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The Search For Novel Inhibitors Of The Mycobacterial Enoyl Reductase Inha, Esther Saul

The Science Journal of the Lander College of Arts and Sciences

Isoniazid (INH), one of two first-line drugs used to treat tuberculosis (TB), has been shown to be a potent inhibitor of InhA, the mycobacterial enoyl reductase. However, the increasing resistance to INH makes it imperative to find alternative drugs that are as effective as the first-line drugs, yet active against INH-resistant strains. Since InhA has been validated as an excellent target of TB, there have been attempts to find novel inhibitors of InhA. Through rational drug design, a variety of high affinity InhA inhibitors were synthesized. Triclosan itself was observed to be a suboptimal inhibitor of InhA with a K …