Antimycobacterial activity generated by the amide coupling of (-)-fenchone derived aminoalcohol with cinnamic acids and analogues

作者：Slavchev Ivaylo; Dobrikov Georgi M^*; Valcheva Violeta; Ugrinova Iva; Pasheva Evdokia; Dimitrov Vladimir

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(21): 5030-5033.

DOI：10.1016/j.bmcl.2014.09.021

• Fenchone
• Amides
• Cinnamic acids
• Tuberculosis

Aminoethyl substituted 2-endo-fenchol prepared from (-)-fenchone was used as scaffold for the synthesis of series of 31 amide structures by N-acylation applying cinnamic acids and analogues. The evaluation of their in vitro activity against Mycobacterium tuberculosis H(37)Rv showed for some of them promising activity-up to 0.2 mu g/ml, combined with relatively low cytotoxicity of the selected active compounds.

• 出版日期2014-11-1