Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, P.R. China.
Curr Top Med Chem. 2013 Aug;13(16):1963-2010. doi: 10.2174/15680266113139990125.
Azole compounds are an important class of nitrogen heterocycles with electron-rich property. This special structure endows azole-based derivatives easily bind with the enzymes and receptors in organisms through noncovalent interactions such as hydrogen bonds, coordination bonds, ion-dipole, cation-π,π-π stacking and hydrophobic effect as well as van der Waals force etc., thereby possessing various applications in medicinal chemistry, especially their protrudent effects such as imidazoles and triazoles against fungal strains. The design, synthesis and antimicrobial activity of azole derivatives have been extensively investigated and have become one of the highly active highlights in recent years, and the progress is quite rapid. In particular, a large number of azole-based antibacterial and antifungal agents have been penetratingly studied as candidates and even some of them have been used in clinic, which have shown the great potential and development value of azole compounds. Based on our researches on azole compounds and referring to other literature, this work scientifically reviewed the researches and developments of azole-based compounds as antibacterial and antifungal agents, including oxazole, imidazole, benzimidazole, triazole, benzotriazole, pyrazole, thiazole, carbazole as well as tetrazole in recent three years. It is hopeful that azole compounds may continue to serve as an important direction for the exploitation of azole-based antibacterial and antifungal drugs with better curative effect, lower toxicity, less side effects, especially fewer resistances and so on.
唑类化合物是一类具有富电子性质的重要氮杂环化合物。这种特殊的结构使唑类衍生物能够通过氢键、配位键、离子偶极、阳离子-π、π-π堆积和疏水作用以及范德华力等非共价相互作用，轻易地与生物体内的酶和受体结合，从而在药物化学中具有广泛的应用，尤其是咪唑和三唑类化合物对真菌菌株的突出作用。唑类衍生物的设计、合成和抗菌活性已经得到了广泛的研究，并且已经成为近年来非常活跃的研究热点之一，进展相当迅速。特别是，大量的唑类抗菌和抗真菌药物作为候选药物进行了深入研究，其中一些甚至已经在临床上使用，这表明了唑类化合物具有巨大的潜力和发展价值。基于我们对唑类化合物的研究，并参考其他文献，本工作对近三年来作为抗菌和抗真菌剂的唑类化合物的研究和开发进行了科学综述，包括噁唑、咪唑、苯并咪唑、三唑、苯并三唑、吡唑、噻唑、咔唑和四唑。希望唑类化合物能够继续成为开发疗效更好、毒性更低、副作用更小、特别是耐药性更少的唑类抗菌和抗真菌药物的重要方向。
