Demarque Daniel P, Espindola Laila S
Laboratory of Pharmacognosy, Department of Pharmacy, Faculty of Health Sciences, University of Brasilia, Brasilia, Brazil.
Laboratory of Pharmacognosy, Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.
Front Chem. 2021 Nov 15;9:779049. doi: 10.3389/fchem.2021.779049. eCollection 2021.
Natural products constitute an important source of molecules for product development. However, despite numerous reports of compounds and active extracts from biodiversity, poor and developing countries continue to suffer with endemic diseases caused by arboviral vectors, including dengue, Zika, chikungunya and urban yellow fever. Vector control remains the most efficient disease prevention strategy. Wide and prolonged use of insecticides has resulted in vector resistance, making the search for new chemical prototypes imperative. Considering the potential of natural products chemistry for developing natural products-based products, including insecticides, this contribution discusses the general aspects and specific characteristics involved in the development of drug leads for vector control. Throughout this work, we highlight the obstacles that need to be overcome in order for natural products compounds to be considered promising prototypes. Moreover, we analyze the bottlenecks that should be addressed, together with potential strategies, to rationalize and improve the efficiency of the drug discovery process.
天然产物是产品开发中分子的重要来源。然而，尽管有大量关于生物多样性中的化合物和活性提取物的报道，但贫穷国家和发展中国家仍继续遭受由虫媒病毒载体引起的地方病之苦，包括登革热、寨卡病毒、基孔肯雅热和城市型黄热病。病媒控制仍然是最有效的疾病预防策略。杀虫剂的广泛和长期使用导致了病媒产生抗性，这使得寻找新的化学原型变得势在必行。考虑到天然产物化学在开发包括杀虫剂在内的基于天然产物的产品方面的潜力，本文论述了开发用于病媒控制的药物先导物所涉及的一般方面和具体特征。在整个研究过程中，我们强调了为使天然产物化合物被视为有前景的原型而需要克服的障碍。此外，我们分析了应该解决的瓶颈以及潜在策略，以合理化和提高药物发现过程的效率。
