http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
곽재환,원선우,정재경,황방연,홍진태,김영수,조정숙,이희순,김태정,이원희,최운화,김성찬,박현정,Eunmiri Roh 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.2
A series of 6- or 7-methylchroman-2-carboxylic acid N-(substituted) phenylamides (2a-s, 3a-s) were synthesized. Their abilities to inhibit nuclear factor-κB (NF-κB) activity were evaluated in lipopolysaccharide (LPS)-stimulated macrophage RAW 264.7 cells. Compounds with substituents such as -H, -CH3, and -CF3 on the phenyl ring were poor inhibitors of NF-κB. The most active NF-κB inhibitors contained4-Cl (3s) and 4-OMe (3g) in the 7-methylchroman-2-carboxamide derivatives and 2-OH (2b) and 4-Cl(2s) in the 6-methylchroman-2-carboxamide derivatives (IC50: 20.2-24.0 μM). These were slightly more potent than a reference compound, KL-1156 (1) (IC50: 43.9 μM).
An efficient synthetic protocol for amide derivatives of Boc-2- aminoisobutyrate
조민미,원선우,이동국,정재경,김선홍,곽영신 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.3
Aminoisobutyric acid (AIB) is an importantbuilding block widely incorporated by medicinal chemistsin molecular design. Owing to the steric challenge, elaboratingAIB’s carboxylic acid using conventional amidationprotocols is often problematic. We discovered that anamidation protocol utilizing methyl Boc-aminoisobutyrateand magnesium amidates of various reactivities producesthe corresponding amide derivatives in good to excellentyields.
Facile ring opening reaction of oxazolone enables efficient amidation for aminoisobutyric acid
조민미,원선우,이동국,윤정연,김선홍,곽영신 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.5
4,4-Dimethyloxazolones derived from N-protectedaminoisobutyric acid (AIB) are particularly knownas poor electrophiles due to the steric hindrance around thecarbonyl and not employed as useful intermediates foramidation whereas numerous examples have been reportedto support the utility of other oxazolones in amidation. AIBis an important and strategical synthon in medicinalchemistry but the peptide bond formation of the N-protectedurethane derivatives of AIB is known to be oftenunproductive due to the rapid formation of the stable 4,4-dimethyloxazolone via an intramolecular cyclization. Wediscovered that the 4,4-dimethyloxazolone of an AIB urethaneis in fact an excellent electrophile that enables efficientamidation even with weakly reactive nucleophiles. The 4,4-dimethyloxazolone can be stored in a pure formand used as a reagent offering an efficient and convenientsynthetic tool for generating AIB-peptide analogs.