40294-35-7Relevant academic research and scientific papers
Novel Aryl-Modified Benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides as Potent Inhibitors of Vascular Endothelial Growth Factor Receptors 1 and 2
Ashok, