Xiaolin Li

TL;DR: The discovery and optimization of a series of 4-(aminomethyl)quinolin-2(1H)-ones, exemplified by 34, that inhibit bacterial DNA gyrase and topoisomerase IV and display potent activity against ciprofloxacin-resistant Gram-negative pathogens are described.

TL;DR: In this article, a compound of formula I and a pharmaceutically acceptable salt thereof are defined, wherein the variables R1, R2, R3, R4, R5, and A-B are defined herein, which are non-immunosuppresive, cyclophilin-binding, mPTP blockers and therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection and HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia

TL;DR: In this paper, the authors have proposed pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections, which are useful as inhibitors of bacterial gyrase activity and bacterial infections.

TL;DR: The evolution of the synthetic strategy to from the original medicinal chemistry route, designed for late diversification, to a convergent and robust development synthesis, which led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency.