RRC ID |
52170
|
著者 |
Saijo R, Sekiya H, Tamai E, Kurihara KI, Maki J, Sakagami H, Kawase M.
|
タイトル |
A Novel Methodology for Synthesis of 1,5,6-Trisubstituted 2(1H)-Pyrazinones of Biological Interest.
|
ジャーナル |
Chem Pharm Bull (Tokyo)
|
Abstract |
In this report, we describe a new method for the synthesis of densely functionalized 2(1H)-pyrazinones. Treatment of mesoionic 1,3-oxazolium-5-olates with carbanions derived from activated methylene isocyanides (p-toluenesulfonylmethyl isocyanide (TosMIC) and ethyl isocyanoacetate) causes a novel ring transformation affording 2(1H)-pyrazinones in moderate to high yields. The cytotoxicity and antibacterial activity of some of the obtained products were studied and some of the products exhibited tumor-specific cytotoxicity.
|
巻・号 |
65(4)
|
ページ |
365-372
|
公開日 |
2017-1-1
|
DOI |
10.1248/cpb.c16-00830
|
PMID |
28381677
|
MeSH |
Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line
Cell Survival / drug effects
Chemistry Techniques, Synthetic*
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Gram-Negative Bacteria / drug effects
Gram-Positive Bacteria / drug effects
Humans
Microbial Sensitivity Tests
Molecular Structure
Pyrazines / chemical synthesis*
Pyrazines / chemistry
Pyrazines / pharmacology*
Structure-Activity Relationship
|
IF |
1.416
|
引用数 |
4
|
リソース情報 |
ヒト・動物細胞 |
Ca9-22(RCB1976)
HSC-2(RCB1945)
HSC-3(RCB1975)
HSC-4(RCB1902) |