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dc.contributor.authorNorcross, Neil R
dc.contributor.authorWilson, Caroline
dc.contributor.authorBaragana, Beatriz
dc.contributor.authorHallyburton, Irene
dc.contributor.authorOsuna-Cabello, Maria
dc.contributor.authorNorval, Suzanne
dc.contributor.authorRiley, Jennifer
dc.contributor.authorFletcher, Daniel
dc.contributor.authorSinden, Robert
dc.contributor.authorDelves, Michael
dc.contributor.authorRuecker, Andrea
dc.contributor.authorDuffy, Sandra
dc.contributor.authorMeister, Stephan
dc.contributor.authorAntonova-Koch, Yevgeniya
dc.contributor.authorCrespo, Benigno
dc.contributor.authorde Cozar, Cristina
dc.contributor.authorSanz, Laura M
dc.contributor.authorJavier Gamo, Francisco
dc.contributor.authorAvery, Vicky M
dc.contributor.authorFrearson, Julie A
dc.contributor.authorGray, David W
dc.contributor.authorFairlamb, Alan H
dc.contributor.authorWinzeler, Elizabeth A
dc.contributor.authorWaterson, David
dc.contributor.authorCampbell, Simon F
dc.contributor.authorWillis, Paul A
dc.contributor.authorRead, Kevin D
dc.contributor.authorGilbert, Ian H
dc.date.accessioned2020-06-26T03:30:19Z
dc.date.available2020-06-26T03:30:19Z
dc.date.issued2019
dc.identifier.issn1860-7179
dc.identifier.doi10.1002/cmdc.201900329
dc.identifier.urihttp://hdl.handle.net/10072/394950
dc.description.abstractHerein we describe the optimization of a phenotypic hit against Plasmodium falciparum based on an aminoacetamide scaffold. This led to N ‐(3‐chloro‐4‐fluorophenyl)‐2‐methyl‐2‐{[4‐methyl‐3‐(morpholinosulfonyl)phenyl]amino}propanamide (compound 28 ) with low‐nanomolar activity against the intraerythrocytic stages of the malaria parasite, and which was found to be inactive in a mammalian cell counter‐screen up to 25 μm . Inhibition of gametes in the dual gamete activation assay suggests that this family of compounds may also have transmission blocking capabilities. Whilst we were unable to optimize the aqueous solubility and microsomal stability to a point at which the aminoacetamides would be suitable for in vivo pharmacokinetic and efficacy studies, compound 28 displayed excellent antimalarial potency and selectivity; it could therefore serve as a suitable chemical tool for drug target identification.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherWiley
dc.relation.ispartofpagefrom1329
dc.relation.ispartofpageto1335
dc.relation.ispartofissue14
dc.relation.ispartofjournalChemMedChem
dc.relation.ispartofvolume14
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.subject.keywordsScience & Technology
dc.subject.keywordsLife Sciences & Biomedicine
dc.subject.keywordsChemistry, Medicinal
dc.subject.keywordsPharmacology & Pharmacy
dc.subject.keywordsaminoacetamides
dc.titleSubstituted Aminoacetamides as Novel Leads for Malaria Treatment
dc.typeJournal article
dc.type.descriptionC1 - Articles
dcterms.bibliographicCitationNorcross, NR; Wilson, C; Baragana, B; Hallyburton, I; Osuna-Cabello, M; Norval, S; Riley, J; Fletcher, D; Sinden, R; Delves, M; Ruecker, A; Duffy, S; Meister, S; Antonova-Koch, Y; Crespo, B; de Cozar, C; Sanz, LM; Javier Gamo, F; Avery, VM; Frearson, JA; Gray, DW; Fairlamb, AH; Winzeler, EA; Waterson, D; Campbell, SF; Willis, PA; Read, KD; Gilbert, IH, Substituted Aminoacetamides as Novel Leads for Malaria Treatment, ChemMedChem, 2019, 14 (14), pp. 1329-1335
dcterms.licensehttp://creativecommons.org/licenses/by/4.0/
dc.date.updated2020-06-26T03:27:25Z
dc.description.versionVersion of Record (VoR)
gro.rights.copyright© 2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
gro.hasfulltextFull Text
gro.griffith.authorDuffy, Sandra
gro.griffith.authorAvery, Vicky M.


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