peripheral sympatholytics

Journal of Medicinal Chemistry, 1986
A family of 7-(trifluoromethyl)-4-aminoquinolines that are hypotensive agents and that act by a novel sympatholytic mechanism is described. Structure-activity relationships in this series have been elucidated. Some of the more potent hypotensives were evaluated for safety in the mouse. A candidate, 1-[(4-fluorophenyl)sulfonyl]-4-[4-[[7-(trifluoromethyl)
J M, McCall, R E, TenBrink, B V, Kamdar, L L, Skaletzky, S C, Perricone, R C, Piper, P J, Delehanty   +6 more
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Giant miniature endplate potentials induced by 4‐aminoquinoline

Acta Physiologica Scandinavica, 1982
In experiments on the isolated extensor digitorum longus muscle of the rat it was shown that 4‐aminoquinoline (125–250 μM) altered the amplitude distribution of spontaneous miniature endplate potentials to include a large portion of giant miniature endplate potentials with slow rise and decay times.
J, Molgó, S, Gomez, R L, Polak, S, Thesleff   +3 more
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Squaric acid/4-aminoquinoline conjugates: Novel potent antiplasmodial agents

European Journal of Medicinal Chemistry, 2013
We report the synthesis and structure-activity relationship (SAR) analysis of a series of hybrid compounds containing a squaric moiety conjugated with heterocyclic moieties from well-known antimalarials. This novel series of compounds presents improved antiplasmodial activity compared with the squaric derivatives described in our previous work.
Ribeiro, Carlos J. A., Kumar, S. P., Gut, Jiri, Gonçalves, Lidia M., Rosenthal, Philip J., Moreira, Rui, Santos, Maria M. M.   +6 more
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4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Bioorganic & Medicinal Chemistry Letters, 2006
Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at ...
Jinlong, Jiang, Peter, Lin, Myle, Hoang, Lehua, Chang, Carina, Tan, Scott, Feighner, Oksana C, Palyha, Donna L, Hreniuk, Jie, Pan, Andreas W, Sailer, Nancy R, Morin, Douglas J, MacNeil, Andrew D, Howard, Lex H T, Van der Ploeg, Mark T, Goulet, Robert J, DeVita   +15 more
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