Journal ArticleDOI
Novel 4-Aminoquinolines Active against Chloroquine-Resistant and Sensitive P. falciparum Strains that also Inhibit Botulinum Serotype A
Bogdan A. Šolaja,Dejan Opsenica,Kirsten S. Smith,Wilbur K. Milhous,Nataša Terzić,Igor Opsenica,James C. Burnett,Jon E. Nuss,Rick Gussio,Sina Bavari +9 more
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TLDR
Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.Abstract:
We report on the initial result of the coupling of 4-amino-7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC90 (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low micromolar levels (7−31 μM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.read more
Citations
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Quinolines and structurally related heterocycles as antimalarials
TL;DR: This review provides a comprehensive literature compilation concerning the study of quinolines and also other heterocycles structurally similar to quinoline scaffold in the treatment of malaria.
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The Lipophilic Bullet Hits the Targets: Medicinal Chemistry of Adamantane Derivatives
Journal ArticleDOI
Quinoline hybrids and their antiplasmodial and antimalarial activities.
TL;DR: This review aims to summarize the recent advances towards the discovery of antiplasmodial and antimalarial hybrids including quinoline skeleton to provide an insight for rational designs of more active and less toxic quinolines hybrids antimalarials.
Journal ArticleDOI
Synthesis and in vitro antitubercular activity of a series of quinoline derivatives.
Marcus Vinícius Nora de Souza,Karla C. Pais,Karla C. Pais,Carlos R. Kaiser,Monica Amado Peralta,Marcelle de Lima Ferreira,Marcelle de Lima Ferreira,Maria C.S. Lourenço +7 more
TL;DR: A series of 33 quinoline derivatives synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv exhibited a significant activity when compared with first line drugs such as ethambutol and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis.
Journal ArticleDOI
Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation.
TL;DR: A short history of hybrid molecules based on aminoquinolines gave interesting and important information useful for organic and medicinal chemistry, which are deeply involved in the design and development of new antimalarial agents.
References
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Journal ArticleDOI
Identification of an antimalarial synthetic trioxolane drug development candidate.
Jonathan L. Vennerstrom,Sarah Arbe-Barnes,Reto Brun,Susan A. Charman,Francis C. K. Chiu,Jacques Chollet,Yuxiang Dong,Arnulf Dorn,Daniel Hunziker,Hugues Matile,Kylie Anne McIntosh,Maniyan Padmanilayam,Josefina Santo Tomas,Christian Scheurer,Bernard Scorneaux,Yuanqing Tang,Heinrich Urwyler,Sergio Wittlin,William N. Charman +18 more
TL;DR: Here it is described how a synthetic peroxide antimalarial drug development candidate was identified in a collaborative drug discovery project.
Journal ArticleDOI
Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue.
TL;DR: Four 7-chloro-4-[[[2-[(N,N-substituted amino)methyl]ferrocenyl]methyl]amino]quinoline derivatives have been synthesized and one of them, 1a, showed high potent antimalarial activity in vivo on mice infected with Plasmodium berghei N. and Plas modium yoelii NS.
Journal ArticleDOI
Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines.
TL;DR: In the studies reported here, structure-activity relationships (SARs) among AQs with different N, N-diethyldiaminoalkane side chains and different substituents at the 7-position occupied by Cl in chloroquine are examined.
Journal ArticleDOI
Endoproteinase Activity of Type A Botulinum Neurotoxin: Substrate Requirements and Activation by Serum Albumin
TL;DR: It is found that bovine and other serum albumins stimulated the type A-catalyzed hydrolysis of synthetic peptide substrates, through a direct effect on the kinetic constants of the reaction.
Journal ArticleDOI
Synthesis and Antimalarial Activity of Side Chain Modified 4-Aminoquinoline Derivatives
TL;DR: A new series of side-chain modified 4-aminoquinolines have been synthesized and found active against P. falciparum in vitro and P. yoelli in vivo, suggesting that this class of compounds act on a heme polymerization target.
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