US 11,845,734 B1
الصحة - Health
2023
مكتب البراءات الأمريكي - US Patent Office
Shabaan; Saadeldin Elsayed Ibrahim (Al-Ahsa, SA), Ahmed; Hany Mohamed Abd El-Lateef (Al-Ahsa, SA)
Novel dual 5-LO inhibitors of well validated electrophilic Michael acceptors and nitrogen-heterocycles are presented and designed to maintain specific structural features of currently known dual 5-LO inhibitors and to overcome their drawbacks. The Michael acceptor scaffold will act as a carrier and will provide a stable anchorage via covalent binding to cysteine/histidine residues within the catalytic cleft and/or the surface interface of the 5-LO; whereas, the nitrogen-heterocycles will ensure the access to the Fe(II) catalytic center. These combinations offer potential for more than one mode of iron chelation and 5-LO inhibition.