Sharma Prabodh Chander, Piplani Mona, Mittal Monika, Pahwa Rakesh
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra-136119, Haryana, India.
Infect Disord Drug Targets. 2016;16(3):140-161. doi: 10.2174/1871526516666160824153226.
Quinolones and fluoroquinolones are principal weapons against variety of bacterial infections and exert their antibacterial potential by interfering the activities of bacterial enzymes. As these agents are associated with some limitations, an important approach to overcome these major constraints is to prepare covalent derivatives, i.e. prodrugs. Prodrug design has been employed to improve the limitations of these drugs such as less aqueous solubility, poor absorption and distribution, toxicity, disagreeable taste, poor lipophilicity etc and for improving their pharmacological profile. This paper highlights the utility of various prodrug strategies in optimizing the therapeutic index of these antibacterial agents and their recent patents. Some of their prodrugs being utilized at preclinical and clinical levels have also been discussed. Hence, this paper has been prepared to present the significant findings of various research papers that would be helpful in motivating scientific researchers to forward the research in direction of utilization of prodrugs in clinical therapy.
喹诺酮类和氟喹诺酮类药物是对抗多种细菌感染的主要武器，它们通过干扰细菌酶的活性发挥抗菌潜力。由于这些药物存在一些局限性，克服这些主要限制的一个重要方法是制备共价衍生物，即前体药物。前体药物设计已被用于改善这些药物的局限性，如较低的水溶性、较差的吸收和分布、毒性、不良味道、较差的亲脂性等，并改善其药理学特性。本文重点介绍了各种前体药物策略在优化这些抗菌药物治疗指数方面的效用及其近期专利。还讨论了一些在临床前和临床水平上使用的前体药物。因此，撰写本文是为了展示各种研究论文的重要发现，这将有助于激励科研人员朝着在前体药物临床治疗中应用的方向推进研究。
