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N,N'-Succinyl bis(p-Aminosalicylate) 유도체의 합성
임채욱,이극선,유재학,이현수,임철부 중앙대학교 약학연구소 2000 약학 논총 Vol.14 No.-
The synthesis of bivalent ligand derivatives of p-aminosalicylate derivatives was described. p-Aminosalicylate was reacted with alcohols to give esters, which was treated with succinyl chloride to yield N,N'-bis(p-aminosalicylate) under Schotten-Baumann condition. The treatment of succinyl chloride with glycine and then reacted with N-hydroxysuccinimide, DCC, and N,N'-bis(p-aminosalicylate) gave N,N'-succinyl bis(p-glycylamino salicylate) derivatives.
임채욱,이극선,오옥희,이현수,임철부 중앙대학교 약학연구소 2000 약학 논총 Vol.14 No.-
The 15 synthesized p-aminosalicylate esters derivatives were evaluated for their antimicrobial activities, in vitro, against Mycobacterium phlei (CACC 75432), Staphylococcus aureus (CHA 78311), Bacillus subtilis (CAUCC 310) and Escherichia coli (P32). Bivalent ligand derivatives (1-6) showed weaker activities than their parent p-aminosalicylate(PAS) in vitro. But some of thiouera derivatives (8 and 10) gave stronger activities against Mycobacterium phlei and Staphylococcus aureus than their parent p-aminosalicylate.