ArticleEuropean journal of medicinal chemistry2018
Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.
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Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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19 citing papers in PubMed.
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- Gametocyte-specific and all-blood-stage transmission-blocking chemotypes discovered from high throughput screening on Plasmodium falciparum gametocytes.Communications biology · 2022Article
- Adapt or Die: Targeting Unique Transmission-Stage Biology for Malaria Elimination.Frontiers in cellular and infection microbiology · 2022Review
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Authors and funding
20 authors.
Alessandra ValloneDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Sarah D'AlessandroEuropean Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy; Dipartimento di Scienze Biomediche, Chirurgiche e Odontoiatriche, Università di Milano, Via Pascal 36, 20133, Milan, Italy.
Simone BrogiDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Margherita BrindisiDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Giulia ChemiDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Gloria AlfanoDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Stefania LamponiDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Soon Goo LeeDepartment of Biology, Washington University in St. Louis, St. Louis, MO, 63130, United States.
Joseph M JezDepartment of Biology, Washington University in St. Louis, St. Louis, MO, 63130, United States.
Karin J M KoolenTropIQ Health Sciences, Transistorweg 5-C02, 6534 AT, Nijmegen, The Netherlands.
Koen J DecheringTropIQ Health Sciences, Transistorweg 5-C02, 6534 AT, Nijmegen, The Netherlands.
Simona SaponaraDepartment of Life Sciences, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Fabio FusiDepartment of Life Sciences, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Beatrice GorelliDepartment of Life Sciences, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.
Donatella TaramelliEuropean Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy; Dipartimento di Scienze Farmacologiche e Biomolecolari, Università di Milano, Via Pascal 36, 20133, Milan, Italy.
Silvia ParapiniEuropean Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy; Dipartimento di Scienze Farmacologiche e Biomolecolari, Università di Milano, Via Pascal 36, 20133, Milan, Italy.
Reto CaldelariInstitute of Cell Biology, University of Bern, Baltzerstrasse 4, 3012, Bern, Switzerland.
Giuseppe CampianiDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy. Electronic address: campiani@unisi.it.
Sandra GemmaDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy. Electronic address: gemma@unisi.it.
Stefania ButiniDepartment of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.
Funding
STRUCTURE AND FUNCTION OF PHOSPHOETHANOLAMINE METHYLTRANSFERASES: NEW ANTI-PARASR01AI097119 · NIAID · WASHINGTON UNIVERSITY · PI JEZ, JOSEPH MARTIN · 2012 to 2015
$998kNIAID NIH HHS R01 AI097119
Abstract
Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for implementing malaria elimination strategies. MMV019918 (1, 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine) was selected from the MMV Malaria Box for its dual activity against both asexual stages and gametocytes. In-depth structure-activity relationship studies and cytotoxicity evaluation led to the selection of 25 for further biological investigation. The potential transmission blocking activity of 25 versus P. falciparum was confirmed through the standard membrane-feeding assay. Both 1 and 25 significantly prolonged atrioventricular conduction time in Langendorff-isolated rat hearts, and showed inhibitory activity of Ba
Indexed as
AntimalarialsDose-Response Relationship, DrugEnzyme InhibitorsFuransLife Cycle StagesMalaria, FalciparumMethyltransferasesMolecular StructureParasitic Sensitivity TestsPiperidinesPlasmodium falciparumStructure-Activity Relationship1-(5-(4-bromo-2-chlorophenyl)furan-2-yl)-N-((piperidin-4-yl)methyl)methanamineAntimalarialsEnzyme InhibitorsFuransMethyltransferasesphosphoethanolamine methyltransferasePiperidinesGametocytesInhibitionMalariaPlasmodium falciparumStructure-activity relationships
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