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https://www.readbyqxmd.com/read/28102941/synthesis-of-primaquine-glyco-conjugates-as-potential-tissue-schizontocidal-antimalarial-agents
#1
Chandra S Azad, Mridula Saxena, Arif J Siddiqui, Jyoti Bhardwaj, Sunil K Puri, Guru P Dutta, Nity Anand, Anil K Saxena
Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to be direct the drug to the liver, where hypnozoites resides...
January 19, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28101469/concurrent-inflammation-augments-antimalarial-drugs-induced-liver-injury-in-rats
#2
Hossein Niknahad, Reza Heidari, Roya Firuzi, Farzaneh Abazari, Maral Ramezani, Negar Azarpira, Massood Hosseinzadeh, Asma Najibi, Arastoo Saeedi
Purpose: Accumulating evidence suggests that drug exposure during a modest inflammation induced by bacterial lipopolysaccharide (LPS) might increase the risk of drug-induced liver injury. The current investigation was designed to test if antimalarial drugs hepatotoxicity is augmented in LPS‑treated animals. Methods: Rats were pre-treated with LPS (100 µg/kg, i.p). Afterward, non-hepatotoxic doses of amodiaquine (25, 50 and 100 mg/kg, oral) and chloroquine (25, 50 and 100 mg/kg, oral) were administered. Results: Interestingly, liver injury was evident only in animals treated with both drug and LPS as estimated by pathological changes in serum biochemistry (ALT, AST, LDH, and TNF-α), and liver tissue (severe hepatitis, endotheliitis, and sinusoidal congestion)...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28094524/antimalarial-pyrido-1-2-a-benzimidazoles-lead-optimization-parasite-life-cycle-stage-profile-mechanistic-evaluation-killing-kinetics-and-in-vivo-oral-efficacy-in-a-mouse-model
#3
Kawaljit Singh, John Okombo, Christel Brunschwig, Ferdinand Ndubi, Linley Barnard, Chad Wilkinson, Peter M Njogu, Mathew Njoroge, Lizahn Laing, Marta Machado, Miguel Prudêncio, Janette Reader, Mariette E Botha, Sindisiwe H Nondaba, Lyn-Marie Birkholtz, Sonja Lauterbach, Alisje Churchyard, Theresa L Coetzer, Jeremy N Burrows, Clive Leonard Yeates, Paolo Denti, Lubbe Wiesner, Timothy J Egan, Sergio Wittlin, Kelly Chibale
Further structure activity relationship (SAR) studies on the recently identified pyrido[1,2-a]benzimidazole (PBI) antimalarials, have led to the identification of potent, metabolically stable compounds with improved in vivo oral efficacy in the P. berghei mouse model and additional activity against parasite liver and gametocyte stages, making them potential candidates for preclinical development. Inhibition of haemozoin formation possibly contributes to the mechanism of action.
January 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28089716/a-characterization-of-the-antimalarial-activity-of-the-bark-of-cylicodiscus-gabunensis-harms
#4
Omar Aldulaimi, Fidelia I Uche, Hamza Hameed, Haddijatou Mbye, Imran Ullah, Falko Drijfhout, Timothy D W Claridge, Paul Horrocks, Wen-Wu Li
ETHNOPHARMACOLOGICAL RELEVANCE AND AIM: A decoction of the bark of Cylicodiscus gabunensis Harms is used as a traditional medicine in the treatment of malaria in Nigeria. This study aims to validate the antimalarial potency of this decoction in vitro against Plasmodium falciparum and define potential bioactive constituents within the C. gabunensis bark. MATERIALS AND METHODS: A bioassay-guided separation and fractionation protocol was applied to C. gabunensis extracts, exploiting the use of a Malaria Sybr Green I Fluorescence assay method to monitor antiproliferative effects on parasites as well as define 50% inhibition concentrations...
January 9, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28086782/in-vivo-antiplasmodial-activity-and-toxicological-assessment-of-hydroethanolic-crude-extract-of-ajuga-remota
#5
Aschalew Nardos, Eyasu Makonnen
BACKGROUND: Malaria is one of the most life-threatening health problems worldwide and treatment has been compromised by drug resistance. Identifying lead molecules from natural products might help to find better anti-malarial drugs, since those obtained from natural sources are still effective against malarial parasites. This study aimed at investigating the in vivo antiplasmodial activity of crude extract of the leaves of Ajuga remota together with its safety in mice models. METHODS: In vivo parasite growth inhibitory effect of crude extract was assessed in mice inoculated with Plasmodium berghei (ANKA strain)...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#6
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/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#7
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070009/a-malaria-ecology-index-predicted-spatial-and-temporal-variation-of-malaria-burden-and-efficacy-of-antimalarial-interventions-based-on-african-serological-data
#8
Gordon C McCord, Jesse K Anttila-Hughes
Reducing the global health burden of malaria is complicated by weak reporting systems for infectious diseases and a paucity of vital statistics registration. This limits our ability to predict changes in malaria health burden intensity, target antimalarial resources where needed, and identify malaria impacts in retrospective data. We refined and deployed a temporally and spatially varying Malaria Ecology Index (MEI) incorporating climatological and ecological data to estimate malaria transmission strength and validate it against cross-sectional serology data from 39,875 children from seven sub-Saharan African countries...
