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https://www.readbyqxmd.com/read/28231522/novel-2-3-disubstituted-quinazoline-4-3h-one-molecules-derived-from-amino-acid-linked-sulphonamide-as-a-potent-malarial-antifolates-for-dhfr-inhibition
#1
Tarosh S Patel, Satish F Vanparia, Urmila H Patel, Ritu B Dixit, Chaitanya J Chudasama, Bhavesh D Patel, Bharat C Dixit
An optimization of a modified Grimmel's method for N-heterocyclization of Leucine linked sulphonamide leading to 2,3-disustituted-4-quinazolin-(3H)-ones was accomplished. Further, nineteen hybrid quinazolinone motifs (5a-5s) were synthesized by N-heterocyclization reaction under microwave irradiation using TEAA (IL) as green solvent as well as catalyst. The in vitro screening of the hybrid entities against the plasmodium species P. falciparum yielded five antimalarial potent molecules 5g, 5l, 5m, 5n &5p owing comparable activity to the reference drugs...
February 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230749/design-of-drug-delivery-systems-containing-artemisinin-and-its-derivatives
#2
REVIEW
Blessing Atim Aderibigbe
Artemisinin and its derivatives have been reported to be experimentally effective for the treatment of highly aggressive cancers without developing drug resistance, they are useful for the treatment of malaria, other protozoal infections and they exhibit antiviral activity. However, they are limited pharmacologically by their poor bioavailability, short half-life in vivo, poor water solubility and long term usage results in toxicity. They are also expensive for the treatment of malaria when compared to other antimalarials...
February 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28222659/antimalarial-solid-self-emulsifying-system-for-oral-use-in-vitro-investigation
#3
Sameer Bhandari, Vikas Rana, Ashok K Tiwary
AIM: The low aqueous solubility of artemether and lumefantrine makes them less bioavailable. It is expected that by formulating self-microemulsifying drug-delivery systems (SMEDDS), their aqueous solubility and absorption will thus be enhanced. Results & methodology: Optimized liquid SMEDDS containing artemether and lumefantrine was adsorbed on Neusilin US2(®) employing spray drying technique to convert it into solid SMEDDS. Almost 90% of both drugs were released within 15 min in their respective official dissolution media...
April 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28220535/interaction-of-approved-drugs-with-synaptic-vesicle-protein-2a
#4
Azeem Danish, Vigneshwaran Namasivayam, Anke C Schiedel, Christa E Müller
Levetiracetam (LEV) and its recently approved derivative brivaracetam are anti-epileptic drugs with a unique mechanism of action. The synaptic vesicle protein 2A (SV2A) was previously identified as their main target. In the current study, we tested a collection of 500 approved drugs for interaction with the human SV2A protein expressed in Chinese hamster ovary cells. Competition binding studies were performed using cell lysates with high SV2A expression and [(3) H]brivaracetam as a radioligand. A hit rate of 3% was obtained, defined as compounds that inhibited radioligand binding by more than 90% at a screening concentration of 20 μM...
February 21, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28219993/low-prevalence-of-substandard-and-falsified-antimalarial-and-antibiotic-medicines-in-public-and-faith-based-health-facilities-of-southern-malawi
#5
Felix Khuluza, Stephen Kigera, Lutz Heide
Substandard and falsified antimalarial and antibiotic medicines represent a serious problem for public health, especially in low- and middle-income countries. However, information on the prevalence of poor-quality medicines is limited. In the present study, samples of six antimalarial and six antibiotic medicines were collected from 31 health facilities and drug outlets in southern Malawi. Random sampling was used in the selection of health facilities. For sample collection, an overt approach was used in licensed facilities, and a mystery shopper approach in nonlicensed outlets...
February 20, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28207169/design-synthesis-and-biological-evaluation-of-novel-1-2-4-trioxanes-as-potential-antimalarial-agents
#6
Amit K Gupta, Kanika Varshney, Vivek Kumar, Kumkum Srivastava, Aditya B Pant, Sunil K Puri, Anil K Saxena
A series of substituted 1,2,4-trioxanes were synthesized and evaluated for their antimalarial potential, in silico ADME properties and cytotoxicity on neuronal cell lines. Among the 15 synthesized substituted 1,2,4-trioxanes, two compounds (compound 15, IC50  = 25.71 nM; compound 21, IC50  = 19.6 nM) exhibited promising in vitro antimalarial potential comparable to those of the existing drugs chloroquine and artemisinin. Both of these compounds were found to be nontoxic up to 20 µM concentration in neuronal PC-12 cells...
