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  1. Article ; Online: Shotgun Kinetic Target-Guided Synthesis Approach Enables the Discovery of Small-Molecule Inhibitors against Pathogenic Free-Living Amoeba Glucokinases.

    Kassu, Mintesinot / Parvatkar, Prakash T / Milanes, Jillian / Monaghan, Neil P / Kim, Chungsik / Dowgiallo, Matthew / Zhao, Yingzhao / Asakawa, Ami H / Huang, Lili / Wagner, Alicia / Miller, Brandon / Carter, Karissa / Barrett, Kayleigh F / Tillery, Logan M / Barrett, Lynn K / Phan, Isabelle Q / Subramanian, Sandhya / Myler, Peter J / Van Voorhis, Wesley C /
    Leahy, James W / Rice, Christopher A / Kyle, Dennis E / Morris, James / Manetsch, Roman

    ACS infectious diseases

    2023  Volume 9, Issue 11, Page(s) 2190–2201

    Abstract: Pathogenic free-living amoebae (pFLA) can cause life-threatening central nervous system (CNS) infections and warrant the investigation of new chemical agents to combat the rise of infection from these pathogens. ...

    Abstract Pathogenic free-living amoebae (pFLA) can cause life-threatening central nervous system (CNS) infections and warrant the investigation of new chemical agents to combat the rise of infection from these pathogens.
    MeSH term(s) Humans ; Amoeba ; Glucokinase ; Naegleria fowleri ; Balamuthia mandrillaris ; Acanthamoeba castellanii
    Chemical Substances Glucokinase (EC 2.7.1.2)
    Language English
    Publishing date 2023-10-11
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ISSN 2373-8227
    ISSN (online) 2373-8227
    DOI 10.1021/acsinfecdis.3c00284
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1

    Monastyrskyi, Andrii / Brockmeyer, Fabian / LaCrue, Alexis N / Zhao, Yingzhao / Maher, Steven P / Maignan, Jordany R / Padin-Irizarry, Vivian / Sakhno, Yana I / Parvatkar, Prakash T / Asakawa, Ami H / Huang, Lili / Casandra, Debora / Mashkouri, Sherwin / Kyle, Dennis E / Manetsch, Roman

    Journal of medicinal chemistry

    2021  Volume 64, Issue 10, Page(s) 6581–6595

    Abstract: Preclinical and clinical development of numerous small molecules is prevented by their poor aqueous solubility, limited absorption, and oral bioavailability. Herein, we disclose a general prodrug approach that converts promising lead compounds into ... ...

    Abstract Preclinical and clinical development of numerous small molecules is prevented by their poor aqueous solubility, limited absorption, and oral bioavailability. Herein, we disclose a general prodrug approach that converts promising lead compounds into aminoalkoxycarbonyloxymethyl (amino AOCOM) ether-substituted analogues that display significantly improved aqueous solubility and enhanced oral bioavailability, restoring key requirements typical for drug candidate profiles. The prodrug is completely independent of biotransformations and animal-independent because it becomes an active compound via a pH-triggered intramolecular cyclization-elimination reaction. As a proof-of-concept, the utility of this novel amino AOCOM ether prodrug approach was demonstrated on an antimalarial compound series representing a variety of antimalarial 4(1
    MeSH term(s) Administration, Oral ; Animals ; Antimalarials/chemistry ; Antimalarials/pharmacokinetics ; Antimalarials/pharmacology ; Antimalarials/therapeutic use ; Cyclization ; Disease Models, Animal ; Ethers/chemistry ; Female ; Half-Life ; Hydrogen-Ion Concentration ; Malaria/drug therapy ; Malaria/parasitology ; Mice ; Mice, Inbred BALB C ; Plasmodium falciparum/drug effects ; Prodrugs/chemistry ; Prodrugs/pharmacokinetics ; Prodrugs/pharmacology ; Prodrugs/therapeutic use ; Quinolones/chemistry ; Quinolones/pharmacokinetics ; Quinolones/pharmacology ; Quinolones/therapeutic use ; Solubility ; Structure-Activity Relationship
    Chemical Substances Antimalarials ; Ethers ; Prodrugs ; Quinolones
    Language English
    Publishing date 2021-05-12
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c01104
    Database MEDical Literature Analysis and Retrieval System OnLINE

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