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This review emphasized on the antituberculosis activity of organotin complexes. The astonishing antituberculosis activity of organotin complexes of mefenamic acid, 2-[(2,6-dimethylphenyl)amino]benzoic acid (HDMPA), and [bis(2,6-dimethylphenyl)amino]benzoic acid, NSAIDs from the carboxylic acid, oxicams family, meclofenamic acid or (N-(2,6-dichloro-m-tolylanthranilic acid), cinnamic acid, (Z)-2-acetamido-3-phenylacrylic acid, 3-methyl-but-2-enoic acid, and 2,2-diphenylacetic acid is scrutinized using Mycobacterium tuberculosis H37Rv. It showed that there exists a beguiling, range of structural diversity for organotin moiety in all these complexes. Biologically active compounds should have available coordination positions at tin. Antituberculosis activity of organotin complexes is influenced by the nature of the ligand environment, organic groups attached to the tin, compound structure, toxicity, and potential mechanism of action; though generally, an MIC ≤ 1 μg ml −1 in a new compound class is considered a good lead. The results of complexes exhibited that triorganotin(IV) complexes have superior antituberculosis activity as compared to diorganotin(IV) complexes. It may be due to the fact that generally toxicity of the organotin compounds is associated with the organic ligand and the toxicity decreases with the order of tri > di > mono-organotins.

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