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https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#1
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Sabroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasites lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites equivalent to the known antimalarials, chloroquine and mefloquine...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28077744/neuropsychiatric-outcomes-after-mefloquine-exposure-among-u-s-military-service-members
#2
Angelia A Eick-Cost, Zheng Hu, Patricia Rohrbeck, Leslie L Clark
Mefloquine was widely prescribed to U.S. military service members until 2009 when use was limited to personnel with contraindications to doxycycline and no contraindications to mefloquine. The need to estimate the occurrence of neuropsychiatric outcomes (NPOs) in service members prescribed mefloquine warranted a comprehensive evaluation of this issue. Active component service members filling a prescription for mefloquine, doxycycline, or atovaquone/proguanil (A/P) between January 1, 2008 and June 30, 2013, were included in the analysis...
January 11, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28068604/2-8-bis-trifluoromethyl-quinoline-analogs-show-improved-anti-zika-virus-activity-compared-to-mefloquine
#3
Giselle Barbosa-Lima, Adriana M Moraes, Adriele da S Araújo, Emerson T da Silva, Caroline S de Freitas, Yasmine R Vieira, Andressa Marttorelli, José Cerbino Neto, Patrícia T Bozza, Marcus V N de Souza, Thiago Moreno L Souza
Zika virus (ZIKV), an arthropod-born Flavivirus, has been associated with a wide range of neurological diseases in adults, foetuses and neonates. Since no vaccine is available, repurposing of antiviral drugs currently in medical use is necessary. Mefloquine has confirmed anti-ZIKV activity. We used medicinal chemistry-driven approaches to synthesize and evaluate the ability of a series of new 2,8-bis(trifluoromethyl)quinoline derivatives to inhibit ZIKV replication in vitro, in order to improve the potency of mefloquine...
December 30, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28063022/identification-of-a-syndrome-class-of-neuropsychiatric-adverse-reactions-to-mefloquine-from-latent-class-modeling-of-fda-adverse-event-reporting-system-data
#4
Remington L Nevin, Jeannie-Marie Leoutsakos
INTRODUCTION: Although mefloquine use is known to be associated with a risk of severe neuropsychiatric adverse reactions that are often preceded by prodromal symptoms, specific combinations of neurologic or psychiatric reactions associated with mefloquine use are not well described in the literature. This study sought to identify a distinct neuropsychiatric syndrome class associated with mefloquine use in reports of adverse events. METHODS: Latent class modeling of US Food and Drug Administration Adverse Event Reporting System (FAERS) data was performed using indicators defined by the Medical Dictionary for Regulatory Activities neurologic and psychiatric high-level group terms, in a study dataset of FAERS reports (n = 5332) of reactions to common antimalarial drugs...
January 6, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28057491/mefloquine-inhibits-voltage-dependent-nav1-4-channel-by-overlapping-the-local-anaesthetic-binding-site
#5
Bertin Paiz-Candia, Angel A Islas, Alfredo Sánchez-Solano, Claudia Mancilla-Simbro, Thomas Scior, Lourdes Millan-PerezPeña, Eduardo M Salinas-Stefanon
Mefloquine constitutes a multitarget antimalaric that inhibits cation currents. However, the effect and the binding site of this compound on Na(+) channels is unknown. To address the mechanism of action of mefloquine, we employed two-electrode voltage clamp recordings on Xenopus laevis oocytes, site-directed mutagenesis of the rat Na(+) channel, and a combined in silico approach using Molecular Dynamics and docking protocols. We found that mefloquine: i) inhibited Nav1.4 currents (IC50 =60μM), ii) significantly delayed fast inactivation but did not affect recovery from inactivation, iii) markedly the shifted steady-state inactivation curve to more hyperpolarized potentials...
January 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28044042/influence-of-the-pfmdr1-gene-on-in-vitro-sensitivities-of-piperaquine-in-thai-isolates-of-plasmodium-falciparum
#6
Mathirut Mungthin, Ekularn Watanatanasup, Naruemon Sitthichot, Nantana Suwandittakul, Rommanee Khositnithikul, Stephen A Ward
Piperaquine combined with dihydroartemisinin is one of the artemisinin derivative combination therapies, which can replace artesunate-mefloquine in treating uncomplicated falciparum malaria in Thailand. The aim of this study was to determine the in vitro sensitivity of Thai Plasmodium falciparum isolates against piperaquine and the influence of the pfmdr1 gene on in vitro response. One hundred and thirty-seven standard laboratory and adapted Thai isolates of P. falciparum were accessed for in vitro piperaquine sensitivity...
