Aminobenzoic Acid Derivative - Explore the Science & Experts | ideXlab

Scan Science and Technology

Contact Leading Edge Experts & Companies

Aminobenzoic Acid Derivative

The Experts below are selected from a list of 30 Experts worldwide ranked by ideXlab platform

Michael Wiese – 1st expert on this subject based on the ideXlab platform

  • a 4 Aminobenzoic Acid Derivative as novel lead for selective inhibitors of multidrug resistance associated proteins
    Bioorganic & Medicinal Chemistry Letters, 2008
    Co-Authors: Stefan Leyers, Hansgeorg Hacker, Jeanette Wiendlocha, Michael Gutschow, Michael Wiese

    Abstract:

    We present a novel lead for inhibitors of multidrug resistance-associated proteins (MRPs). Compound 1 (4-[(5,6,7,8-tetrahydro-4-oxo-4H-[1]benzothieno[2,3-d][1,3]thiazin-2-yl)amino]benzoic Acid) was about six times more potent than the known inhibitor MK571 at MRP1, while at MRP2 its effect was similar to that of MK571. Structural analogs were also evaluated. Among them, compound 2, sharing the 4-Aminobenzoic Acid substructure with 1, also inhibited MRP1. Both Derivatives were inactive against P-gp. It can be concluded that their carboxyl group is needed for inhibition of MRPs and accounts for the selectivity of these compounds.

Stefan Leyers – 2nd expert on this subject based on the ideXlab platform

  • a 4 Aminobenzoic Acid Derivative as novel lead for selective inhibitors of multidrug resistance associated proteins
    Bioorganic & Medicinal Chemistry Letters, 2008
    Co-Authors: Stefan Leyers, Hansgeorg Hacker, Jeanette Wiendlocha, Michael Gutschow, Michael Wiese

    Abstract:

    We present a novel lead for inhibitors of multidrug resistance-associated proteins (MRPs). Compound 1 (4-[(5,6,7,8-tetrahydro-4-oxo-4H-[1]benzothieno[2,3-d][1,3]thiazin-2-yl)amino]benzoic Acid) was about six times more potent than the known inhibitor MK571 at MRP1, while at MRP2 its effect was similar to that of MK571. Structural analogs were also evaluated. Among them, compound 2, sharing the 4-Aminobenzoic Acid substructure with 1, also inhibited MRP1. Both Derivatives were inactive against P-gp. It can be concluded that their carboxyl group is needed for inhibition of MRPs and accounts for the selectivity of these compounds.

Michael Gutschow – 3rd expert on this subject based on the ideXlab platform

  • a 4 Aminobenzoic Acid Derivative as novel lead for selective inhibitors of multidrug resistance associated proteins
    Bioorganic & Medicinal Chemistry Letters, 2008
    Co-Authors: Stefan Leyers, Hansgeorg Hacker, Jeanette Wiendlocha, Michael Gutschow, Michael Wiese

    Abstract:

    We present a novel lead for inhibitors of multidrug resistance-associated proteins (MRPs). Compound 1 (4-[(5,6,7,8-tetrahydro-4-oxo-4H-[1]benzothieno[2,3-d][1,3]thiazin-2-yl)amino]benzoic Acid) was about six times more potent than the known inhibitor MK571 at MRP1, while at MRP2 its effect was similar to that of MK571. Structural analogs were also evaluated. Among them, compound 2, sharing the 4-Aminobenzoic Acid substructure with 1, also inhibited MRP1. Both Derivatives were inactive against P-gp. It can be concluded that their carboxyl group is needed for inhibition of MRPs and accounts for the selectivity of these compounds.