Ghosh Chandradhish, Haldar Jayanta
Chemical Biology and Medicinal Chemistry Laboratory, New Chemistry Unit, Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) Jakkur, Bengaluru 560064, Karnataka (India).
ChemMedChem. 2015 Oct;10(10):1606-24. doi: 10.1002/cmdc.201500299. Epub 2015 Aug 20.
Infectious diseases continue to be one of the major contributors to human morbidity. The rapid rate at which pathogenic microorganisms have developed resistance against frontline antimicrobials has compelled scientists to look for new alternatives. Given their vast antimicrobial repertoire, substantial research effort has been dedicated toward the development of antimicrobial peptides (AMPs) as alternative drugs. However, inherent limitations of AMPs have driven substantial efforts worldwide to develop synthetic mimics of AMPs. This review focuses on the progress that has been made toward the development of small molecules that emulate the properties of AMPs, both in terms of design and biological activity. Herein we provide an extensive discussion of the structural features of various designs and we examine biological properties that have been exploited. Furthermore, we raise a number of questions for which the field has yet to provide solutions and discuss possible future research directions that remain either unexploited or underexploited.
传染病仍然是导致人类发病的主要因素之一。致病微生物对一线抗菌药物产生耐药性的速度之快,迫使科学家们寻找新的替代方案。鉴于抗菌肽具有广泛的抗菌谱,大量的研究工作致力于将其开发为替代药物。然而,抗菌肽的固有局限性促使全球范围内大力研发抗菌肽的合成模拟物。本综述重点关注在开发模拟抗菌肽特性的小分子方面所取得的进展,包括设计和生物活性方面。在此,我们广泛讨论了各种设计的结构特征,并研究了已被利用的生物学特性。此外,我们提出了一些该领域尚未解决的问题,并讨论了可能仍未被开发或未得到充分开发的未来研究方向。