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Synthesis of Novel tricyclic pyrazolo(1,4)oxathiinopyrazines and Evaluation of Their Competency Towards the Inhibition of Lactate Dehydrogenase Activity-Inhibition of LDH Activity

机译:新型三环吡唑(1,4)恶病毒嘧啶的合成及其对乳酸脱氢酶活性抑制LDH活性的持态性的评价

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摘要

We have evaluated the LDH inhibitory property of novel pyrazolo[4′,3′:5,6][1,4]oxathiino[2,3-b]pyrazine derivatives which have been synthesized from easily available starting materials through a one-pot protocol that offers the use of elemental sulfur as the sulfur source. These newly synthesized compounds may aid to drug development for neoplastic and non-neoplastic diseases characterized by increased glucose metabolism. Additionally, they may act as suitable starting materials which can be further structurally modified for the development of new LDH inhibitors with higher efficacy and specificity.
机译:我们已经评估了新型吡唑的LDH抑制性质[4',3',3':5,6] [1,4]血吡嗪衍生物,其已经通过一个罐从易于使用的原料中合成的 提供使用元素硫作为硫源的协议。 这些新合成的化合物可以有助于针对肿瘤和非肿瘤疾病的药物发育,其特征在于葡萄糖代谢增加。 另外,它们可以充当合适的起始材料,其可以进一步修饰,用于开发具有更高疗效和特异性的新LDH抑制剂。

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