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  • N-Aryl-2-aminobenzimidazoles: Novel, Efficacious, Antimalarial Lead Compounds

    Author(s)
    Ramachandran, Sreekanth
    Hameed, Shahul P
    Srivastava, Abhishek
    Shanbhag, Gajanan
    Morayya, Sapna
    Rautela, Nikhil
    Awasthy, Disha
    Kavanagh, Stefan
    Bharath, Sowmya
    Reddy, Jitendar
    Panduga, Vijender
    Prabhakar, KR
    Saralaya, Ramanatha
    Nanduri, Robert
    Raichurkar, Anandkumar
    Menasinakai, Sreenivasaiah
    Achar, Vijayashree
    Belen Jimenez-Diaz, Maria
    Santos Martinez, Maria
    Angulo-Barturen, Inigo
    Ferrer, Santiago
    Maria Sanz, Laura
    Javier Gamo, Francisco
    Duffy, Sandra
    Avery, Vicky M
    Waterson, David
    Lee, Marcus CS
    Coburn-Flynn, Olivia
    Fidock, David A
    Iyer, Pravin S
    Narayanan, Shridhar
    Hosagrahara, Vinayak
    Sambandamurthy, Vasan K
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2014
    Metadata
    Show full item record
    Abstract
    From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against the asexual blood stage of Plasmodium falciparum (Pf). Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the identification of 12 as a lead molecule. Compound 12 was efficacious in the P. berghei (Pb) model of malaria. This compound displayed an excellent pharmacokinetic profile with a long half-life (19 h) in rat blood. This profile led to an extended survival of animals for over 30 days following a dose of 50 mg/kg in the Pb malaria model. ...
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    From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against the asexual blood stage of Plasmodium falciparum (Pf). Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the identification of 12 as a lead molecule. Compound 12 was efficacious in the P. berghei (Pb) model of malaria. This compound displayed an excellent pharmacokinetic profile with a long half-life (19 h) in rat blood. This profile led to an extended survival of animals for over 30 days following a dose of 50 mg/kg in the Pb malaria model. Compound 12 retains its potency against a panel of Pf isolates with known mechanisms of resistance. The fast killing observed in the in vitro parasite reduction ratio (PRR) assay coupled with the extended survival highlights the promise of this novel chemical class for the treatment of malaria.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    57
    DOI
    https://doi.org/10.1021/jm500715u
    Subject
    Chemical Sciences not elsewhere classified
    Medicinal and Biomolecular Chemistry
    Organic Chemistry
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/140944
    Collection
    • Journal articles

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