February 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28199305/sterile-protection-against-human-malaria-by-chemoattenuated-pfspz-vaccine
#7
Benjamin Mordmüller, Güzin Surat, Heimo Lagler, Sumana Chakravarty, Andrew S Ishizuka, Albert Lalremruata, Markus Gmeiner, Joseph J Campo, Meral Esen, Adam J Ruben, Jana Held, Carlos Lamsfus Calle, Juliana B Mengue, Tamirat Gebru, Javier Ibáñez, Mihály Sulyok, Eric R James, Peter F Billingsley, K C Natasha, Anita Manoj, Tooba Murshedkar, Anusha Gunasekera, Abraham G Eappen, Tao Li, Richard E Stafford, Minglin Li, Phil L Felgner, Robert A Seder, Thomas L Richie, B Kim Lee Sim, Stephen L Hoffman, Peter G Kremsner
A highly protective malaria vaccine would greatly facilitate the prevention and elimination of malaria and containment of drug-resistant parasites. A high level (more than 90%) of protection against malaria in humans has previously been achieved only by immunization with radiation-attenuated Plasmodium falciparum (Pf) sporozoites (PfSPZ) inoculated by mosquitoes; by intravenous injection of aseptic, purified, radiation-attenuated, cryopreserved PfSPZ ('PfSPZ Vaccine'); or by infectious PfSPZ inoculated by mosquitoes to volunteers taking chloroquine or mefloquine (chemoprophylaxis with sporozoites)...
February 15, 2017: Nature
https://www.readbyqxmd.com/read/28193656/within-host-selection-of-drug-resistance-in-a-mouse-model-reveals-dose-dependent-selection-of-atovaquone-resistance-mutations
#8
Suci Nuralitha, Lydia S Murdiyarso, Josephine E Siregar, Din Syafruddin, Jessica Roelands, Jan Verhoef, Andy I M Hoepelman, Sangkot Marzuki
The evolutionary selection of malaria parasites within individual host plays a critical role in the emergence of drug resistance. We have compared the selection of atovaquone resistance mutant in mouse models reflecting two different causes of failure in malaria treatment, inadequate sub-therapeutic dose and incomplete therapeutic dose.The two models are based on cycles of insufficient treatment of P. berghei-infected mice: repeated inadequate treatment associated with sub-therapeutic dose (0.1 mg Kg(-1) BW; RIaT) and repeated incomplete treatment with therapeutic dose (14...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28193646/simplified-reversed-chloroquines-to-overcome-malaria-resistance-to-quinoline-based-drugs
#9
Bornface Gunsaru, Steven J Burgess, Westin Morrill, Jane X Kelly, Shawheen Shomloo, Martin J Smilkstein, Katherine Liebmann, David H Peyton
Building on our earlier work of attaching a chemosensitizer (reversal agent) to a known drug pharmacophore, we have now expanded the structure-activity relationship study to include simplified versions of the chemosensitizer. The change from two aromatic rings in this head group to a single ring, in fact, does not appear to detrimentally affect the antimalarial activity of the compounds. Data from in vitro heme binding and β-hematin inhibition assays suggest that the single aromatic RCQ compounds retain similar activities against P...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28192202/ethnomedicinal-uses-of-plants-for-the-treatment-of-malaria-in-soon-valley-khushab-pakistan
#10
Amin Shah, Sarvat Rahim
ETHNOPHARMACOLOGICAL RELEVANCE: To best of our knowledge this is the first quantitative ethno-medicinal study with the aim of documenting the indigenous knowledge and practices of using plants for malarial therapy in Soon Valley, Khushab, Pakistan. In this Valley, malaria is among the major public health problems but, until now, the population still mostly relies on herbal medicine for treatment. MATERIALS AND METHODS: Ethno-medicinal data were documented from 63 informants by using semi-structured questionnaires and interviewing the informants about their knowledge of plants regarding malaria and related symptoms...
