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