Dube Phelelisiwe S, Angula Klaudia T, Legoabe Lesetja J, Jordaan Audrey, Boitz Zarella Jan M, Warner Digby F, Doggett J Stone, Beteck Richard M
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.
SAMRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, University of Cape Town Observatory, Cape Town 7925, South Africa.
ACS Omega. 2023 May 4;8(19):17086-17102. doi: 10.1021/acsomega.3c01406. eCollection 2023 May 16.
Herein, we describe 39 novel quinolone compounds bearing a hydrophilic amine chain and varied substituted benzyloxy units. These compounds demonstrate broad-spectrum activities against acid-fast bacterium, Gram-positive and -negative bacteria, fungi, and leishmania parasite. Compound maintained antitubercular activity against moxifloxacin-, isoniazid-, and rifampicin-resistant , while exhibited low micromolar activities (<1 μg/mL) against World Health Organization (WHO) critical pathogens: , , and . Compounds in this study are metabolically robust, demonstrating % remnant of >98% after 30 min in the presence of human, rat, and mouse liver microsomes. Several compounds thus reported here are promising leads for the treatment of diseases caused by infectious agents.
在此，我们描述了39种带有亲水性胺链和不同取代苄氧基单元的新型喹诺酮化合物。这些化合物对抗酸菌、革兰氏阳性和阴性菌、真菌以及利什曼原虫寄生虫具有广谱活性。化合物对耐莫西沙星、异烟肼和利福平的结核分枝杆菌保持抗结核活性，而对世界卫生组织（WHO）的关键病原体：金黄色葡萄球菌、肺炎链球菌和鲍曼不动杆菌表现出低微摩尔活性（<1 μg/mL）。本研究中的化合物代谢稳定性良好，在人、大鼠和小鼠肝微粒体存在的情况下30分钟后仍有>98%的残留率。本文报道的几种化合物是治疗由感染因子引起的疾病的有前景的先导物。
