Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119, Haryana, India.
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119, Haryana, India ; Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Ajmer 305801, Rajasthan, India.
J Adv Res. 2015 Jan;6(1):63-71. doi: 10.1016/j.jare.2014.11.002. Epub 2014 Nov 15.
Natural products are increasingly being considered "critical and important" in drug discovery paradigms as a number of them such as camptothecin, penicillin, and vincristine serve as "lead molecules" for the discovery of potent compounds of therapeutic interests namely irinotecan, penicillin G, vinblastine respectively. Derived compounds of pharmacological interests displayed a wide variety of activity viz. anticancer, anti-inflammatory, antimicrobial, anti-protozoal, etc.; when modifications or derivatizations are performed on a parent moiety representing the corresponding derivatives. Pyridoacridine is such a moiety which forms the basic structure of numerous medicinally important natural products such as, but not limited to, amphimedine, ascididemin, eilatin, and sampangine. Interestingly, synthetic analogues of natural pyridoacridine exhibit diverse pharmacological activities and in view of these, natural pyridoacridines can be considered as "lead compounds". This review additionally provides a brief but critical account of inherent structure activity relationships among various subclasses of pyridoacridines. Furthermore, the current aspects and future prospects of natural pyridoacridines are detailed for further reference and consideration.
天然产物在药物发现模式中越来越被认为是“关键和重要的”,因为它们中的许多物质,如喜树碱、青霉素和长春新碱,分别作为伊立替康、青霉素 G 和长春碱等具有治疗意义的有效化合物的“先导分子”。具有药理活性的衍生化合物显示出广泛的活性,如抗癌、抗炎、抗菌、抗原生动物等;当对代表相应衍生物的母体部分进行修饰或衍生化时。吡啶并吖啶是这样一种部分,它构成了许多具有医学重要性的天然产物的基本结构,如,但不限于, Amphimedine、Ascididemin、Eilatin 和 Sampangine。有趣的是,天然吡啶并吖啶的合成类似物表现出多种药理活性,鉴于这些,天然吡啶并吖啶可以被认为是“先导化合物”。本综述还简要但批判性地介绍了各种吡啶并吖啶亚类之间的固有结构-活性关系。此外,详细介绍了天然吡啶并吖啶的当前方面和未来前景,以供进一步参考和考虑。