Microwave synthesis, characterization and bio-efficacy evaluation of novel chalcone based 6-carbethoxy-2-cyclohexen-1-one and 2H-indazol-3-ol derivatives

作者：Shakil N A^*; Singh Manish K; Sathiyendiran M; Kumar J; Padaria Jasdeep C

来源：European Journal of Medicinal Chemistry, 2013, 59: 120-131.

DOI：10.1016/j.ejmech.2012.10.038

• Chalcone
• Cyclohexenone
• Indazole
• Anti-fungal
• Anti-bacterial
• Anti-oxidant

Novel chalcone based 6-carbethoxy-2-cyclohexen-1-one and 2H-indazol-3-ol derivatives were synthesized and characterized by using spectral techniques like IR, H-1 NMR, C-13 NMR, COSY, DEPT, and GC-MS. All these compounds were screened for anti-fungal, anti-bacterial and anti-oxidant activity. Cyclohexenone derivatives, in general, showed better anti-fungal and anti-bacterial activity than parent chalcones. Whereas, all the Indazole derivatives showed very good anti-oxidant activity and some were also found to be active as anti-bacterial agent. Among the screened compounds, 15 was found to be most active as anti-fungal agent (against Rhizoctonia solani, LC50 = 2.36 mu g mL(-1)), 15b was found to be most active anti-bacterial agent (against Klebsiella pneumonia, MIC = 24.68 mu g mL(-1)) and 14b emerged as most active anti-oxidant (IC50 = 19.81 mu g mL(-1)).

• 出版日期2013-1