January 2, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28039388/efficacy-and-safety-of-artesunate-mefloquine-therapy-for-treating-uncomplicated-plasmodium-falciparum-malaria-systematic-review-and-meta-analysis
#7
REVIEW
Henry Maia Peixoto, Paola Barbosa Marchesini, Maria Regina Fernandes de Oliveira
INTRODUCTION: The present study is a systematic review of the literature on the efficacy and safety of the treatment of uncomplicated Plasmodium falciparum infections with artesunate-mefloquine (ASMQ) compared to other artemisinin-based combination therapies (ACTs), designed to assist decision makers in Brazil. METHODS: Twenty-four randomized controlled trials (RCTs) were selected in four electronic databases and in complementary sources. Meta-analyses were performed to evaluate the efficacy expressed by relative risks (RR) obtained from treatment failure confirmed by the PCR...
December 29, 2016: Transactions of the Royal Society of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28035111/comparison-of-who-mark-iii-and-hrp-ii-elisa-for-in-vitro-sensitivity-of-plasmodium-falciparum
#8
Supriya Sharma, Neelima Mishra, Neena Valecha, Anupkumar R Anvikar
BACKGROUND & OBJECTIVES: Antimalarial drug resistance is a serious challenge to malaria control worldwide. In vitro sensitivity assays provide an early indication of emerging drug resistance. In vitro susceptibility of field and culture adapted Plasmodium falciparum isolates to different antimalarials was compared using two Methods: World Health Organization (WHO) micro-test (MARK III) and histidine rich protein II (HRP II) based enzyme- linked immunosorbent assay (ELISA). METHODS: In total, 50 P...
October 2016: Journal of Vector Borne Diseases
https://www.readbyqxmd.com/read/28028628/risk-of-drug-resistance-in-plasmodium-falciparum-malaria-therapy-a-systematic-review-and-meta-analysis
#9
Li-Juan Zhou, Jing Xia, Hai-Xia Wei, Xiao-Jun Liu, Hong-Juan Peng
Plasmodium falciparum is responsible for the vast majority of the morbidity and mortality associated with malaria infection globally. Although a number of studies have reported the emergence of drug resistance in different therapies for P. falciparum infection, the degree of the drug resistance in different antimalarials is still unclear. This research investigated the risk of drug resistance in the therapies with different medications based on meta-analyses. Relevant original randomized control trials (RCTs) were searched in all available electronic databases...
December 27, 2016: Parasitology Research
https://www.readbyqxmd.com/read/27986683/high-rate-of-treatment-failures-in-nonimmune-travelers-treated-with-artemether-lumefantrine-for-uncomplicated-plasmodium-falciparum-malaria-in-sweden-retrospective-comparative-analysis-of-effectiveness-and-case-series
#10
Klara Sondén, Katja Wyss, Irina Jovel, Antero Vieira da Silva, Anton Pohanka, Muhammad Asghar, Manijeh Vafa Homann, Lars L Gustafsson, Urban Hellgren, Anna Färnert
BACKGROUND: Artemisinin-based combination therapy (ACT) is the first-line treatment of Plasmodium falciparum malaria. Since the introduction of artemether-lumefantrine (AL) for treatment of uncomplicated malaria in Sweden, treatment failures have been reported in adults. METHODS: A retrospective comparative analysis of treatment regimen for P. falciparum malaria in adults in Stockholm during 2000-2015 was performed to evaluate the effectiveness of AL. Parasite genotyping and drug concentrations were investigated in the AL treatment failures...
October 24, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941941/potentiation-of-amitriptyline-anti-hyperalgesic-like-action-by-astroglial-connexin-43-inhibition-in-neuropathic-rats
#11
Tiffany Jeanson, Adeline Duchêne, Damien Richard, Sylvie Bourgoin, Christèle Picoli, Pascal Ezan, Franck Mouthon, Christian Giaume, Michel Hamon, Mathieu Charvériat
Antidepressants, prescribed as first line treatment of neuropathic pain, have a limited efficacy and poorly tolerated side effects. Because recent studies pointed out the implication of astroglial connexins (Cx) in both neuropathic pain and antidepressive treatment, we investigated whether their blockade by mefloquine could modulate the action of the tricyclic antidepressant amitriptyline. Using primary cultures, we found that both mefloquine and amitriptyline inhibited Cx43-containing gap junctions, and that the drug combination acted synergically...
