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114th General Meeting of Korean Chemical Society Synthesis and Antitubercular Activity of Extended Carbon C-7 substituted Nitroimidazole analogues of PA-824

Submission Date :
8 / 28 / 2014 , 15 : 26 : 18
Abstract Number :
Presenting Type:
Poster Presentation
Presenting Area :
Authors :
강영구, 박찬용, Garima Arora1, Ramandeep Singh1, 유찬모*, 이일영2,*
성균관대학교 화학과, Korea
1Translational Health Science and Technology Institute, India, India
2한국화학연구원 신물질연구단 난치성질환치료제연구센터, Korea
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Approved : 2 cases
Assigned Code :
MEDI.P-967 Assigend Code Guideline
Presenting Time :
10월 15일 (수요일) 16:00~19:00
Recently the re-emergence of tuberculosis (TB) in the world wide, accompanied by the rise of multidrug-resistant (MDR) strains, emphasizes the need for the discovery of new therapeutic drugs with greater efficacy, safety and novel mechanism of action against this disease. In the course of continuing efforts to sturdy for development new TB drug candidates like salicylanilides, recently we selected PA-824 as a promising new class. The PA-824 ((6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3] oxazine) containing nitroimiazole has entered phase II clinical trials as novel TB therapeutics. OPC-67683 has already done clinical trials. The mechanism of action of PA-824 and OPC-67683 involved as mycolic acid synthesis inhibitors and intracellular nitric oxide (NO) release for respiratory poisoning under aerobic and anaerobic conditions. Although many side chain analogue at C-6 position of PA-824, we try to extend carbon at C-7 position nitroimidazole derivate to improve inhibitory effect for antituberculosis than conventional monocyclic nitro imidazole compound.