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dc.contributor.authorHameed, Shahul P
dc.contributor.authorChinnapattu, Murugan
dc.contributor.authorShanbag, Gajanan
dc.contributor.authorManjrekar, Praveena
dc.contributor.authorKoushik, Krishna
dc.contributor.authorRaichurkar, Anandkumar
dc.contributor.authorPatil, Vikas
dc.contributor.authorJatheendranath, Sandesh
dc.contributor.authorRudrapatna, Suresh S
dc.contributor.authorBarde, Shubhada P
dc.contributor.authorRautela, Nikhil
dc.contributor.authorAwasthy, Disha
dc.contributor.authorMorayya, Sapna
dc.contributor.authorNarayan, Chandan
dc.contributor.authorKavanagh, Stefan
dc.contributor.authorSaralaya, Ramanatha
dc.contributor.authorBharath, Sowmya
dc.contributor.authorViswanath, Pavithra
dc.contributor.authorMukherjee, Kakoli
dc.contributor.authorBandodkar, Balachandra
dc.contributor.authorSrivastava, Abhishek
dc.contributor.authorPanduga, Vijender
dc.contributor.authorReddy, Jitender
dc.contributor.authorPrabhakar, KR
dc.contributor.authorSinha, Achyut
dc.contributor.authorBelen Jimenez-Diaz, Maria
dc.contributor.authorSantos Martinez, Maria
dc.contributor.authorAngulo-Barturen, Inigo
dc.contributor.authorFerrer, Santiago
dc.contributor.authorMaria Sanz, Laura
dc.contributor.authorJavier Gamo, Francisco
dc.contributor.authorDuffy, Sandra
dc.contributor.authorAvery, Vicky M
dc.contributor.authorMagistrado, Pamela A
dc.contributor.authorLukens, Amanda K
dc.contributor.authorWirth, Dyann F
dc.contributor.authorWaterson, David
dc.contributor.authorBalasubramanian, V
dc.contributor.authorIyer, Pravin S
dc.contributor.authorNarayanan, Shridhar
dc.contributor.authorHosagrahara, Vinayak
dc.contributor.authorSambandamurthy, Vasan K
dc.contributor.authorRamachandran, Sreekanth
dc.date.accessioned2017-11-20T04:45:43Z
dc.date.available2017-11-20T04:45:43Z
dc.date.issued2014
dc.identifier.issn0022-2623
dc.identifier.doi10.1021/jm500535j
dc.identifier.urihttp://hdl.handle.net/10072/140995
dc.description.abstractWhole-cell high-throughput screening of the AstraZeneca compound library against the asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino imidazoles, a robust starting point for initiating a hit-to-lead medicinal chemistry effort. Structure–activity relationship studies followed by pharmacokinetics optimization resulted in the identification of 23 as an attractive lead with good oral bioavailability. Compound 23 was found to be efficacious (ED90 of 28.6 mg·kg–1) in the humanized P. falciparum mouse model of malaria (Pf/SCID model). Representative compounds displayed a moderate to fast killing profile that is comparable to that of chloroquine. This series demonstrates no cross-resistance against a panel of Pf strains with mutations to known antimalarial drugs, thereby suggesting a novel mechanism of action for this chemical class.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.publisher.placeUnited States
dc.relation.ispartofpagefrom5702
dc.relation.ispartofpageto5713
dc.relation.ispartofissue13
dc.relation.ispartofjournalJournal of Medicinal Chemistry
dc.relation.ispartofvolume57
dc.subject.fieldofresearchChemical Sciences not elsewhere classified
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode039999
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.titleAminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorDuffy, Sandra
gro.griffith.authorAvery, Vicky M.


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