Design, synthesis, and molecular dynamics simulation studies of some novel kojic acid fused 2-amino-3-cyano-4H-pyran derivatives as tyrosinase inhibitors

Table 1 Tyrosinase inhibitory activities of compounds 6a-o

Entry	Compounds	R₁	R₂	% Inhibition at 80 µM^a	% Inhibition at 30 µM^a	IC₅₀ (µM)
1	6a	H	H	47.90 ± 3.90	–	–
2	6b	H	4-F	89.27 ± 2.59	79.81 ± 6.18	7.69 ± 1.99
3	6c	H	4-Cl	50.01 ± 4.34	44.09 ± 2.94	79.25 ± 3.30
4	6d	H	4-Br	66.36 ± 3.64	48.86 ± 3.53	33.96 ± 2.53
5	6e	H	4-Me	48.63 ± 6.37	–	–
6	6f	H	H	42.27 ± 2.72	–	–
7	6g	H	4-F	88.63 ± 6.36	77.95 ± 4.54	9.72 ± 2.47
8	6h	H	4-Cl	67.95 ± 4.54	65.90 ± 5.09	10.66 ± 4.96
9	6i	H	4-Br	67.72 ± 7.27	59.54 ± 5.44	15.34 ± 3.17
10	6j	H	4-Me	20.45 ± 4.54	–	–
11	6k	OMe	H	10.25 ± 3.48	–	–
12	6l	OMe	4-F	49.09 ± 4.91	–	–
13	6m	OMe	4-Cl	49.31 ± 6.12	–	–
14	6n	OMe	4-Br	21.36 ± 3.63	–	–
15	6o	OMe	4-Me	44.31 ± 4.18	–	–
16	Kojic acid	–	–	–	–	23.64 ± 2.56

ISSN: 2661-801X