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Development of Human A3 Adenosine Receptor Antagonists as Anti-inflammatory Agents

등록일
2007년 8월 8일 16시 04분 16초
접수번호
0193
발표코드
목20G5심 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 16시 : 00분
발표형식
심포지엄
발표분야
의약화학 - Recent Overview for Overcoming Immune and Inflammatory Diseases
저자 및
공동저자
정낙신
이화여자대학교 약학과,
Many nonpurine heterocyclic A3 adenosine receptor (AR) antagonists have recently been synthesized, but these were found to be weak or ineffective at the rat A3AR and were unsuitable for evaluation in small animal models or for further drug developments. A3AR antagonists of which the affinity and selectivity are independent of species are sought as drug candidates. Because nucleoside analogues have been suitable for this purpose, we searched for novel nucleoside templates with potent and selective binding affinity to human as well as rat A3AR on the basis of A3AR agonists, 2-chloro-N6-substiuted-4′-thioadenosine-5′-uronamides by 1) modification of 5'-monoalkylamides to 5'-dialkylamides; 2) shift of 5′-uronamides to the 1’-position; 3) removal of 5′-uronamides. From this study, we discovered 5′-dialkylamide and 4’-truncated derivatives are pure A3 AR antagonists and they showed potent biological activity in models of a number of disorders related to the A3AR, such as glaucoma and inflammation (This work was supported by Seoul R&D program 10541).

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