Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
Eur J Med Chem. 2019 May 15;170:157-172. doi: 10.1016/j.ejmech.2019.03.018. Epub 2019 Mar 11.
Emergence of drug resistance has created unmet medical need for the development of new classes of antibiotics. Discovery of new antibacterial agents with new mode of action remains a high priority universally. 4(3H)-quinazolinone, a fused nitrogen heterocyclic compound has emerged as a biologically privileged structure, possessing a wide range of biological properties viz. anticancer, antibacterial, antitubercular, antifungal, anti-HIV, anticonvulsant, anti-inflammatory and analgesic activities. Promising antibacterial properties of quinazolinones have enthused the medicinal chemists to explore and develop this fused heterocyclic system for new antibacterial agents. Utilization of quinazolinone core for the design and synthesis of new antibacterial agents has recently gained momentum. This review aims to provide an overview of the structures and antibacterial activity of various 4(3H)-quinazolinone derivatives covering various aspects of in vitro and in vivo pharmacological activities and structure activity relationships (SARs).
耐药性的出现为开发新类别的抗生素带来了未满足的医学需求。因此,发现具有新作用模式的新型抗菌药物仍然是全球的高度优先事项。4(3H)-喹唑啉酮是一种稠合氮杂环化合物,已成为一种具有广泛生物活性的生物优势结构,具有抗癌、抗菌、抗结核、抗真菌、抗 HIV、抗惊厥、抗炎和镇痛作用。喹唑啉酮类化合物具有有前景的抗菌特性,这激发了药物化学家探索和开发这种稠合杂环系统以获得新的抗菌药物。最近,利用喹唑啉酮核心设计和合成新型抗菌药物的研究进展迅速。本文综述了各种 4(3H)-喹唑啉酮衍生物的结构和抗菌活性,涵盖了体外和体内药理学活性以及构效关系(SARs)的各个方面。