• Use of this drug is contraindicated in the presence of retinal or visual field changes either attributable to 4-aminoquinoline compounds or to any other etiology, and in patients with known hypersensitivity to 4-aminoquinoline compounds. (nih.gov)
  • 2014 ) Synthesis and evaluation of antimalarial properties of novel 4-aminoquinoline hybrid compounds. (academictree.org)
  • The evaluation of antimalarial drugs for possible reproductive toxicity especially at doses higher than recommended doses becomes very important as both malaria and infertility are of global concern. (ijpsr.com)
  • Chloroquine phosphate tablets are an antimalarial and amebicidal drug. (nih.gov)
  • Aminoquinoline drugs formulated as salts (chloroquine-phosphate, primaquine-diphosphate), but not chloroquine-base, also inhibited the reaction. (ox.ac.uk)
  • The compound has been used as a precursor for the synthesis of its derivatives. (wikipedia.org)
  • aminobenzoyl) benzenesulfonamide, and the synthesis of this and of some related compounds is described. (caltech.edu)
  • The synthesis of some 8-aminoquinolines related to isoplasmocid was carried out as part of a cooperative project to study to study their action on experimental poliomyelitis in monkeys. (caltech.edu)
  • Pyrimidine is used as parent substance for the synthesis of a wide variety of heterocyclic compounds and raw material for the synthesis of new molecule [ 12 ]. (biomedcentral.com)
  • All of these compounds, with the exception of primaquine (used primarily to combat P. vivax infections), are thought to share a common target: the formation of the parasite-specific substance hemozoin, described below, although additional targets may also be involved in some cases. (medscape.com)
  • Primaquine (PQ) diphosphate is an 8-aminoquinoline antimalarial drug with unique therapeutic properties. (rsbmt.org.br)
  • Primaquine (PQ) diphosphate is a prototypical drug in the 8-aminoquinoline group of antimalarial agents. (rsbmt.org.br)
  • In 2018, the US Food and Drug Administration approved the uses of a new hepatic schizontocidal and hypnozoitocidal 8-aminoquinoline called tafenoquine for the respective prevention of all malarias and for the treatment of those that relapse (P. vivax and Plasmodium ovale). (nih.gov)
  • The investigated compounds inhibit three unrelated pathogens (the Botulinum neurotoxin serotype A light chain (BoNT/A LC), Plasmodium falciparum malaria, and Ebola filovirus) via three different mechanisms of action. (ac.rs)
  • Malaria Hydroxychloroquine is 4-aminoquinoline antimalarial [see Microbiology (12.4)] and antirheumatic agent.Rheumatoid Arthritis, Systemic Lupus Erythematosus and Chronic Discoid LupusErythematosus The mechanisms underlying the anti-inflammatory and immunomodulatory effects of hydroxychloroquine sulfate in the treatment of rheumatoid arthritis, chronic discoid lupus erythematosus and systemic lupus erythematosus are not fully known. (drugcentral.org)
  • It has a role as an antimalarial, an antirheumatic drug and a dermatologic drug. (nih.gov)
  • Another antimalarial drug, mefloquine, which is not a 4-aminoquinoline like CQ/HCQ, has emerged as a potential anti-SARS-CoV-2 antiviral in vitro and has also been previously repurposed for respiratory diseases. (bvsalud.org)
  • For the eradication of malaria from hyperendemic regions of tropical Africa it is apparent that use may have to be made of antimalarial drugs, administered individually on a census basis, in addition to measures directed against the mosquito. (nih.gov)
  • The suppressive activity of existing compounds among individuals having different degrees of immunity is well established, and trials among large groups of people have been conducted with single drugs and with combination of drugs. (nih.gov)
  • Comparative efficacy and safety of chloroquine and alternative antimalarial drugs: a meta-analysis from six African countries. (nih.gov)
  • Notable examples include nerve damage among individuals homozygous for some variants of the N-acetyltransferase 2 gene ("slow acetylators") given isoniazid as an antituberculosis therapy, hemolytic anemia among glucose 6-phosphate dehydrogenase-deficient patients given aminoquinoline antimalarial drugs, and varied rates of biotransformation of debrisoquine, an antihypertensive drug, due to genetic variation at the CYP2D6 locus. (cdc.gov)
  • Repurposing approved and abandoned non-oncological drugs is an alternative approach to the identification and development of anticancer therapeutics, and antimalarials that target autophagic-lysosomal functions have recently attracted considerable attention as candidates for oncological repurposing. (nih.gov)
