AAI-101 CAS# 1001404-83-6
Enmetazobactam, also known as AAI-101, is a novel β-lactam/β-lactamase inhibitor. AAI101 is similar in structure to tazobactam, with one important difference. AAI101 possesses a strategically placed methyl group that gives the inhibitor a net neutral charge, enhancing bacterial cell penetration. AAI101 paired with cefepime, also a zwitterion, was approved for the treatment of serious Gram-negative infections. AAI101 was found to restore the activity of cefepime against class A ESBLs (e.g., CTX-M-15) and demonstrated increased potency compared to that of piperacillin-tazobactam when tested against an established isogenic panel.
📌 参考资料/链接:
1.1Solvents:Dichloromethane;15 - 20 min, 35 - 42 °C; 60 min, 40 - 42 °C; 15 min, 40 - 42 °C2.160 - 90 min, 0 - 5 °C; 30 min, 0 - 5 °C3.1Reagents:Sodium 2-ethylhexanoateSolvents:Ethanol;60 - 90 min, 20 - 25 °C; 30 min, 20 - 25 °C
📄 详细内容
CAS No. 1001404-83-6 AAI-101 synthetic routes

Method of forming methylpenam triazolyl derivatives as β-lactamase inhibitorsAssignee: Allecra Therapeutics SASInventors: Faini, Andrea; et alWorld Intellectual Property OrganizationPatent#WO2015173378 A2
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