C07D499/68

METALLO-BETA-LACTAMASE INHIBITOR
20240245783 · 2024-07-25 ·

A compound represented by formula (I), formula (II), or formula (IV), or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the compound or a pharmaceutically acceptable salt thereof, for use in inhibiting metallo-?-lactamases.

MERCAPTOACETOPHENONE AMINOHYDRAZONES, THEIR SALTS AND USES THEREOF

A new class of antibiotics, namely, mercaptoacetophenone aminohydrazones, their analogues, their method of preparation, their salts, and their use in cases of bacterial infections, either alone or with other compounds.

Method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin

A method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin is provided. The method employs immobilized penicillin acylase mutant to catalyze the one-step synthesis of amoxicillin from penicillin potassium, and develops a separation process for the resulting reaction mixture. The technical scheme mainly comprises: Firstly separating the immobilized penicillin acylase mutant from the reaction solution through filtration; subsequently isolating amoxicillin via crystallization; followed by separating and recovering phenylacetic acid through toluene extraction and back extraction. This separation method enables rapid and efficient isolation of amoxicillin with high production yield, achieving an average crystallization rate of 93.22%. Concurrently, it demonstrates effective separation and recovery of phenylacetic acid while allowing recyclable use of the toluene extractant.

Method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin

A method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin is provided. The method employs immobilized penicillin acylase mutant to catalyze the one-step synthesis of amoxicillin from penicillin potassium, and develops a separation process for the resulting reaction mixture. The technical scheme mainly comprises: Firstly separating the immobilized penicillin acylase mutant from the reaction solution through filtration; subsequently isolating amoxicillin via crystallization; followed by separating and recovering phenylacetic acid through toluene extraction and back extraction. This separation method enables rapid and efficient isolation of amoxicillin with high production yield, achieving an average crystallization rate of 93.22%. Concurrently, it demonstrates effective separation and recovery of phenylacetic acid while allowing recyclable use of the toluene extractant.

Mutual Prodrugs of Cromoglicic Acid
20250269041 · 2025-08-28 · ·

Disclosed herein are mutual prodrugs of cromoglicic acid and topical antiseptics, antibiotics, anti-inflammatory agents, keratin softeners, vasoconstrictors, retinoids and retinoid-like drugs and their compositions thereof, and methods for, e.g., treating disorders, and conditions by administration of the compositions. Topical and oral compositions of mutual prodrugs of cromoglicic acid, and derivatives and analogs of cromoglicic acid are also provided.

One-step method for synthesizing amoxicillin from penicillin or salt thereof through enzyme catalysis

A one-step method for synthesizing amoxicillin from penicillin or a salt thereof through an enzyme catalysis is provided. Conventional amoxicillin production requires sequential use of distinct penicillin acylases for hydrolysis and synthesis steps, necessitating isolation of the intermediate 6-aminopenicillanic acid (6-APA) and resulting in elevated manufacturing costs and suboptimal process efficiency. To address these limitations, the inventive method utilizes a mutant of penicillin acylase derived from Kluyvera citrophila as the exclusive biocatalyst in an aqueous reaction system. By reacting penicillin G potassium salt with D-p-hydroxyphenylglycine methyl ester, the process achieves direct amoxicillin synthesis in a single enzymatic step, attaining a product yield of 99%. This method exhibits advantages including fast catalytic rate, high product yield, environmentally friendly pure aqueous reaction system, low cost, and excellent economic benefits.

One-step method for synthesizing amoxicillin from penicillin or salt thereof through enzyme catalysis

A one-step method for synthesizing amoxicillin from penicillin or a salt thereof through an enzyme catalysis is provided. Conventional amoxicillin production requires sequential use of distinct penicillin acylases for hydrolysis and synthesis steps, necessitating isolation of the intermediate 6-aminopenicillanic acid (6-APA) and resulting in elevated manufacturing costs and suboptimal process efficiency. To address these limitations, the inventive method utilizes a mutant of penicillin acylase derived from Kluyvera citrophila as the exclusive biocatalyst in an aqueous reaction system. By reacting penicillin G potassium salt with D-p-hydroxyphenylglycine methyl ester, the process achieves direct amoxicillin synthesis in a single enzymatic step, attaining a product yield of 99%. This method exhibits advantages including fast catalytic rate, high product yield, environmentally friendly pure aqueous reaction system, low cost, and excellent economic benefits.