抗分枝杆菌活性：新型 3-(取代苯基)-6,7-二甲氧基-3a,4-二氢-3H-茚并[1,2-c]异噁唑类似物的合成。
Antimycobacterial activity: synthesis of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues.
机构信息
Pharmacogenetic and Novel Therapeutic, Institute for Research in Molecular Medicine, Universiti of Sains Malysia, Pennag-11800, Malaysia.
出版信息
J Enzyme Inhib Med Chem. 2011 Aug;26(4):598-602. doi: 10.3109/14756366.2010.529805.
In this study, a series of novel 3-(substituted phenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues were synthesized and evaluated for antimycobacterial activity against Mycobacterium tuberculosis (MTB) H(37)Rv and isoniazid resistant M. tuberculosis (INHR-MTB). All the newly synthesized compounds were showing moderate to high inhibitory activities. The compound 6,7-dimethoxy-3-(4-chloro phenyl)-4H-indeno[1,2-c]isoxazole (4b) was found to be the most promising compound, active against MTB H(37)Rv and INHR-MTB with minimum inhibitory concentrations of 0.22 and 0.34 μM.
在这项研究中，合成了一系列新型 3-(取代苯基)-6,7-二甲氧基-3a,4-二氢-3H-茚并[1,2-c]异噁唑类似物，并评估了它们对结核分枝杆菌（MTB）H37Rv 和异烟肼耐药结核分枝杆菌（INHR-MTB）的抗微生物活性。所有新合成的化合物均表现出中等至强的抑制活性。发现化合物 6,7-二甲氧基-3-(4-氯苯基)-4H-茚并[1,2-c]异噁唑（4b）是最有前途的化合物，对 MTB H37Rv 和 INHR-MTB 的最小抑菌浓度分别为 0.22 和 0.34 μM。
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