January 9, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28069075/domestic-trends-in-malaria-research-and-development-in-china-and-its-global-influence
#9
Yang-Mu Huang, Lu-Wen Shi, Rui She, Jing Bai, Shi-Yong Jiao, Yan Guo
BACKGROUND: Though many countries, including China, are moving towards malaria elimination, malaria remains a major global health threat. Due to the spread of antimalarial drug resistance and the need for innovative medical products during the elimination phase, further research and development (R&D) of innovative tools in both epidemic and elimination areas is needed. This study aims to identify the trends and gaps in malaria R&D in China, and aims to offer suggestions on how China can be more effectively involved in global malaria R&D...
January 10, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/28065567/synthesis-identification-and-in-vitro-biological-evaluation-of-some-novel-quinoline-incorporated-1-3-thiazinan-4-one-derivatives
#10
S Umamatheswari, C Sankar
The present study describes the synthesis of two new series of 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a-j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one derivatives (5a-7j). All the compounds were synthesized in moderate to good yield by one-pot three component cyclo-condensation reaction. The newly synthesized compounds were characterized by FT-IR, (1)H, (13)C NMR and elemental analysis. The compounds were screened for their in vitro antibacterial activity against a panel of pathogenic bacterial strains, antitubercular activity against Mycobacterium tuberculosis H37Rv and also for their in vitro antimalarial activity against Plasmodium falciparum...
June 16, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28064377/octopus-a-platform-for-the-virtual-high-throughput-screening-of-a-pool-of-compounds-against-a-set-of-molecular-targets
#11
Eduardo Habib Bechelane Maia, Vinícius Alves Campos, Bianca Dos Reis Santos, Marina Santos Costa, Iann Gabriel Lima, Sandro J Greco, Rosy I M A Ribeiro, Felipe M Munayer, Alisson Marques da Silva, Alex Gutterres Taranto
Octopus is an automated workflow management tool that is scalable for virtual high-throughput screening (vHTS). It integrates MOPAC2016, MGLTools, PyMOL, and AutoDock Vina. In contrast to other platforms, Octopus can perform docking simulations of an unlimited number of compounds into a set of molecular targets. After generating the ligands in a drawing package in the Protein Data Bank (PDB) format, Octopus can carry out geometry refinement using the semi-empirical method PM7 implemented in MOPAC2016. Docking simulations can be performed using AutoDock Vina and can utilize the Our Own Molecular Targets (OOMT) databank...
January 2017: Journal of Molecular Modeling
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
#12
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/28062360/determination-of-glutathione-redox-potential-and-ph-value-in-subcellular-compartments-of-malaria-parasites
#13
Franziska Mohring, Mahsa Rahbari, Bernd Zechmann, Stefan Rahlfs, Jude M Przyborski, Andreas J Meyer, Katja Becker
The malaria parasite Plasmodium falciparum is exposed to multiple sources of oxidative challenge during its complex life cycle in the Anopheles vector and its human host. In order to further elucidate redox-based parasite host cell interactions and mechanisms of drug action, we targeted the genetically encoded glutathione redox sensor roGFP2 coupled to human glutaredoxin 1 (roGFP2-hGrx1) as well as the ratiometric pH sensor pHluorin to the apicoplast and the mitochondrion of P. falciparum. Using live cell imaging, this allowed for the first time the determination of the pH values of the apicoplast (7...
January 4, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28059970/artesunate-protects-against-the-organ-injury-and-dysfunction-induced-by-severe-hemorrhage-and-resuscitation
#14
Regina Sordi, Kiran K Nandra, Fausto Chiazza, Florence L Johnson, Claudia P Cabrera, Hew D Torrance, Noriaki Yamada, Nimesh S A Patel, Michael R Barnes, Karim Brohi, Massimo Collino, Christoph Thiemermann
OBJECTIVE: To evaluate the effects of artesunate on organ injury and dysfunction associated with hemorrhagic shock (HS) in the rat. BACKGROUND: HS is still a common cause of death in severely injured patients and is characterized by impairment of organ perfusion, systemic inflammatory response, and multiple organ failure. There is no specific therapy that reduces organ injury/dysfunction. Artesunate exhibits pharmacological actions beyond its antimalarial activity, such as anticancer, antiviral, and anti-inflammatory effects...
February 2017: Annals of Surgery
https://www.readbyqxmd.com/read/28056963/antimalarial-activity-of-syzygium-guineense-during-early-and-established-plasmodium-infection-in-rodent-models
#15
Solomon Asmamaw Tadesse, Zewdu Birhanu Wubneh
BACKGROUND: In Ethiopia, the leaves of Syzygium guineense have been found useful for the prevention and cure of malaria, and demonstrated antiplasmodial activity in vitro. Nevertheless, no scientific study has been conducted to confirm its antimalarial activity in vivo. Therefore, the objective of the study was to evaluate the antimalarial effect of Syzygium guineense leaf extract in mice. METHODS: Inoculation of the study mice was carried out by using the malaria parasite, Plasmodium berghei...
