An expedient synthesis of novel 2-substituted thiazolo[4,5-f]isoquinolines/quinolines and benzo[1,2-d:4,3-d′]bisthiazoles and their potential as inhibitors of COX-1 and COX-2

被引：13

作者：

Chakrabarty, Manas ^{[1
]}

Mukherji, Ajanta ^{[1
]}

Karmakar, Sulakshana ^{[1
]}

Mukherjee, Ratna ^{[1
]}

Nagai, Kenichiro ^{[2
]}

Geronikaki, Athina ^{[3
]}

Eleni, Pitta ^{[3
]}

机构：

[1] Bose Inst, Dept Chem, 93-1 APC Rd, Kolkata 700009, India

[2] Kitasato Univ, Sch Pharm, Minato Ku, Tokyo 1088641, Japan

[3] Aristotle Univ Thessaloniki, Dept Pharmaceut Chem, Sch Pharm, Thessaloniki 54124, Greece

来源：

ARKIVOC | 2010年

关键词：

Thiazoloisoquinolines; thiazoloquinolines; benzobisthiazoles; COX-inhibition; AROMATIC NITROCOMPOUNDS; BIOLOGICAL EVALUATION; DERIVATIVES; THIAZOLOISOQUINOLINES; AGENTS; DIAMINOBENZOBISTHIAZOLES; BIOSYNTHESIS; MUTAGENICITY; ASSIGNMENTS; REDUCTION;

D O I：

10.3998/ark.5550190.0011.b22

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient, general synthesis of 2-substituted thiazolo[4,5-f]isoquinolines, thiazolo[4,5-f]quinolines and benzo[1,2-d:4,3-d']bisthiazoles has been accomplished from 5-nitroisoquinoline/quinoline and 6-nitrobenzothiazole, respectively, and all the products have been thoroughly identified spectroscopically (IR, H-1 and C-13 NMR, LR/HR EI/FAB/ESI-MS). The synthesis of thiazolo[4,5-f]isoquinolines constitutes the first synthesis of this class of heteroarenes. Eighteen compounds, covering all three types, were screened for inhibition of COX-1 and COX-2, and some of them showed moderate activities.

引用

页码：265 / 290

页数：26

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