26840-48-2Relevant academic research and scientific papers
Synthesis and pharmacological activity of 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazoles
Spasov,Zhukovskaya,Brigadirova,Abbas,Anisimova,Sysoeva,Rashchenko,Litvinov,Mayka, O. Yu.,Babkov,Morkovnik
, p. 1905 - 1912 (2018/02/06)
An efficient method for the synthesis of novel 9H-imidazo[1,2-a]benzimidazole derivatives containing a biphenyl substituent at position 2 was developed. These compounds, belonging to the privileged substructures, have been tested for a wide range of pharmacological activities in the in vitro test panel. It was shown that the synthesized derivatives demonstrated high antioxidant activity, some of them inhibit type 1B protein tyrosine phosphatase, activate AMP-activated protein kinase, possess antiplatelet properties, and a rare and very interesting kind of activity, the ability to break cross-links of glycated proteins. The most active compounds can be suggested for further optimization.
Synthesis, in vitro antiplatelet activity and molecular modelling studies of 10-substituted 2-(1-piperazinyl)pyrimido[1,2-a]benzimidazol-4(10H)-ones
Di Braccio, Mario,Grossi, Giancarlo,Signorello, Maria Grazia,Leoncini, Giuliana,Cichero, Elena,Fossa, Paola,Alfei, Silvana,Damonte, Gianluca
, p. 564 - 578 (2013/05/21)
The multistep preparation of the new 10-substituted 2-(1-piperazinyl) pyrimido[1,2-a]benzimidazol-4(10H)-ones 6a-o, and of the two isomers 10-ethyl-2-(diethylamino)pyrimido[1,2-a]benzimidazol-4(10H)-one 6p and 10-ethyl-4-(diethylamino)pyrimido[1,2-a]benzimidazol-2(10H)-one 13, as well as the in vitro evaluation of their inhibitory activity on human platelet aggregation induced in platelet-rich plasma by ADP, collagen or the Ca 2+ ionophore A23187 were here described. Nine out of fifteen 2-(1-piperazinyl)derivatives (6g-o) showed good inhibitory properties towards all the platelet aggregation agonists used. Moreover, a molecular modelling study has been performed on two of the best compounds of this series (6i and 6o) to confirm in silico their interactions with the catalytic site of human platelet PDE3, using the X-ray data of the PDE3B isoform in complex with an inhibitor.
Synthesis and some conversions of N-substituted benzimidazole-2-sulfonic acids
Divaeva,Kuzmenko,Morkovnik,Komissarov
, p. 463 - 468 (2008/02/02)
A series of N-substituted benzimidazole-2-sulfonic acids was synthesized in good yield by the N-alkylation of benzimidazole-2-sulfonic acids by alkylation with simple and functionalized alkylating agents under mild conditions. The corresponding N-substitu
NOVEL CANNABINOID CB2 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 63-64, (2010/02/11)
Novel selective cannabinoid CB2 receptor ligands, primarily agonists, have a number of biological and pharmacological activities, including bronchial action, immunomodulatory action and analgesia. Hence, they are useful for treating diseases or
