14770-79-7Relevant academic research and scientific papers
Thiophene/thiazole-benzene replacement on guanidine derivatives targeting α2-Adrenoceptors
Flood, Aoife,Trujillo, Cristina,Sanchez-Sanz, Goar,Kelly, Brendan,Muguruza, Carolina,Callado, Luis F.,Rozas, Isabel
, p. 38 - 50 (2017)
Searching for improved antagonists of α2-adrenoceptors, a thorough theoretical study comparing the aromaticity of phenyl-, pyridinyl-, thiophenyl- and thiazolylguanidinium derivatives has been carried out [at M06-2X/6–311++G(p,d) computational level] confirming that thiophene and thiazole will be good ‘ring equivalents’ to benzene in these guanidinium systems. Based on these results, a small but chemically diverse library of guanidine derivatives (15 thiophenes and 2 thiazoles) were synthesised to explore the effect that the bioisosteric change has on affinity and activity at α2-adrenoceptors in comparison with our previously studied phenyl derivatives. All compounds were tested for their α2-adrenoceptor affinity and unsubstituted guanidinothiophenes displayed the strongest affinities in the same range as the phenyl analogues. In the case of cycloakyl systems, thiophenes with 6-membered rings showed the largest affinities, while for the thiazoles the 5-membered analogue presented the strongest affinity. From all the compounds tested for noradrenergic activity, only one compound exhibited agonistic activity, while two compounds showed very promising antagonism of α2-adrenoceptors.
Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells
Yu, Meng,Zeng, Minghui,Pan, Zhaoping,Wu, Fengbo,Guo, Li,He, Gu
supporting information, (2020/02/03)
In this study, a series of thieno [2,3-d]pyrimidine derivatives were designed, synthesized and evaluated as novel AKT1 inhibitors. In vitro antitumor assay results showed that compounds 9d-g and 9i potently suppressed the enzymatic activities of AKT1 and
NEW BICYCLIC THIOPHENYLAMIDE COMPOUNDS
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Page/Page column 248; 249, (2014/01/09)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and use thereof as fatty-acid binding protein (FABP) 4/5 inhibitors in the treatment of e.g. type 2 diabetes, atherosclerosis or cancer.
