usnic酸和异烟肼合成酰基腙及其抗结核分枝杆菌活性

Pub Date : 2017-09-01 DOI:10.15446/REV.COLOMB.QUIM.V46N3.61980

Melissa Barrera Tomas, Gloria Eva Tomas Chota, Patricia Sheen Cortavarría, Patricia Fuentes Bonilla, Miguel Angel Inocente Camones, J. Contreras

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引用次数: 7

摘要

从秘鲁苔草（Cajamarca Peru）中分离得到化合物usnic酸（1），并对其酰基腙（2）的合成和表征进行了评价，该化合物由usnic和异烟肼在乙醇溶液中回流缩合反应得到，总收率为95%。基于四氮唑微板测定法（TEMA），根据异烟肼的抗结核分枝杆菌活性对两种化合物进行评估并与异烟肼进行比较。化合物1在H37Rv（易感型）、TB DM 97（耐药野生型）和MDR DM 1098（多药耐药型）菌株的每次测试中具有16.0μg/mL的MIC（最小抑制浓度）值。在类似的试验中，化合物2的MIC值分别为2.0、64.0和64.0μg/mL。

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Synthesis of acyl-hydrazone from usnic acid and isoniazid and its anti-Mycobacterium tuberculosis activity

Compound usnic acid (1), isolated from lichen Evernia prunastri (Cajamarca-Peru) and the synthesis and characterization of its acyl-hydrazone (2), from the condensation reaction between usnic acid and isoniazid in an ethanol solution under reflux, giving an overall yield of 95%, were evaluated. Both compounds were evaluated and compared with isoniazid according to its anti-Mycobacterium tuberculosis activity based on the tetrazolium microplate assay (TEMA). Compound 1 had MIC (minimal inhibitory concentration) value of 16.0 μg/mL in each test of H37Rv (susceptible type), TB DM 97 (resistant wild type) and MDR DM 1098 (multi drug resistances type) strains. In similar tests, compound 2 MIC values were 2.0, 64.0 and 64.0 μg/mL respectively.

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