Pharmaceutical Studies on the Esterification of Chloramphenicol with Antipyretics (I)

Chloramphenicol과 해열제와의 Ester화합물에 관한 약제학적 연구 (I)

Chloramphenicol (CAF) was esterified with aspirin, naproxen and acetaminophen in order to develop new prodrugs which have double effect-antibiotic activity and antipyretic effect. Chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate (CAF-NAX), and chloramphenicol acetaminophen succinate (CAF-SUC-ACET) were synthesized by using dicyclohoxylcarbodiimidc (D.C.C.) because of two hydroxyl group of chloramphenicol. Three synthetic prodrugs did not show bitterness and antibiotic activity in vitro, and were hydrolyzed in liver homogenate, but weren't in acid.