Efficient synthesis of new (R)-2-amino-1-butanol derived ureas, thioureas and acylthioureas and in vitro evaluation of their antimycobacterial activity

The synthesis of 22 structurally diverse urea, thiourea and acylthiourea derivatives containing the (R)-2-amino-1-butanol motif has been performed. The evaluation of their in vitro activity against Mycobacterium tuberculosis (H37Rv and strain 43) showed promising results in the case of the acylthiourea derivatives (MIC range 0.36–7.46 μM for H37Rv strain).

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► 22 Urea, thiourea and acylthiourea derivatives of (R)-2-amino-1-butanol were synthesized.
► 6 Compounds possess perceptible in vitro antimycobacterial activity – up to 20 fold more than EMB.
► 1 Acylthiourea preserve its moderate activity against MDR TB strain.
► The most active compound is less cytotoxic.