苯并噻唑衍生物及其生物学意义的研究进展

Rima Mahapatra, K. Hazra
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引用次数: 0

摘要

苯并噻唑是一种具有广泛药理活性的分子。在苯并噻唑的结构中加入一个氟原子增强了药物的各种活性,因为氟原子改变了碳键上的氢原子或氧原子,从而改善了理想的药理学性质,如更长的生物半衰期,与目标受体结合的能力更高,并且还增强了药物的亲脂性。使氟成为药物发现中非常重要的分子的特殊性质包括氟原子的半径非常小,对电子的攻击能力更高,氟原子的极化率非常低。文献表明,苯并噻唑结构中的氟等强电子攻击基团可表现出药物的抗癌活性,苯并噻唑与磺胺或与β -内酰胺环结合可增强抗炎和抗氧化活性。苯并噻唑与恶二唑具有很强的驱虫活性[1-5]。
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A Review on Benzothiazole Derivatives and Their Biological Significances
Benzothiazole is a molecule that has a wide range of pharmacological activities. The addition of a fluorine atom into the structure of benzothiazole enhances the various activities of the drug as the alteration of hydrogen or oxygen atom from a carbon bond by a fluorine atom improves desirable pharmacological properties such as greater biological half-life, higher ability to bind with the targeted receptor, and also enhances the lipophilic character of the drug. The special property that makes fluorine a very important molecule in the drug discovery includes a very small radius of the fluorine atom, a higher attacking power towards electrons, and a very low polarizability of the fluorine atom. Literature reveals that strong electron-attacking groups like fluorine in the structure of benzothiazole can exhibit anticancer activity of the drug, benzothiazole with Sulphonamide or with beta-lactam ring enhances the anti-inflammatory and antioxidant activity. Benzothiazole with oxadiazole shows potent anthelmintic activity [1-5].
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