  • CQ is also rightly considered to be one of the most successful drugs ever produced, being a safe and cheap compound that has saved countless millions of lives. (medscape.com)
  • Unfortunately, malaria parasites have known resistance to older antimalarial drugs, which stems from the historical use of these drugs as a monotherapy or even as a folk remedy. (biomedcentral.com)
  • Although new types of antimalarial drugs are in development ( https://www.mmv.org/research-development/mmv-supported-projects ), their slow progress to the clinic means that current ACT developers need to select partner drugs from a limited set of older antimalarial compounds. (biomedcentral.com)
  • Aminoquinoline-based scaffolds such as ferroquine are promising but should be combined with good partner drugs for enhanced efficacy. (biomedcentral.com)
  • Recent declines in the clinical effectiveness of antimalarial drugs, including artemisinin-based combination therapy, have prompted the need to revise the definitions of and/or to recategorize antimalarial drug resistance to include extensively drug-resistant malaria. (cdc.gov)
  • This confusion is compounded by the fact that each pathogen is increasingly resistant to more drugs, and new descriptive terms such as multidrug resistant (MDR) and, for TB, extensively drug-resistant (XDR) have been introduced to describe these changes. (cdc.gov)
  • Standardization of the physicochemical parameters to assess in vitro the beta-hematin inhibitory activity of antimalarial drugs. (ox.ac.uk)
  • Like all drugs, antimalarials have the potential to cause adverse effects, though most people using chemoprophylaxis will have no or only minor adverse effects. (canada.ca)
  • Among them, compounds 2, 5, 10, 11 and 12 have significant antimicrobial activity against used bacterial and fungal strains and also found to be more active than the standard drugs. (biomedcentral.com)
  • The treatment of malaria has posed great challenge to medicine and development of efficient antimalarial drugs. (ijpsr.com)
  • The possibility of overdose and misappropriation in the usage of antimalarial agents are very common, all of which could lead to toxic effects of the drugs 7, 8 . (ijpsr.com)
  • Antimalarial drugs have been implicated in male infertility and CQ has been found to have dose dependent reduction in fertility of male rats 15, 16 . (ijpsr.com)
  • Artemisinin has been a very potent and effective antimalarial drug, especially when used in combination with other malaria medicines. (mmv.org)
  • Patients in whom chloroquine or hydroxychloroquine have failed to prevent or cure clinical malaria or parasitemia, or patients who acquired malaria in a geographic area where chloroquine resistance is known to occur should be treated with another form of antimalarial therapy (see WARNINGS and INDICATIONS AND USAGE, Limitations of Use). (nih.gov)
  • In a search for effective compounds against both the blood- and liver-stages of infection by malaria parasites with the ability to block the transmission of the disease to mosquito vectors, a series of hybrid compounds combining either a 1,2,4-trioxane or 1,2,4,5-tetraoxane and 8-aminoquinoline moieties were synthesized and screened for their antimalarial activity. (unl.pt)
  • In pregnant women, pharmacokinetics of antimalarials are affected by the large volume of distribution and higher clearance rate, suggesting that higher dosages might be warranted, particularly for treatment of malaria in pregnant women. (canada.ca)
  • Chloroquine (CQ) has been used widely as an antimalarial drug due to its quick action on blood schizontocide of different malarial parasite species for prophylaxis and treatment of malaria. (ijpsr.com)
  • It is an aminoquinoline commonly used in the tropics to treat malaria 9 . (ijpsr.com)
  • A variety of derivatives of 4-aminoquinoline are antimalarial agents useful in treating erythrocytic plasmodial infections. (wikipedia.org)
  • Pyrimidine is an aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds, from this facts, we have designed and synthesized a new class of pyrimidin-2-ol/thiol/amine derivatives and screened for its in vitro antimicrobial activity. (biomedcentral.com)
  • Read more about how MMV is working to tackle antimicrobial resistance to antimalarials. (mmv.org)
  • This is due to the development of resistance of parasite to mainly antimalarial agents 4, 5 resulting in huge impact on the socio-economy 6 . (ijpsr.com)
  • Quinoline-antimalarials inhibit BH formation. (ox.ac.uk)
  • Mechanism of Action: Chloroquine, a 4-aminoquinoline, is an anti-protozoal agent. (nih.gov)
  • A 4-aminoquinoline compound with anti-inflammatory properties. (nih.gov)
