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  • Aminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents

    Author(s)
    Hameed, Shahul P
    Chinnapattu, Murugan
    Shanbag, Gajanan
    Manjrekar, Praveena
    Koushik, Krishna
    Raichurkar, Anandkumar
    Patil, Vikas
    Jatheendranath, Sandesh
    Rudrapatna, Suresh S
    Barde, Shubhada P
    Rautela, Nikhil
    Awasthy, Disha
    Morayya, Sapna
    Narayan, Chandan
    Kavanagh, Stefan
    Saralaya, Ramanatha
    Bharath, Sowmya
    Viswanath, Pavithra
    Mukherjee, Kakoli
    Bandodkar, Balachandra
    Srivastava, Abhishek
    Panduga, Vijender
    Reddy, Jitender
    Prabhakar, KR
    Sinha, Achyut
    Belen Jimenez-Diaz, Maria
    Santos Martinez, Maria
    Angulo-Barturen, Inigo
    Ferrer, Santiago
    Maria Sanz, Laura
    Javier Gamo, Francisco
    Duffy, Sandra
    Avery, Vicky M
    Magistrado, Pamela A
    Lukens, Amanda K
    Wirth, Dyann F
    Waterson, David
    Balasubramanian, V
    Iyer, Pravin S
    Narayanan, Shridhar
    Hosagrahara, Vinayak
    Sambandamurthy, Vasan K
    Ramachandran, Sreekanth
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2014
    Metadata
    Show full item record
    Abstract
    Whole-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 ...
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    Whole-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.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    57
    Issue
    13
    DOI
    https://doi.org/10.1021/jm500535j
    Subject
    Medicinal and biomolecular chemistry
    Organic chemistry
    Other chemical sciences not elsewhere classified
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/140995
    Collection
    • Journal articles

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