Synthesis and QSAR Studies of Claramine Derivatives, a New Class of Broad-Spectrum Antimicrobial Agents.

The development of new antibiotics has been recognized for over two decades as a major challenge in combating multidrug-resistant bacteria. Herein, we report the synthesis and QSAR studies of claramine derivatives, a new class of broad-spectrum antimicrobial agents active against both susceptible and resistant Gram-positive and Gram-negative strains. The observed antimicrobial activities were rationalized based on key topological parameters of the derivatives, while cytotoxicity was interpreted by correlating half maximal inhibitory concentration (IC50) values with QSAR models. Owing to the low cytotoxicity observed for several analogues, this molecular class represents a promising alternative for the development of novel agents to counteract multidrug resistance.