Diarylmethanes (DAMs) and triarylmethanes (TAMs) are molecules with two or three aryl groups (phenyls or heterocycles) bonded to a central carbon atom and they have numerous applications. The biological and therapeutic relevancy of this class of molecules have been demonstrated in diverse areas such as antimicrobials, infectious, cardiovascular and nervous system disorders, genital tract diseases, estrogen related disorders and bone remodeling is quite well known. These interesting compounds have also been used as starting materials for the development of high value added molecules. Several synthetic approaches towards bioactive diarylmethanes and triarylmethanes have been published in the literature. This article reviews some approaches followed for the synthesis of diarylmethanes and triarylmethanes as well their biological applications. We will also illustrate the synthesis and antibacterial evaluation of a new triarylmethane series developed in our laboratory using McMurry coupling reaction.