keyword
MENU ▼
Read by QxMD icon Read
search

antimalarial activity

keyword
https://www.readbyqxmd.com/read/28327793/insights-into-cytochrome-bc1-complex-binding-mode-of-antimalarial-2-hydroxy-1-4-naphthoquinones-through-molecular-modelling
#1
Ana Carolina Rennó Sodero, Bárbara Abrahim-Vieira, Pedro Henrique Monteiro Torres, Pedro Geraldo Pascutti, Célia Rs Garcia, Vitor Francisco Ferreira, David Rodrigues da Rocha, Sabrina Baptista Ferreira, Floriano Paes Silva
BACKGROUND: Malaria persists as a major public health problem. Atovaquone is a drug that inhibits the respiratory chain of Plasmodium falciparum, but with serious limitations like known resistance, low bioavailability and high plasma protein binding. OBJECTIVES: The aim of this work was to perform molecular modelling studies of 2-hydroxy-1,4-naphthoquinones analogues of atovaquone on the Qo site of P. falciparum cytochrome bc1 complex (Pfbc1) to suggest structural modifications that could improve their antimalarial activity...
April 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28327785/ultrastructural-alterations-in-schistosoma-mansoni-juvenile-and-adult-male-worms-after-in-vitro-incubation-with-primaquine
#2
Reem Osama A Kamel, Fatma El-Zahraa Anwar Bayaumy
BACKGROUND: Praziquantel has been cited as the only drug for treating schistosomiasis. However, concerns over drug resistance have encouraged the search for novel drug leads. The antimalarial drug primaquine possesses interesting anti-schistosmal properties. OBJECTIVES: This study is the first to document the potential role of primaquine as a schistosomicide and the ultrastructural changes induced by primaquine on juvenile or adult male worms of Schistosoma mansoni...
April 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28322919/evaluation-of-preclinical-antimalarial-drugs-which-can-overcome-direct-acting-antivirals-resistant-hepatitis-c-viruses-using-the-viral-reporter-assay-systems
#3
Youki Ueda, Hiromichi Dansako, Shinya Satoh, Hye-Sook Kim, Yusuke Wataya, Hiroyuki Doi, Masanori Ikeda, Nobuyuki Kato
Persistent hepatitis C virus (HCV) infection causes chronic liver diseases and is a major global health problem. Recently developed treatments with direct-acting antivirals (DAAs) have largely improved the sustained virologic response rate of patients with chronic hepatitis C. However, this approach is still hindered by its great expense and the problem of drug resistance. Using our cell-based HCV assay systems, we reported that the preclinical antimalarial drugs N-89 and N-251 exhibited potent anti-HCV activities...
March 18, 2017: Virus Research
https://www.readbyqxmd.com/read/28321151/the-antimalarial-chloroquine-suppresses-lps-induced-nlrp3-inflammasome-activation-and-confers-protection-against-murine-endotoxic-shock
#4
Xiaoli Chen, Ning Wang, Yuanfeng Zhu, Yongling Lu, Xin Liu, Jiang Zheng
Activation of the NLRP3 inflammasome, which catalyzes maturation of proinflammatory cytokines like IL-1β and IL-18, is implicated and essentially involved in many kinds of inflammatory disorders. Chloroquine (CQ) is a traditional antimalarial drug and also possesses an anti-inflammatory property. In this study, we investigated whether CQ suppresses NLRP3 inflammasome activation and thereby confers protection against murine endotoxic shock. CQ attenuated NF-κB and MAPK activation and prohibited expression of IL-1β, IL-18, and Nlrp3 in LPS treated murine bone marrow-derived macrophages (BMDMs), demonstrating its inhibitory effect on the priming signal of NLRP3 activation...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28320254/antimalarial-and-antiplasmodial-activity-of-husk-extract-and-fractions-of-zea-mays
#5
Jude E Okokon, Bassey S Antia, Dinesh Mohanakrishnan, Dinkar Sahal
CONTEXT: Zea mays L. (Poacae) husk decoctions are traditionally used in the treatment of malaria by various tribes in Nigeria. OBJECTIVE: To assess the antimalarial and antiplasmodial potentials of the husk extract and fractions on malaria parasites using in vivo and in vitro models. MATERIALS AND METHODS: The ethanol husk extract and fractions (187-748 mg/kg, p.o.) of Zea mays were investigated for antimalarial activity against Plasmodium berghei using rodent (mice) malaria models and in vitro activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using the SRBR green assay method...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28319782/synthesis-and-antiplasmodial-activity-of-novel-indoleamide-derivatives-bearing-sulfonamide-and-triazole-pharmacophores
#6
N Devender, Sarika Gunjan, Renu Tripathi, Rama Pati Tripathi
Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28318947/docking-synthesis-and-antimalarial-activity-of-novel-4-anilinoquinoline-derivatives
#7
Shilpa Vijayaraghavan, Supriya Mahajan
A series of 4-anilinoquinoline triazine derivatives were designed, synthesized and screened for in vivo antimalarial activity against a chloroquine-sensitive strain of Plasmodium berghei. The compounds were further subjected to in vitro antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum and β-haematin inhibition studies. All the compounds exhibited in vivo antimalarial activity better than that shown by the standard drug, chloroquine. Twelve out of fifteen compounds showed better inhibition than that of chloroquine against chloroquine-resistant W2 strain of Plasmodium falciparum...
