نتایج جستجو برای: antimalarial compounds

تعداد نتایج: 232060  

Journal: :The Journal of organic chemistry 2015
Christopher J Schulze Gabriel Navarro Daniel Ebert Joseph DeRisi Roger G Linington

Despite significant advances in antimalarial chemotherapy over the past 30 years, development of resistance to frontline drugs remains a significant challenge that limits efforts to eradicate the disease. We now report the discovery of a new class of antimalarials, salinipostins A-K, with low nanomolar potencies and high selectivity indices against mammalian cells (salinipostin A: Plasmodium fa...

Journal: :Antimicrobial agents and chemotherapy 1972
C C Smith C S Genther

Series of strains of Streptococcus faecium ATCC 8043, Lactobacillus casei ATCC 7469, and Pediococcus cerevisiae ATCC 8081 with increasing resistance to the active antifolate antimalarial drugs chlorguanide triazine (CGT), pyrimethamine (PM), and trimethoprim (TMP) were isolated. These mutant strains, stable for at least 3 to 5 years, were examined for cross-resistance and collateral susceptibil...

Afiat Berbudi, Anas Subarnas Maulana Alkandahri, Novi Vicahyani Utami Utami

Objective: One of the biggest health problems in the world, which occurs in more than 90 countries, is the spread of malaria. Cep-cepan leaves (Castanopsis  costata), was empirically used as an antimalarial herb in North Sumatra. Since its use has not been scientifically studied, we investigated the antimalarial activity of extract and fractions of C. costata ...

Journal: :Memorias do Instituto Oswaldo Cruz 2007
Valter F de Andrade-Neto Adrian M Pohlit Ana Cristina S Pinto Ellen Cristina C Silva Karla L Nogueira Márcia R S Melo Marycleuma C Henrique Rodrigo C N Amorim Luis Francisco R Silva Mônica R F Costa Rita C S Nunomura Sergio M Nunomura Wilson D Alecrim M das Graças C Alecrim F Célio M Chaves Pedro Paulo R Vieira

In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhib...

Journal: :ACS medicinal chemistry letters 2014
Daniela Miranda Rita Capela Inês S Albuquerque Patrícia Meireles Isa Paiva Fátima Nogueira Richard Amewu Jiri Gut Philip J Rosenthal Rudi Oliveira Maria M Mota Rui Moreira Francesc Marti Miguel Prudêncio Paul M O'Neill Francisca Lopes

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. These hybrid compounds showed...

2013
María Belén Jiménez-Díaz Sara Viera Javier Ibáñez Teresa Mulet Noemí Magán-Marchal Helen Garuti Vanessa Gómez Lorena Cortés-Gil Antonio Martínez Santiago Ferrer María Teresa Fraile Félix Calderón Esther Fernández Leonard D. Shultz Didier Leroy David M. Wilson José Francisco García-Bustos Francisco Javier Gamo Iñigo Angulo-Barturen

The emergence of resistance to available antimalarials requires the urgent development of new medicines. The recent disclosure of several thousand compounds active in vitro against the erythrocyte stage of Plasmodium falciparum has been a major breakthrough, though converting these hits into new medicines challenges current strategies. A new in vivo screening concept was evaluated as a strategy...

2016
Madhulata Kumari Neeraj Tiwari Naidu Subbarao Subhash Chandra

Malaria is a mosquito-borne lifethreatening disease. Though it is treatable but due to emerging resistance against well-known drugs like 8aminoquinolines and artemisinin analogs, it is urgent need to develop novel drugs for the treatment of malaria. In order to develop a new drug, imidazolopiperazine derivatives have been shown antimalarial efficacy against wild-type as well as drug resistant m...

Journal: :Molecules 2013
Cleydson Breno R Santos Josinete B Vieira Cleison C Lobato Lorane I S Hage-Melim Raimundo N P Souto Clarissa S Lima Elizabeth V M Costa Davi S B Brasil Williams Jorge C Macêdo José Carlos T Carvalho

The Hartree-Fock method and the 6-31G** basis set were employed to calculate the molecular properties of artemisinin and 20 derivatives with antimalarial activity. Maps of molecular electrostatic potential (MEPs) and molecular docking were used to investigate the interaction between ligands and the receptor (heme). Principal component analysis and hierarchical cluster analysis were employed to ...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 1997
P K Rathod T McErlean P C Lee

Continual exposure of malarial parasite populations to different drugs may have selected not only for resistance to individual drugs but also for genetic traits that favor initiation of resistance to novel unrelated antimalarials. To test this hypothesis, different Plasmodium falciparum clones having varying numbers of preexisting resistance mechanisms were treated with two new antimalarial age...

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