During drug development, lipophilicity is the most important physicochemical property that might be analyzed for tuberculosis drug discovery because this property can affect the solubility, permeability and bioavailability of compounds . Furthermore, lipophilicity is recognized to impact on a number of drug-like characteristics including pharmacokinetics and toxicology properties . For instance, compounds with high lipophilicity have been related to hepatotoxicity and undesirable non-specific interactions . Nevertheless, highly lipophilic compounds should not be discarded in screening programs for antituberculosis drugs. One example is the drug bedaquiline, which has a cLogP value of 7.3. Likewise, low lipophilicity is not an impediment to tuberculosis drug discovery, considering the number of approved drugs with low lipophilicity, including isoniazid (cLogP = −0.67), ethambutol (cLogP = 0.12), pyrazinamide (cLogP = −0.68), kanamycin (cLogP = −5.2) and cycloserine (cLogP = −1.2). Therefore, we have evaluated the relationship between MIC values and cLogP (Figure 14). The data showed that the majority of active compounds described in this review presented cLogP values in a range from 2 to 6.