March 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28315598/n-piperonyl-substitution-on-aminoquinoline-pyrimidine-hybrids-effect-on-the-antiplasmodial-potency
#8
Rohit Kholiya, Shabana I Khan, Aparna Bahuguna, Mohit Tripathi, Diwan S Rawat
A series of 4-aminoquinoline-piperonyl-pyrimidine hybrids were synthesized with the aim of identifying compounds with enhanced antimalarial activity. All the synthesized molecules were evaluated in vitro against cultured Plasmodium falciparum W2 and D6 strains and exhibited potent antiplasmodial activities with IC50 values in the range of 0.02-5.16 μM. Out of the 22 synthesised hybrids, 12 were found to be better (up to eight-fold more active) than chloroquine (CQ), particularly against the CQ-resistant W2 strain of P...
March 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28302017/targeting-pyrimidine-pathway-of-plasmodium-knowlesi-new-strategies-towards-identification-of-novel-antimalarial-chemotherapeutic-agents
#9
Mayank Rashmi, Manoj Kumar Yadav, D Swati
Plasmodium knowlesi has been recently recognized as a human malarial parasite, particularly in the region of south-east Asia. The effective prevention and treatment of this disease is increasingly bound to fail due to the emergence of drug resistance. Hence, design of new drugs against known targets is gaining importance. Pyrimidine pathway is a crucial metabolic pathway in P. knowlesi, and the enzymes involved are also unique in terms of their structure and function as compared to its human counterpart. Thus targeting Dihydroorotase, an enzyme involved in the pyrimidine pathway, provides a promising route for novel drug development...
March 15, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28302011/the-pharmacological-mechanisms-and-therapeutic-activities-of-hydroxychloroquine-in-rheumatic-and-related-diseases
#10
Changfeng Hu, Lu Lu, Jie-Ping Wan, Chengping Wen
Hydroxychloroquine (HCQ) is known as one of the most fascinating synthetic antimalarial drugs during the last 50 years. It is currently among the most commonly employed medicines for the clinical treatment of rheumatic diseases, especially systemic lupus erythematosus and rheumatoid arthritis. In related mechanism studies, it has been found that HCQ possesses various immunomodulatory and anti-inflammatory activities. In addition, the effects of HCQ on anti-platelet, metabolic pathways, and antineoplasticity have also been disclosed in more recent studies...
March 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28291583/factors-predictive-of-high-disease-activity-early-in-the-course-of-sle-in-patients-from-a-latin-american-cohort
#11
Victor R Pimentel-Quiroz, Manuel F Ugarte-Gil, Guillermo J Pons-Estel, Enrique R Soriano, Verónica Saurit, Emilia I Sato, Lilian T Lavras Costallat, José Fernando Molina, Antonio Iglesias-Gamarra, Gil Reyes-Llerena, Oscar J Neira, Leonor A Barile, Luis H Silveira, María Ines Segami, Rosa Chacón-Díaz, Daniel Wojdyla, Graciela S Alarcón, Bernardo A Pons-Estel
AIMS: To determine the factors predictive of disease activity early in the course of SLE (baseline visit). METHODS: Patients from GLADEL, a multi-national, multi-ethnic, Latin-American lupus cohort were included. Disease activity was evaluated at baseline with the SLEDAI score. Demographic characteristics (age at diagnosis, gender, ethnicity, marital status, educational level, medical coverage and socioeconomic status) were assessed. Disease duration was defined as the time between the fourth ACR criterion and baseline...