December 12, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27940685/prenatal-iron-deficiency-neonatal-ferritin-and-infant-cognitive-function
#12
Michael O Mireku, Leslie L Davidson, Michael J Boivin, Romeo Zoumenou, Achille Massougbodji, Michel Cot, Florence Bodeau-Livinec
OBJECTIVE: To investigate the impact of prenatal maternal iron deficiency (ID) on cord blood serum ferritin (CBSF) concentration and infant cognitive and motor development. METHODS: Our prospective cohort study included 636 mother-singleton child pairs from 828 eligible pregnant women who were enrolled during their first antenatal care (ANC) visit in Allada, Benin, into a clinical trial comparing the efficacy of mefloquine and sulfadoxine-pyrimethamine. Venous blood samples of women were assessed for ferritin and hemoglobin concentrations at the first and second ANC visits (occurring at least 1-month apart) and at delivery...
December 2016: Pediatrics
https://www.readbyqxmd.com/read/27936682/catalytic-kinetic-resolution-of-saturated-n-heterocycles-by-enantioselective-amidation-with-chiral-hydroxamic-acids
#13
Imants Kreituss, Jeffrey W Bode
The preparation of enantioenriched chiral compounds by kinetic resolution dates back to the laboratories of Louis Pasteur in the middle of the 19th century. Unlike asymmetric synthesis, this process can always deliver enantiopure material (ee > 99%) if the reactions are allowed to proceed to sufficient conversion and the selectivity of the process is not unity (s > 1). One of the most appealing and practical variants is acylative kinetic resolution, which affords easily separable reaction products, and several highly efficient enzymatic and small molecule catalysts are available...
December 20, 2016: Accounts of Chemical Research
https://www.readbyqxmd.com/read/27919892/significant-divergence-in-sensitivity-to-antimalarial-drugs-between-neighboring-plasmodium-falciparum-populations-along-the-eastern-border-of-myanmar
#14
Weilin Zeng, Yao Bai, Meilian Wang, Zenglei Wang, Shuang Deng, Yonghua Ruan, Shi Feng, Zhaoqing Yang, Liwang Cui
Malaria parasites in different endemic areas display different levels of resistance to antimalarial drugs as the result of varied drug use histories. To provide updated knowledge of drug sensitivities during the malaria elimination phase in Southeast Asia, an epicenter of multidrug resistance, we determined in vitro susceptibilities of culture-adapted Plasmodium falciparum isolates from two eastern border regions (Wa and Kachin) of Myanmar to ten drugs. Despite their close proximity, the Kachin parasites displayed higher IC50 values than the Wa parasites to chloroquine, piperaquine, naphthoquine, mefloquine, quinine, pyrimethamine, pyronaridine, lumefantrine and dihydroartemisinin...
December 5, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27895848/four-artemisinin-based-treatments-in-african-pregnant-women-with-malaria
#15
Divine Pekyi, Akua A Ampromfi, Halidou Tinto, Maminata Traoré-Coulibaly, Marc C Tahita, Innocent Valéa, Victor Mwapasa, Linda Kalilani-Phiri, Gertrude Kalanda, Mwayiwawo Madanitsa, Raffaella Ravinetto, Theonest Mutabingwa, Prosper Gbekor, Harry Tagbor, Gifty Antwi, Joris Menten, Maaike De Crop, Yves Claeys, Celine Schurmans, Chantal Van Overmeir, Kamala Thriemer, Jean-Pierre Van Geertruyden, Umberto D'Alessandro, Michael Nambozi, Modest Mulenga, Sebastian Hachizovu, Jean-Bertin B Kabuya, Joyce Mulenga
BACKGROUND: Information regarding the safety and efficacy of artemisinin combination treatments for malaria in pregnant women is limited, particularly among women who live in sub-Saharan Africa. METHODS: We conducted a multicenter, randomized, open-label trial of treatments for malaria in pregnant women in four African countries. A total of 3428 pregnant women in the second or third trimester who had falciparum malaria (at any parasite density and regardless of symptoms) were treated with artemether-lumefantrine, amodiaquine-artesunate, mefloquine-artesunate, or dihydroartemisinin-piperaquine...
