121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-590
Subject Construction of Novel 2,5-Piperazinedione Drug-Like Library via Microwave-Assisted Reaction
Authors Si Yeon Han, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
Abstract In this work, we described synthesis of 1-(1,3,4-oxadiazol-2-yl)piperazine-2,5-dione derivatives in solution phase. Many researchers have conducted study about biological activities of 2,5-piperazinedione due to its structural similarities with peptides. Furthermore, 1,3,4-oxadiazoles have been used as potent scaffolds which are reported to produce compounds of interest in various therapeutic areas such as anti-inflammatory, antimicrobial, anticonvulsant, and antihypertensive. In this reason, we were highly interested in the 1,3,4-oxadiazole moiety and tried to establish the 2,5-piperazinedione-containing 1,3,4-oxadiazole libraries. This synthetic methodology involves the preparation of 2,5-piperazinedione core skeleton through cyclization of methyl 2-(2-(amino)acetamido)acetate derived from a reaction between N-α-chloroacetyl amino acid methyl ester and various amines via Microwave heating. It is well known that Microwave reaction in chemical synthesis can decrease reaction time dramatically and generate the desired compounds in high yields and purities at low cost compared to conventional thermal heating. Here in, we report an efficient method for the synthesis of 1-(1,3,4-oxadiazol-2-yl)piperazine-2,5-dione derivatives based on the combinatorial chemistry techniques. References : Yang, Seung-Ju; Lee, Jae-Min; Lee, Gee-Hyung; Kim, NaYeon; Kim, Yong-Sang; Gong, Young-Dae. Bulletin of the Korean Chemical Society Volume 35, Issue 12, 2014, pp.3609-3617
E-mail pywy0626@naver.com