February 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28183182/a-redox-active-fluorescent-ph-indicator-for-detecting-plasmodium-falciparum-strains-with-reduced-responsiveness-to-quinoline-antimalarial-drugs
#11
Mouhamad Jida, Cecilia P Sanchez, Karène Urgin, Katharina Ehrhardt, Saravanan Mounien, Aurelia Geyer, Mourad Elhabiri, Michael Lanzer, Elisabeth Davioud-Charvet
Mutational changes in the Plasmodium falciparum chloroquine resistance transporter (PfCRT) have been associated with differential responses to a wide spectrum of biologically active compounds including current and former quinoline and quinoline-like antimalarial drugs. PfCRT confers altered drug responsiveness by acting as a transport system, expelling drugs from the parasite's digestive vacuole where these drugs exert, at least part of, their antiplasmodial activity. To preserve the efficacy of these invaluable drugs, novel functional tools are required for epidemiological surveys of parasite strains carrying mutant PfCRT variants and for drug development programs aimed at inhibiting or circumventing the action of PfCRT...
February 10, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28181705/pyrrolidine-containing-bisphosphonates-as-potential-anti-resorption-bone-drugs
#12
Lorena De Luca, Andrea Chiminazzo, Laura Sperni, Giorgio Strukul, Alessandro Scarso
Bisphosphonates, particularly those with N-substituted groups, are currently the most popular drugs for the treatment of osteoporosis. However, their chemical structures are still rather simple and new synthetic methods are needed to expand their molecular complexity and also improve their specificity of action towards other targets as anticancer, antibacterial, and antimalarial drugs. Herein, we report a new class of potential antiresorption bisphosphonate drugs that have a pyrrolidine unit with different substituents, obtained through a simple dipolar cycloaddition reaction between azomethine ylides and vinylidenebisphosphonate derivatives as precursors...
January 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28178878/disease-characterization-of-systemic-lupus-erythematosus-sle-patients-in-quebec
#13
R Ng, S Bernatsky, E Rahme
Objective Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by an array of organ manifestations that can appear during flares and disappear during remissions. The objectives of this study were: (i) to examine SLE manifestation groups longitudinally in an SLE cohort; and (ii) to assess the association between early antimalarial treatment and renal manifestations. Methods Seven SLE manifestation groups-cutaneous, hematologic, lung, musculoskeletal, neuropsychiatric, serositis, renal-were tracked using Kaplan-Meier survival curves in an incident SLE cohort from Quebec health administrative data ( n = 2010)...
January 1, 2017: Lupus
https://www.readbyqxmd.com/read/28178358/substrate-analogous-inhibitors-exert-antimalarial-action-by-targeting-the-plasmodium-lactate-transporter-pffnt-at-nanomolar-scale
#14
André Golldack, Björn Henke, Bärbel Bergmann, Marie Wiechert, Holger Erler, Alexandra Blancke Soares, Tobias Spielmann, Eric Beitz
Resistance against all available antimalarial drugs calls for novel compounds that hit unexploited targets in the parasite. Here, we show that the recently discovered Plasmodium falciparum lactate/proton symporter, PfFNT, is a valid druggable target, and describe a new class of fluoroalkyl vinylogous acids that potently block PfFNT and kill cultured parasites. The original compound, MMV007839, is derived from the malaria box collection of potent antimalarials with unknown targets and contains a unique internal prodrug principle that reversibly switches between a lipophilic transport form and a polar, substrate-analogous active form...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28176804/griseofulvin-impairs-intraerythrocytic-growth-of-plasmodium-falciparum-through-ferrochelatase-inhibition-but-lacks-activity-in-an-experimental-human-infection-study
#15
Clare M Smith, Ante Jerkovic, Thy Thuc Truong, Simon J Foote, James S McCarthy, Brendan J McMorran
Griseofulvin, an orally active antifungal drug used to treat dermatophyte infections, has a secondary effect of inducing cytochrome P450-mediated production of N-methyl protoporphyrin IX (N-MPP). N-MPP is a potent competitive inhibitor of the heme biosynthetic-enzyme ferrochelatase, and inhibits the growth of cultured erythrocyte stage Plasmodium falciparum. Novel drugs against Plasmodium are needed to achieve malaria elimination. Thus, we investigated whether griseofulvin shows anti-plasmodial activity. We observed that the intraerythrocytic growth of P...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28173854/anti-influenza-virus-activity-of-extracts-from-the-stems-of-jatropha-multifida-linn-collected-in-myanmar
#16
Masaki Shoji, So-Yeun Woo, Aki Masuda, Nwet Nwet Win, Hla Ngwe, Etsuhisa Takahashi, Hiroshi Kido, Hiroyuki Morita, Takuya Ito, Takashi Kuzuhara
BACKGROUND: To contribute to the development of novel anti-influenza drugs, we investigated the anti-influenza activity of crude extracts from 118 medicinal plants collected in Myanmar. We discovered that extract from the stems of Jatropha multifida Linn. showed anti-influenza activity. J. multifida has been used in traditional medicine for the treatment of various diseases, and the stem has been reported to possess antimicrobial, antimalarial, and antitumor activities. However, the anti-influenza activity of this extract has not yet been investigated...
