Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent

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 30 maintained antitubercular activity against moxifloxacin-, isoniazid-, and rifampicin-resistant Mycobacterium tuberculosis, while 37 exhibited low micromolar activities (1 mu g/mL) against World Health Organization (WHO) critical pathogens: Cryptococcus neoformans, Acinetobacter baumannii, and Pseudomonas aeruginosa. 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.

Automated summary

In this study, 39 novel quinolone compounds with a hydrophilic amine chain and varied substituted benzyloxy units were described. These compounds demonstrated broad-spectrum activities against acid-fast bacterium, Gram-positive and-negative bacteria, fungi, and leishmania parasite. Compound 30 showed antitubercular activity against drug-resistant Mycobacterium tuberculosis, while compound 37 exhibited low micromolar activities against critical pathogens.