February 2, 2017: Seminars in Arthritis and Rheumatism
https://www.readbyqxmd.com/read/28289029/antimalarial-hybrid-molecules-a-close-reality-or-a-distant-dream
#12
Drishti Agarwal, Rinkoo D Gupta, Satish K Awasthi
Emergence of drug resistant Plasmodium falciparum strains has led to a situation of haste in the scientific and pharmaceutical communities. Hence, all their efforts are redirected towards finding alternate chemotherapeutic agents that are capable of combating multi-drug resistant parasite strains. In the above light, scientists have come up with the concept of hybridisation of two or more active pharmacophores into a single chemical entity, resulting in 'antimalarial hybrids.' The approach has been applied widely for lead generation against deadly diseases such as cancer and AIDS, with proven potential to be used as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery...
March 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28285258/4-nitro-styrylquinoline-is-an-antimalarial-inhibiting-multiple-stages-of-plasmodium-falciparum-asexual-life-cycle
#13
Bracken F Roberts, Yongsheng Zheng, Jacob Cleaveleand, Sukjun Lee, Eunyoung Lee, Lawrence Ayong, Yu Yuan, Debopam Chakrabarti
Drugs against malaria are losing their effectiveness because of emerging drug resistance. This underscores the need for novel therapeutic options for malaria with mechanism of actions distinct from current antimalarials. To identify novel pharmacophores against malaria we have screened compounds containing structural features of natural products that are pharmacologically relevant. This screening has identified a 4-nitro styrylquinoline (SQ) compound with submicromolar antiplasmodial activity and excellent selectivity...
February 21, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28284429/pharmacology-of-mangostins-and-their-derivatives-a-comprehensive-review
#14
REVIEW
Ming-Hui Wang, Kuo-Jun Zhang, Qin-Lan Gu, Xiao-Ling Bi, Jin-Xin Wang
Mangosteen (Garcinia mangostana Linn.) is a well-known tropical tree indigenous to Southeast Asia. Its fruit's pericarp abounds with a class of isoprenylated xanthones which are referred as mangostins. Numerous in vitro and in vivo studies have shown that mangostins and their derivatives possess diverse pharmacological activities, such as antibacterial, antifungal, antimalarial, anticarcinogenic, antiatherogenic activities as well as neuroprotective properties in Alzheimer's disease (AD). This review article provides a comprehensive review of the pharmacological activities of mangostins and their derivatives to reveal their promising utilities in the treatment of certain important diseases, mainly focusing on the discussions of the underlying molecular targets/pathways, modes of action, and relevant structure-activity relationships (SARs)...
February 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28279189/therapeutic-strategies-of-drug-repositioning-targeting-autophagy-to-induce-cancer-cell-death-from-pathophysiology-to-treatment
#15
REVIEW
Go J Yoshida
The 2016 Nobel Prize in Physiology or Medicine was awarded to the researcher that discovered autophagy, which is an evolutionally conserved catabolic process which degrades cytoplasmic constituents and organelles in the lysosome. Autophagy plays a crucial role in both normal tissue homeostasis and tumor development and is necessary for cancer cells to adapt efficiently to an unfavorable tumor microenvironment characterized by hypo-nutrient conditions. This protein degradation process leads to amino acid recycling, which provides sufficient amino acid substrates for cellular survival and proliferation...