January 5, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28056938/hepatoprotective-effect-of-the-solvent-extracts-of-viola-canescens-wall-ex-roxb-against-ccl4-induced-toxicity-through-antioxidant-and-membrane-stabilizing-activity
#16
Abdullah, Mir Azam Khan, Waqar Ahmad, Manzoor Ahmad, Mohammad Nisar
BACKGROUND: Viola canescens Wall. ex. Roxb. exhibits analgesic, antimalarial and antispasmodic activities. It is used folklorically for the treatment of liver diseases, hypertension, malaria and cancer. The current study investigates phytochemical constituents, antioxidant and hepatoprotective activity of solvent extracts of whole plant of Viola canescens. METHODS: Phytochemicals, acute toxicity study and antioxidant activity of Viola canescens methanolic extract (VCME), ethyl acetate fraction (EAF), and partially purified EAF (90% EAF and combination of 80% EAF + 20% methanol fraction (EAF + Me) was carried out...
January 5, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28056932/in-vivo-antimalarial-activity-of-crude-extracts-and-solvent-fractions-of-leaves-of-strychnos-mitis-in-plasmodium-berghei-infected-mice
#17
Selamawit Fentahun, Eyasu Makonnen, Tesfaye Awas, Mirutse Giday
BACKGROUND: Malaria is a major public health problem in the world which is responsible for death of millions particularly in sub-Saharan Africa. Today, the control of malaria has become gradually more complex due to the spread of drug-resistant parasites. Medicinal plants are the unquestionable source of effective antimalarials. The present study aimed to evaluate antiplasmodial activity and acute toxicity of the plant Strychnos mitis in Plasmodium berghei infected mice. METHODS: Standard procedures were employed to investigate acute toxicity and 4-day suppressive effect of crude aqueous and hydro-methanolic extracts of the leaves of Strychnos mitis against P...
January 5, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28052200/structure-activity-relationship-of-the-antimalarial-ozonide-artefenomel-oz439
#18
Yuxiang Dong, Xiaofang Wang, Sriraghavan Kamaraj, Vivek J Bulbule, Francis C K Chiu, Jacques Chollet, Manickam Dhanasekaran, Christopher D Hein, Petros Papastogiannidis, Julia Morizzi, David M Shackleford, Helena Barker, Eileen Ryan, Christian Scheurer, Yuanqing Tang, Qingjie Zhao, Lin Zhou, Karen L White, Heinrich Urwyler, William N Charman, Hugues Matile, Sergio Wittlin, Susan A Charman, Jonathan L Vennerstrom
Building on insights gained from the discovery of the antimalarial ozonide arterolane (OZ277), we now describe the structure-activity relationship (SAR) of the antimalarial ozonide artefenomel (OZ439). Primary and secondary amino ozonides had higher metabolic stabilities than tertiary amino ozonides, consistent with their higher pKa and lower log D7.4 values. For primary amino ozonides, addition of polar functional groups decreased in vivo antimalarial efficacy. For secondary amino ozonides, additional functional groups had variable effects on metabolic stability and efficacy, but the most effective members of this series also had the highest log D7...
January 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28049347/strategies-to-enhance-biologically-active-secondary-metabolites-in-cell-cultures-of-artemisia-current-trends
#19
Mohammad Ali, Bilal Haider Abbasi, Nisar Ahmad, Haji Khan, Gul Shad Ali
The genus Artemisia has been utilized worldwide due to its immense potential for protection against various diseases, especially malaria. Artemisia absinthium, previously renowned for its utilization in the popular beverage absinthe, is gaining resurgence due to its extensive pharmacological activities. Like A. annua, this species exhibits strong biological activities like antimalarial, anticancer and antioxidant. Although artemisinin was found to be the major metabolite for its antimalarial effects, several flavonoids and terpenoids are considered to possess biological activities when used alone and also to synergistically boost the bioavailability of artemisinin...
January 3, 2017: Critical Reviews in Biotechnology
https://www.readbyqxmd.com/read/28042842/novel-2-3-dihydro-1h-pyrrolo-3-2-1-ij-quinazolin-1-ones-synthesis-and-biological-evaluation
#20
Malose J Mphahlele, Tebogo A Khoza, Peaceful Mabeta
Herein we describe the synthesis and evaluation of a series of novel 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones for in vitro cytotoxicity against three human cancer cell lines as well as for potential antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The title compounds were prepared via PdCl₂-mediated endo-dig cyclization of 2-aryl-8-(arylethynyl)-6-bromo-2,3-dihydroquinazolin-4(1H)-ones. The latter were prepared, in turn, via initial Sonogashira cross-coupling of 2-amino-5-bromo-3-iodobenzamide with aryl acetylenes followed by boric acid-mediated cyclocondensation of the intermediate 2-amino-3-(arylethynyl)-5-bromobenzamides with benzaldehyde derivatives...
December 30, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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