Synthesis and structure-activity relationship studies of novel anti-infectives for cross screening in tuberculosis and malaria disease models

Autor: Gessner, Richard Klaus

Includes abstract.
Includes bibliographical references (p. 205).
Some 12-16 hours after the invasion of the human erythrocyte by the malaria parasite Plasmodium falciparum, there appear in the erythrocyte membrane ‘new permeability pathwa

Externí odkaz: http://hdl.handle.net/11427/6308

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization

Autor: Soares de Melo, Candice, Feng, Tzu-Shean, van der Westhuyzen, Renier, Gessner, Richard K., Street, Leslie J., Morgans, Garreth L., Warner, Digby F., Moosa, Atica, Naran, Krupa, Lawrence, Nina, Boshoff, Helena I.M., Barry, Clifton E., III, Harris, C. John, Gordon, Richard, Chibale, Kelly

Publikováno v: In Bioorganic & Medicinal Chemistry 15 November 2015 23(22):7240-7250

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies

Autor: Wilson, Colin R, Gessner, Richard K, Moosa, Atica, Seldon, Ronnett, Warner, Digby F, Mizrahi, Valerie, Soares de Melo, Candice, Simelane, Sandile B, Nchinda, Aloysius, Abay, Efrem, Taylor, Dale, Njoroge, Mathew, Brunschwig, Christel, Lawrence, Nina, Boshoff, Helena I M, Barry, Clifton E, Sirgel, Frederick A, van Helden, Paul, Harris, C John, Gordon, Richard, Ghidelli-Disse, Sonja, Pflaumer, Hannah, Boesche, Markus, Drewes, Gerard, Sanz, Olalla, Santos, Gracia, Rebollo-Lopez, Maria José, Urones, Beatriz, Selenski, Carolyn, Lafuente-Monasterio, Maria Jose, Axtman, Matthew, Lelièvre, Joël, Ballell, Lluis, Mueller, Rudolf, Street, Leslie J, Ghorpade, Sandeep R, Chibale, Kelly

Publikováno v: Journal of Medicinal Chemistry
Repositorio Institucional de la Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid

A BioFocus DPI SoftFocus library of ∼35 000 compounds was screened against Mycobacterium tuberculosis (Mtb) in order to identify novel hits with antitubercular activity. The hits were evaluated in biology triage assays to exclude compounds suggeste

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::37b3fd45d5467f6c625df281433a5c7d
http://europepmc.org/articles/PMC5748279

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