For many years, macrolides were the first choice of antibiotics in the treatment of bacterial infections. However, with the overuse of antibiotics, many bacterial strains have developed resistance to applicable antibiotics, a problem we still face today. Macrolides were effective antibiotics on the pathogens of most common respiratory diseases, but today their effectiveness in inhibiting protein synthesis is no longer at the same level. However, it has been observed that macrolides in combination with another active molecule have excellent antibacterial activity. This led to the development of the idea for the synthesis of a double-acting molecule consisting of a macrolide backbone to which various other pharmacophore groups are attached. Quinolones (macrolones), acylides, nonsteroidal anti-inflammatory drugs (NSAIDs), steroids, and glycoconjugates are some of the most effective side chains attached to the macrolide ring. This final paper describes molecules found by searching the literature, which have antibacterial and/or anti-inflammatory activity. The length of the linker between the two molecules is a significant factor in the antibacterial effect. The greatest antibacterial efficacy is achieved by modification of cladinose sugar or modification in the C-3 position of the macrocyclic ring. Macrolide and steroid/NSAID hybrids showed improved activity with more specific activity due to improved accumulation within inflammatory cells. In the case of glycoconjugates, however, a reduced antibacterial effect of disaccharides in relation to monosaccharides has been confirmed, with supposedly playing steric disturbances a major role.