Journal ArticleDOI
Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: a review.
Md. Mushtaque,Shahjahan +1 more
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TLDR
The role of modification of the core structure of CQ and its effects on the biological activities are described and the attempt has been made to predict the future prospects of such drugs to reemerge as antimalarial agents.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2015-01-27. It has received 74 citations till now. The article focuses on the topics: Antimalarial Agent.read more
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Chloroquine analogues in drug discovery: new directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases
TL;DR: This review is concerned with the lysosomotropic, anti-inflammatory and immunomodulatory mechanisms of chloroquine, hydroxychloroquines, quinacrine and related analogues, and the current evidence for both their beneficial effects and potential adverse manifestations in various diseases.
Journal ArticleDOI
The past, present and future of anti-malarial medicines
TL;DR: The range of anti-malarial medicines developed over the years are reviewed, beginning with the discovery of quinine in the early 1800s, through to modern day ACT and the recently-approved tafenoquine.
Journal ArticleDOI
Chloroquine against malaria, cancers and viral diseases.
TL;DR: The underlying mechanisms behind the antimalarial, anticancer and antiviral effects of CQ are reviewed and the clinical evidence for the use of C Q and hydroxychloroquine (HCQ) against COVID-19 is discussed.
Journal ArticleDOI
The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines
Luiz C. S. Pinheiro,Lívia M. Feitosa,Lívia M. Feitosa,Marilia O. Gandi,Marilia O. Gandi,Flávia F. Silveira,Flávia F. Silveira,Nubia Boechat,Nubia Boechat +8 more
TL;DR: The importance of quinoline and non-quinoline derivatives in vitro with activity against the W2 chloroquine-resistant (CQR) Plasmodium falciparum clone strain and in vivo against Plas modium berghei-infected mouse model is demonstrated.
Journal ArticleDOI
Evaluation of 7-arylaminopyrazolo[1,5-a]pyrimidines as anti-Plasmodium falciparum, antimalarial, and Pf-dihydroorotate dehydrogenase inhibitors
Luís Felipe S.P. Azeredo,Julia Penna Coutinho,Valquíria A. P. Jabor,Patricia R. Feliciano,Maria Cristina Nonato,Carlos R. Kaiser,Carla Maria S. Menezes,Amanda S.O. Hammes,Ernesto Raul Caffarena,Lucas Villas Bôas Hoelz,Nicolli B de Souza,Glaécia A. N. Pereira,Isabela P. Ceravolo,Antoniana U. Krettli,Nubia Boechat,Nubia Boechat +15 more
TL;DR: Fifteen 7-arylpyrazolo[1,5-a]pyrimidine derivatives are designed and synthesized using ring bioisosteric replacement and molecular hybridization of functional groups based on the highly active 5-methyl-N-(naphthalen-2-yl)-2-(trifluoromethyl)- [1,2,4]triazolo-7-amine and showed increased drug activity.
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Development of a New Generation of 4-Aminoquinoline Antimalarial Compounds Using Predictive Pharmacokinetic and Toxicology Models
Sunetra Ray,Peter B. Madrid,Paul Catz,Susanna E. LeValley,Michael J. Furniss,Linda L. Rausch,R. Kiplin Guy,Joseph L. DeRisi,Lalitha V. Iyer,Carol E. Green,Jon C. Mirsalis +10 more
TL;DR: Two lead molecules, 18 and 4, with promising in vitro therapeutic efficacy, improved ADMET properties, low risk for drug-drug interactions, and desirable pharmacokinetic profiles are identified and are desirable candidates to pursue in future clinical trials.
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A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease.
James C. Burnett,Dejan Opsenica,Kamaraj Sriraghavan,Rekha G. Panchal,Gordon Ruthel,Ann R. Hermone,Tam Luong Nguyen,Tara Kenny,Douglas Lane,Connor F. McGrath,James J. Schmidt,Jonathan L. Vennerstrom,Rick Gussio,Bogdan A. Šolaja,Sina Bavari +14 more
TL;DR: Four new, potent inhibitors of a structurally diverse small molecule (non-peptidic) inhibitors of the botulinum neurotoxin serotype A (BoNT/A) light chain (LC) are identified, supporting the structure-based pharmacophore contribution to inhibition.
Journal ArticleDOI
In Vitro Activity of Ferroquine Is Independent of Polymorphisms in Transport Protein Genes Implicated in Quinoline Resistance in Plasmodium falciparum
Maud Henry,Sébastien Briolant,Albin Fontaine,Joel Mosnier,Eric Baret,Rémy Amalvict,Thierry Fusai,Laurent Fraisse,Christophe Rogier,Bruno Pradines +9 more
TL;DR: The in vitro activity of ferroquine against 15 Plasmodium falciparum strains was assessed and compared with those of chloroquine, quinine (QN), monodesethylamodiaquine (MDAQ), and mefloquine (MQ).
Journal ArticleDOI
Synthesis, Characterization, and Pharmacological Evaluation of Silicon-Containing Aminoquinoline Organometallic Complexes As Antiplasmodial, Antitumor, and Antimycobacterial Agents
Yiqun Li,Carmen de Kock,Pete Smith,Hajira Guzgay,Denver T. Hendricks,Krupa Naran,Valerie Mizrahi,Digby F. Warner,Kelly Chibale,Gregory S. Smith +9 more
TL;DR: Two silicon-containing analogues (1, 2) of chloroquine, modified in the lateral side chain with organosilicon moieties, were synthesized and further reacted with dinuclear half-sandwich transition metal precursors [Ru(Ar)(μ-Cl)Cl]2 as discussed by the authors.
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Harnessing evolutionary fitness in Plasmodium falciparum for drug discovery and suppressing resistance
Amanda K. Lukens,Leila S. Ross,Richard W. Heidebrecht,Francisco-Javier Gamo,Maria J. Lafuente-Monasterio,Michael Booker,Daniel L. Hartl,Roger C. Wiegand,Dyann F. Wirth,Dyann F. Wirth +9 more
TL;DR: These findings indicate that pairing inhibitors that target the bulk wild-type population and the small, emerging resistant population can suppress the rise and spread of drug resistance.