The growth of resistance to antimycobacterial drugs dictates the need to develop new agents with high therapeutic efficacy and low toxicity. The present review analyzes and summarizes literature data over the past decade on the synthesis and study of antimycobacterial agents using both an empirical approach and molecular docking. Pyrimidines, amides, coumarins, chalcones, furans, azomethines, salicylanilides, oxazolidines, nitroimidazoles, benzothiazinones, diarylquinolines, azaindoles, imidazopyridines, benzimidazoles, and riminophenazines, some of which are in various stages of clinical trials, are of most interest to researchers. Special attention is paid to identifying the targets of new compounds and studying their mechanisms of action when creating antimycobacterial agents.