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<em>Mycobacterium tuberculosis</em> FabH, an essential enzyme in the mycolic acid biosynthetic pathway, is an attractive target for novel anti-tubercolosis agents. Structure-based design and synthesis of 1-(4-carboxybutyl)-4-(4-(substituted benzyloxy)phenyl)-1<em>H</em>-pyrrole-2-carboxylic acid derivatives <strong>7a–h</strong>, a subset of eight potential FabH inhibitors, is described in this paper. The Vilsmeier-Haack reaction was employed as a key step. The structures of all the newly synthesized compounds were identified by IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, ESI-MS and HRMS. The alamarBlue™ microassay was employed to evaluate the compounds <strong>7a–h</strong> against <em>Mycobacterium tuberculosis</em> H<sub>37</sub>Rv. The results demonstrate that the compound <strong>7d</strong> possesses good <em>in vitro</em><em> </em>antimycobacterial activity against <em>Mycobacterium</em><em> tuberculosis </em>H<sub>37</sub>Rv (Minimum Inhibitory Concentration value [MIC], 12.5 µg/mL).These compounds may prove useful in the discovery and development of new anti-tuberculosis drugs.