Synthesis, characterization and biological evaluation of benzothiazoles and tetrahydrobenzothiazoles bearing urea or thiourea moieties as vasorelaxants and inhibitors of the insulin releasing process
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- 作者：Kamel Harrouchea ; Jean-Francois Renardb ; Nafila Bouidera ; Pascal de Tulliob ; Eric Goffinb ; Philippe Lebrunc ; Gilles Fauryd ; Bernard Pirotteb ; b.pirotte@ulg.ac.be" class="auth_mail" title="E-mail the corresponding author ; Smail Khelilia
- 关键词：Diazoxide ; Pinacidil ; Benzothiazole ; Benzothiadiazine ; KATP channel ; Potassium channel openers
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 June 2016
- 年：2016
- 卷：115
- 期：Complete
- 页码：352-360
- 全文大小：490 K
文摘
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A series of 1,3-benzothiazoles and 4,5,6,7-tetrahydro-1,3-benzothiazoles were synthesized.
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Several 1,3-benzothiazole derivatives showed a myorelaxant activity higher than diazoxide.
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Their myorelaxant activity was explained, at least in part, by the opening of KATP channels.
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Some 1,3-benzothiazole derivatives also provoked a marked inhibition of insulin secretion.