111600-85-2Relevant articles and documents
Synthesis and anti-inflammatory activity of ethynylthiazoles
Geronikaki,Vasilevsky,Hadjipavlou-Litina,Lagunin,Poroikov
, p. 675 - 680 (2006)
A series of acetylene derivatives of thiazole using the Sonogashira cross-coupling method was synthesized and evaluated in vivo for their anti-inflammatory activity. Four compounds exhibited good anti-inflammatory activity and two inhibited soybean lipoxy
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Keeley,ábrányi-Balogh,Keseru
supporting information, p. 263 - 267 (2019/03/05)
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed correlations between the electronic properties of the heterocyclic cores and their reactivity against GSH that are helpful in identifying suitable fragments for cysteines with specific nucleophilicity. The most important advantage of these fragments is that they show only minimal structural differences from non-electrophilic counterparts. Therefore, they could be used effectively in the design of targeted covalent inhibitors with minimal influence on key non-covalent interactions.
(DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES
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Page/Page column 79, (2009/10/09)
The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.