Antibiotic resistance is a major global problem in both developed and developing countries.1 The selection pressures on microorganisms when in contact with antibacterial agents underlies the emergence of resistance,2 and the efficacy of first and second line antibiotics is decreasing at an alarming rate.3 A series of novel unique structural organophosphorus aminopyrimidines were developed as potentially DNA-targeting membrane active inhibitors through an efficient one-pot procedure from aldehydes, phosphonate and aminopyrimidine. The biological assay revealed that some prepared compounds displayed antibacterial activities. In this report, we were able to find several new derivatives that have an inhibitory effect. Specifically, tyrosinase is a key enzyme, which catalyzes a rate-limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors.

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