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Design and synthesis of pyrimido[4,5-b][1,4]benzothiazine derivatives, as potent 15-lipoxygenase inhibitors

2006; Elsevier BV; Volume: 15; Issue: 5 Linguagem: Inglês

10.1016/j.bmc.2006.12.022

1464-3391

Mehdi Bakavoli, Mohsen Nikpour, Mostafa Gholizadeh, Mohammad Reza Saberi, Hamid Sadeghian,

Quinazolinone synthesis and applications

A group of 2-substituted pyrimido[4,5-b][1,4]benzothiazines were designed, synthesized, and evaluated as potential inhibitors of 15-lipoxygenase (15-LO). Compounds 4d and 4e showed the best IC50 of 15-LO inhibition (IC50=18 and 34 microM, respectively). All compounds were docked into 15-LO. As a result the sulfur atom was oriented toward the iron atom of the active site of 15-LO. We suggest the interaction of the iron atom is essential for the activity of the inhibitors.