새로운 엽산 대사 길항제의 합성 및 약리활성

• 영문명: Synthesis and Pharmacological Activities of New Folic Acid Antagonists
• 발행기관: 대한약학회
• 저자명: 신관석(Kwan Seog Sin) 성선영(Sun Young Sung) 남재우(Jae Woo Nam) 최상운(Sang Un Choi) 이정옥(Chong Ock Lee)
• 간행물 정보: 『약학회지』제36권 제4호 (1992년), 326~333쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1992.08.30

영문 초록

A new series of methotrexate analogues was prepared in which the beta-position of the glutamic acid moiety is substituted by the aryl groups. The glutamic acid moiety was modified in order to enhance the lipophilic property. Reaction of N-acetylglicine ester[1] with ethyl 3-arylacrylate derivatives[2] produced trans-3-aryl-2-carboxy-5-pyrrolidone derivatives[3], which were hydrolyzed to give beta-aryl-glutamic acid derivatives[4]. The compounds[4] were treated with the p-aminobenzoic acid moiety and then with the pteridine ring moiety to give beta-arylmethotrexate derivatives[6,7]. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against murine leukemias and against human tumor cell lines in vitro. Several compounds showed significant antibacterial activity.