Title:Novel Synthesized Tyrosinase Inhibitors: A Systematic Patent Review
(2012-Present)
Volume: 31
Issue: 3
Author(s): Erika Beltran, Mairim Russo Serafini, Izabel Almeida Alves and Diana Marcela Aragón Novoa*
Affiliation:
- Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá D.C.,
Colombia
Keywords:
Tyrosinase, melanin, melanogenesis, hyperpigmentation, synthetic inhibitors, tyrosinase.
Abstract: Tyrosine is an enzyme responsible for melanin production. Its abnormal accumulation
in different parts of the body is known as hyperpigmentation. Tyrosinase inhibitors
have been used as one of the main approaches to treat these kinds of cosmetic and
medical issues. This review aimed to discuss the advances in patents for this class of inhibitors,
focusing on synthetic ones, by studying recent patent applications (2012-2022).
We performed a screening using the European Patent Office’s Espacenet database, from
which 15 inventions were selected and fully studied. China has more patent applications,
all of them were focused on synthetic methods and the majority declared at least two additional
applications as antibrowning agents for fruits and vegetables, biological pesticides,
and medicine to treat diseases like Parkinson’s or melanoma. The strategies employed by
the investigators focused on the examination of previous literature, which oriented on the
type of structures that have been found to show good inhibitory activity; the study also
examined aspects of their reaction mechanisms and information about the structureactivity
relationship. For some groups of inhibitors, such as benzaldehyde and anthraquinone
derivatives, the data were meaningful and extensive. In contrast, arginyl and troponoids
compounds were difficult to analyze due to the limited research works.
