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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents: design, synthesis, biological evaluation and SAR studies.
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2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents: design, synthesis, biological evaluation and SAR studies.

机译：2,3-二甲氧基己-2-烯吡喃糖-4-尿糖作为有希望的新型抗结核药：设计，合成，生物学评估和SAR研究。

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摘要

The alarming resurgence of tuberculosis (TB) underlines the urgent need for development of new and potent anti-TB drugs. Towards this goal we herein report the design and synthesis of 2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents. These easily accessible, small molecules were found to exhibit in vitro activity against Mycobacterium tuberculosis H37Rv in a MIC range of 0.78 mug/mL to 25 mug/mL. A detailed SAR study on these hex-2-enopyranosid-4-uloses led to the identification of compound 5g (S007-724) which on the basis of low MIC (0.78 mug/mL-M. tuberculosis H37Rv; 1.56 mug/mL-MDR, SDR strains of M. tuberculosis; 0.78 mug/mL-inhibition of intracellular replication of M. tuberculosis) and SI value of 13.5 has been identified as a promising lead molecule.
机译：令人震惊的结核病复活表明，迫切需要开发新的有效的抗结核药物。为了实现这一目标，我们在此报告了2,3-二脱氧己基-2-烯吡喃糖苷-4-uloses的设计和合成，它们是有前途的新型抗结核药。发现这些易于获取的小分子在MIC范围为0.78马克/毫升至25马克/毫升的条件下，具有抗结核分枝杆菌H37Rv的体外活性。对这些hex-2-enopyranosid-4-uloses的详细SAR研究导致鉴定了化合物5g（S007-724），该化合物基于低MIC（0.78杯/ mL-结核分枝杆菌H37Rv; 1.56杯/ mL- MDR，结核分枝杆菌的SDR菌株，0.78马克杯/毫升（抑制结核分枝杆菌的细胞内复制）和SI值13.5被确定为有前途的先导分子。

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