<p>A series of <i>N</i>-arylidene-5-aryl-1,3,4-oxadiazol-2-amines (<b>2a-d, 3a-d</b> &amp; <b>4a-d</b>) were synthesized with the help of aryl acids, semicarbazide, and aryl benzaldehyde. These synthesized compounds were characterized by elemental analysis, FT-IR, <sup>1</sup>H NMR, and mass spectral data analysis. The title compounds were evaluated as <i>in-vitro</i> antimycobacterial agents against <i>Mycobacterium tuberculosis</i> H37RV via the Microplate Alamar Blue Dye Assay (MABA) method. The <i>in-vitro</i> antimycobacterial result revealed that the most active compounds (<b>2c, 2d, 3c, 3d, 4d</b> &amp; <b>4d</b>) showed a minimum inhibitory concentration (MIC) value of 6.25 μg/ml when compared with the standard drugs Ciprofloxacin, Pyrazinamide (3.125 μg/ml), and Streptomycin (6.25 μg/ml). Most of the title compounds exhibited MIC values ranging from 6.25 to 12.5 μg/ml. Compound <b>3a</b> was found to be the least effective compound. Also, the electron-withdrawing group (Cl &amp; NO<sub>2</sub>) on the phenyl ring was found to be more effective than the electron-releasing groups (OH). All the synthesized compounds encouraged us to continue to progress and improve other novel compounds with effective antimycobacterial potential.</p>

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Synthesis and In-Vitro Antimycobacterial Evaluation of N-Arylidene-5-Aryl-1,3,4-Oxadiazol-2-Amines Derivatives

  • Mazen Almehmadi,
  • Osama Abdulaziz,
  • Mamdouh Allahyani,
  • Abdullah Y. A. Alzahrani,
  • Kamal Kant Joshi,
  • Mohammad Asif

摘要

A series of N-arylidene-5-aryl-1,3,4-oxadiazol-2-amines (2a-d, 3a-d & 4a-d) were synthesized with the help of aryl acids, semicarbazide, and aryl benzaldehyde. These synthesized compounds were characterized by elemental analysis, FT-IR, 1H NMR, and mass spectral data analysis. The title compounds were evaluated as in-vitro antimycobacterial agents against Mycobacterium tuberculosis H37RV via the Microplate Alamar Blue Dye Assay (MABA) method. The in-vitro antimycobacterial result revealed that the most active compounds (2c, 2d, 3c, 3d, 4d & 4d) showed a minimum inhibitory concentration (MIC) value of 6.25 μg/ml when compared with the standard drugs Ciprofloxacin, Pyrazinamide (3.125 μg/ml), and Streptomycin (6.25 μg/ml). Most of the title compounds exhibited MIC values ranging from 6.25 to 12.5 μg/ml. Compound 3a was found to be the least effective compound. Also, the electron-withdrawing group (Cl & NO2) on the phenyl ring was found to be more effective than the electron-releasing groups (OH). All the synthesized compounds encouraged us to continue to progress and improve other novel compounds with effective antimycobacterial potential.