Structural analog of Cyclotheonellazole A, and synthetic method therefor and application method thereof

US12162894B2 · kind B2 · utility

Assignee

• The Second People's Hospital of Shenzhen (Shenzhen Institute of Geriatrics) · CN

Inventors

• Zhengzhi Wu · Nanhu, CN
• Bohua Long · Dongguan, CN
• Zhiyue Li · Lo Wu, CN
• Liuyang Pu · Lo Wu, CN
• Shengquan Hu · Lo Wu, CN
• Limin Li · Longbeilingcun, CN

Key dates

• Filing date: Dec 4, 2023
• Grant date: Dec 10, 2024
• Expiry date: Dec 4, 2043

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A structural analog of Cyclotheonellazole A, and a synthetic method therefor and an application method thereof are provided. A compound with a structure of formula (I) and a pharmaceutically acceptable salt thereof are provided. The formula (I) is as follows: R1, R2, R3 and R4 are independently selected form the group consisting of H, a C1-C6 alkyl group, a C1-C6 alkoxy group, a halogen group, a hydroxyl group, an amino group, a nitro group, a cyano group, and a sulfydryl group. Based on the total synthetic route of Cyclotheonellazole A, the classical reverse synthesis analysis is utilized, the structural modification is purposefully carried out, a mother nucleus of the natural product remains unchanged, and the structural analog 1a is obtained by replacing a left side chain with a simple formylamine, thereby confirming the excellent protease inhibitory activity thereof, and having a strong application prospect in the pharmaceutical industry.