February 7, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28171830/a-review-on-antioxidant-potential-of-bioactive-heterocycle-benzofuran-natural-and-synthetic-derivatives
#17
REVIEW
Karam Chand, Rajeshwari, Asha Hiremathad, Mahak Singh, M Amelia Santos, Rangappa S Keri
The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. In this context, oxygen heterocycles exhibit diverse biological and pharmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Among oxygen containing heterocycles, benzofuran (synthetic and natural isolated) and its derivatives have attracted medicinal chemists and pharmacologists due to their pronounced biological activities and their potential applications as pharmacological agents such as antioxidant, antitumor, antiplatelet, antimalarial, antiinflammatory, antidepressant and anticonvulsant properties...
November 18, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28167052/heme-binding-activity-of-methoxyflavones-from-pentzia-monodiana-maire-asteraceae
#18
Sergio Ortiz, Kamel Dali-Yahia, Pedro Vasquez-Ocmin, Raphaël Grougnet, Philippe Grellier, Sylvie Michel, Alexandre Maciuk, Sabrina Boutefnouchet
A heme-binding assay based on mass spectrometry was performed on P. monodiana Maire (Asteraceae) extracts to identify metabolites able to form adducts with heminic part of haemoglobin, as potential antimalarial drugs. Main adducts were characterized and their stability was measured. Isolation of main constituents of P. monodiana Maire lead to identification of the two methoxyflavones 3'-O-methyleupatorin (7) and artemetin (8) involved in the adducts formation. Four seco-tanapartholides (1-4), a guaianolide (5), a germacranolide (6) and two other methoxyflavones (9, 10) were also characterized...
February 3, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28166813/hidden-reservoir-of-resistant-parasites-the-missing-link-in-the-elimination-of-falciparum-malaria
#19
Rashad Abdul-Ghani, Mohammed A K Mahdy, John C Beier, Leonardo K Basco
BACKGROUND: To successfully eliminate malaria, an integrated system that includes a number of approaches and interventions-aimed at overcoming the threat of antimalarial drug resistance-is required. Significant progress has been made in reducing malaria incidence through large-scale use of artemisinin-based combination therapies and insecticide-treated nets. To consolidate these gains, attention should be paid to the missing links in the elimination of malaria. One of these gaps is the residual reservoir of submicroscopic resistant parasites, which remains after case management or other control measures have been carried out...
February 6, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/28163958/a-prospective-comparative-field-study-to-evaluate-the-efficacy-of-a-traditional-plant-based-malaria-prophylaxis
#20
Prakash Bangalore Nagendrappa, Pradeep Annamalai, Muruli Naik, Vinay Mahajan, Ashwini Mathur, Ghosh Susanta, Frederick Gay, Padma Venkatasubramanian
BACKGROUND: An unceasing threat of resistance of malarial parasites to available antimalarial drugs makes the development of new drugs imperative. Natural plant-based products are an alternative source for discovering new antimalarial drugs. AIM: To determine the prophylactic efficacy of a traditionally used plant-based drug on prevention of malaria in endemic villages of Odisha, India. METHODS: A total of 267 healthy human volunteers of both sexes, aged 18-60 years were enrolled in Odisha, India, to receive either minimum 20 doses of aqueous extract of Traditional Plant-based Malaria Prophylactic drug 74, twice a week (experimental group), or no drug (control group) for 14 weeks...
January 2017: Journal of Intercultural Ethnopharmacology
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