At present, the development of medicinal relevant products relies on well-defined criteria and requirements to optimize physicochemical characteristics of drug candidates. Novel approaches in organic synthesis heavily rely on the lead-oriented synthesis concept introduced in 2012, which outlines stringent criteria for favorable physicochemical and structural characteristics that facilitate the direct use of compounds in the initial stages of the drug development. Churcher and co-workers proposed criteria for the lead compounds encompassing molecular weight (MW = 200…350), lipophilicity (LogP = -1…3), etc.