September 2016: Malawi Medical Journal: the Journal of Medical Association of Malawi
https://www.readbyqxmd.com/read/27890675/synergistic-drug-combination-effectively-blocks-ebola-virus-infection
#16
Wei Sun, Shihua He, Carles Martínez-Romero, Jennifer Kouznetsova, Gregory Tawa, Miao Xu, Paul Shinn, Ethan G Fisher, Yan Long, Omid Motabar, Shu Yang, Philip E Sanderson, Peter R Williamson, Adolfo García-Sastre, Xiangguo Qiu, Wei Zheng
Although a group of FDA-approved drugs were previously identified with activity against Ebola virus (EBOV), most of them are not clinically useful because their human blood concentrations are not high enough to inhibit EBOV infection. We screened 795 unique three-drug combinations in an EBOV entry assay. Two sets of three-drug combinations, toremifene-mefloquine-posaconazole and toremifene-clarithromycin-posaconazole, were identified that effectively blocked EBOV entry and were further validated for inhibition of live EBOV infection...
January 2017: Antiviral Research
https://www.readbyqxmd.com/read/27889812/research-progress-of-hydroxychloroquine-and-autophagy-inhibitors-on-cancer
#17
REVIEW
Ting-Ting Shi, Xiao-Xu Yu, Li-Jun Yan, Hong-Tao Xiao
PURPOSE: Hydroxychloroquine (HCQ), the analog of chloroquine, augments the effect of chemotherapies and radiotherapy on various tumors identified in the current clinical trials. Meanwhile, the toxicity of HCQ retinopathy raises concern worldwide. Thus, the potent autophagy inhibitors are urgently needed. METHODS: A systematic review was related to 'hydroxychloroquine' or 'chloroquine' with 'clinical trials,' 'retinopathy' and 'new autophagy inhibitors.' This led to many cross-references involving HCQ, and these data have been incorporated into the following study...
November 26, 2016: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/27889529/antiviral-activities-of-selected-antimalarials-against-dengue-virus-type-2-and-zika-virus
#18
Anuradha Balasubramanian, Tadahisa Teramoto, Amol A Kulkarni, Apurba K Bhattacharjee, Radhakrishnan Padmanabhan
In a previous study, twelve antimalarial compounds, amodiaquine (AQ) and derivatives, were shown to have potent anti-dengue viral (DENV) activity by using the stable DENV2 Renilla luciferase reporter replicon expressing BHK-21 cells, infectivity (plaque), and the qRT-PCR assays. In this study, we performed molecular modeling on these compounds to determine their stereo-electronic properties required for optimal antiviral activity. Based on the similarity of calculated stereo-electronic profiles, specifically the electrostatic potential profiles of the compounds, and in silico screening of related compounds from literature, we identified three additional compounds, Quinacrine (QC), Mefloquine (MQ), and GSK369796...
January 2017: Antiviral Research
https://www.readbyqxmd.com/read/27866919/in-vitro-sensitivity-of-antimalarial-drugs-and-correlation-with-clinico-parasitological-response-following-treatment-with-a-3-day-artesunate-mefloquine-combination-in-patients-with-falciparum-malaria-along-the-thai-myanmar-border
#19
Phunuch Muhamad, Artitaya Thiengsusuk, Papichaya Phompradit, Kesara Na-Bangchang
A 3-day artesunate-mefloquine combination therapy has been using as first-line treatment for acute uncomplicated Plasmodium falciparum malaria in Thailand since 1995 on the background of mefloquine resistance. The aim of the present study was to assess sensitivity of P. falciparum isolates (n=44) in an area along the Thai-Myanmar border (year 2009) to artesunate, mefloquine, chloroquine and quinine, including their correlation with clinico-parasitological response. Twenty, 19, and 5 isolates were collected from patients with 'Adequate Clinical and Parasitological Response (ACPR)', 'Late Parasitological Failure (LPF)' and 're-infection', respectively...
February 2017: Acta Tropica
https://www.readbyqxmd.com/read/27853090/steroid-pulse-therapy-may-mitigate-prolonged-neurological-manifestations-after-eradication-of-severe-plasmodium-falciparum-parasitemia
#20
Chihiro Hasegawa, Akiko Inagaki, Gohei Yamada, Koji Morita, Isamu Kitamura, Koya Ariyoshi
A 58-year-old Japanese man with a high parasitemia of Plasmodium falciparum, returning from Uganda, was admitted to our hospital since his consciousness level rapidly deteriorated after the initial dose of mefloquine. Despite the parasitemia was cleared by quinine by day 7, the coma remained unchanged and diffuse leukoencephalopathy was detected on magnetic resonance image. Steroid pulse therapy was initiated on day 8. Subsequently, the neurological manifestations improved and he was discharged on day 73 without any sequelae...
2016: Internal Medicine
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