March 9, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28274284/the-antimalarial-action-of-fk506-and-rapamycin-evidence-for-a-direct-effect-on-fk506-binding-protein-pffkbp35
#16
Paul Monaghan, Darren B Leneghan, Wesley Shaw, Angus Bell
FK506 and rapamycin (Rap) are immunosuppressive drugs that act principally on T-lymphocytes. The receptors for both drugs are FK506-binding proteins (FKBPs), but the molecular mechanisms of immunosuppression differ. An FK506-FKBP complex inhibits the protein phosphatase calcineurin, blocking a key step in T-cell activation, while the Rap -FKBP complex binds to the protein kinase target of rapamycin (TOR), which is involved in a subsequent signalling pathway. Both drugs, and certain non-immunosuppressive compounds related to FK506, have potent antimalarial activity...
March 9, 2017: Parasitology
https://www.readbyqxmd.com/read/28273638/antimalarial-activity-and-safety-assessment-of-flueggea-virosa-leaves-and-its-major-constituent-with-special-emphasis-on-their-mode-of-action
#17
Shiv Vardan Singh, Ashan Manhas, Yogesh Kumar, Sonali Mishra, Karuna Shanker, Feroz Khan, Kumkum Srivastava, Anirban Pal
A clinical emergency stands due to the appearance of drug resistant Plasmodium strains necessitate novel and effective antimalarial chemotypes, where plants seem as the prime option, especially after the discovery of quinine and artemisinin. The present study was aimed towards bioprospecting leaves of Flueggea virosa for its antimalarial efficacy and active principles. Crude hydro-ethanolic extract along with solvent derived fractions were tested in vitro against Plasmodium falciparum CQ sensitive (3D7) and resistant (K1) strains, where all the fractions exhibited potential activity (IC50 values <10μg/mL) against both the strains...
March 5, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28263085/exploration-of-thiaheterocyclic-hhdac6-inhibitors-as-potential-antiplasmodial-agents
#18
Rob De Vreese, Carmen de Kock, Peter J Smith, Kelly Chibale, Matthias D'hooghe
AIM: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan-histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoform-selective HDACis. RESULTS: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28262680/a-potent-antimalarial-benzoxaborole-targets-a-plasmodium-falciparum-cleavage-and-polyadenylation-specificity-factor-homologue
#19
Ebere Sonoiki, Caroline L Ng, Marcus C S Lee, Denghui Guo, Yong-Kang Zhang, Yasheen Zhou, M R K Alley, Vida Ahyong, Laura M Sanz, Maria Jose Lafuente-Monasterio, Chen Dong, Patrick G Schupp, Jiri Gut, Jenny Legac, Roland A Cooper, Francisco-Javier Gamo, Joseph DeRisi, Yvonne R Freund, David A Fidock, Philip J Rosenthal
Benzoxaboroles are effective against bacterial, fungal and protozoan pathogens. We report potent activity of the benzoxaborole AN3661 against Plasmodium falciparum laboratory-adapted strains (mean IC50 32 nM), Ugandan field isolates (mean ex vivo IC50 64 nM), and murine P. berghei and P. falciparum infections (day 4 ED90 0.34 and 0.57 mg kg(-1), respectively). Multiple P. falciparum lines selected in vitro for resistance to AN3661 harboured point mutations in pfcpsf3, which encodes a homologue of mammalian cleavage and polyadenylation specificity factor subunit 3 (CPSF-73 or CPSF3)...
March 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/28261884/modulation-of-antimalarial-activity-at-a-putative-bisquinoline-receptor-in-vivo-using-fluorinated-bisquinolines
#20
Alistar John Fielding, Valentina Lukinovic, Philip Evans, Said Alizadeh, Roger Bisby, Mike Drew, Alessio Del Casino, James Dunn, Laura Randle, Nicola Dempster, Nahar Lutfun, Sarker Satyajit, Fabián G Cantú Reinhard, Sam P de Visser, Mike Dascombe, Fyaz Ismail
Antimalarials can interact with heme covalently, by - interactions or hydrogen bonding. Consequently, the prototropy of 4-aminoquinolines and quinoline methanols was investigated using quantum mechanics. Calculations showed mefloquine protonated preferentially at the piperidine and was impeded at the endocyclic nitrogen due to electronic rather than steric factors. In gas phase calculations, 7-substituted mono- and bis-4-aminoquinolines were preferentially protonated at the endocyclic quinoline nitrogen...
March 6, 2017: Chemistry: a European Journal
keyword
keyword
43150
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"