  • Here we report for the first time that amodiaquine (AQ), a clinical 4-aminoquinoline antimalarial with unexplored cancer-directed chemotherapeutic potential, causes autophagic-lysosomal and proliferative blockade in melanoma cells that surpasses that of its parent compound chloroquine. (nih.gov)
  • A pyrimidine derivative, proguanil, also emerged from the antimalarial pipeline during World War II. (mmv.org)
  • ACTs combine new endoperoxide-type compounds (such as artemether or artesunate) with older antimalarial drug classes, such as an aryl alcohol (lumefantrine) or an aminoquinoline (e.g., piperaquine), and provide rapid symptomatic relief. (biomedcentral.com)
  • Pyrimidine aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds [ 2 ]. (biomedcentral.com)
  • An antimalarial with properties similar to chloroquine that acts against eryt hrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions. (chemspider.com)
  • However, identification of compounds with activity against late stage P falciparum gametocytes is challenging as this stage is relatively metabolically inert and in vitro culture methods to produce gametocytes are much less straightforward than for asexual stage parasites. (biomedcentral.com)
  • This provides the first indication that compounds other than 8-aminoquinolines could be effective antimalarials against relapsing parasites. (bvsalud.org)
  • 7-chloro-4-[5-(n-ethyl-n-2-hydroxyethylamino)-2-pentyl] aminoquinoline, its acid addition salts, and method of preparation Application Date: July 23, 1949 Grant Date: March 27, 1951 Current Assignee: STWB Inc This patent proposes a method to prepare 7-chloro-4-(5-(N- ethyl-N - 2 - hydroxyethylamino)-2-pentyl) aminoquinoline. (copperpodip.com)
  • The compound is useful as an antimalarial agent and can be used either in the free base form or in the form of its acid-addition salts. (copperpodip.com)
  • Since cumulative research suggests that dependence on autophagy represents a specific vulnerability of malignant melanoma cells, we screened a focused compound library of antimalarials for antimelanoma activity. (nih.gov)
  • These compounds were tested elsewhere and found to be without specific activity. (caltech.edu)
  • Quantitative structure-activity relationship models for describing biological activity against the BoNT/A LC and malarial strains also include overall compound polarity, electron density distribution, and proton donor/acceptor potential. (ac.rs)
  • [ 14 ] It is appropriate to begin with the 4-aminoquinoline CQ, which became clinically available in 1947 as a less toxic and more readily produced substitute for QN, and is one of the longest-serving of the synthetic antimalarials that appeared over the course of the last century. (medscape.com)
  • It has been found that certain strains of P. falciparum have become resistant to 4-aminoquinoline compounds (including chloroquine and hydroxychloroquine). (nih.gov)
  • Chloroquine is an antimalarial agent. (nih.gov)
  • Accordingly, sensitive and reliable methods to analyze PQ in the blood plasma are essential to monitor drug levels in patients under treatment and to study the kinetics of this antimalarial agent in animal models. (rsbmt.org.br)
  • Given the lack of affordable alternatives, chloroquine remains the first-line antimalarial agent in most African countries. (ijpsr.com)
  • For radical cure of P. vivax and P. ovale infections, concomitant therapy with an 8-aminoquinoline drug is necessary. (nih.gov)
  • Other compounds, including methylene blue (potential transmission blocker) and fosmidomycin (DXP reductoisomerase inhibitor), are available but cannot be used in children. (biomedcentral.com)
  • Furthermore, models for Ebola filovirus inhibition are presented qualitatively to provide insights into parameters that may contribute to the compounds' antiviral activities. (ac.rs)
  • Standardization of test conditions is essential for studying the interaction of compounds with this process and screening potential inhibitors. (ox.ac.uk)
  • Not recommended in patients with known allergy to 4-aminoquinoline compounds. (com.pk)
  • To assess drug tolerance and if time permits, start the antimalarial regimen several days or weeks (depending on the antimalarial prescribed) before travel (see Chapter 4). (canada.ca)
  • For example, aminoquinolines work by the same mechanism as quinine, which is the active ingredient in antimalarial tonic water and Jesuit's bark. (biomedcentral.com)
  • 4-Aminoquinoline is a form of aminoquinoline with the amino group at the 4-position of the quinoline. (wikipedia.org)
  • In 1945, a modification of this compound via hydroxylation led to the development of Hydroxychloroquine(C18H26ClN3O), which was found to be less toxic and remains in use, without change, to this day. (copperpodip.com)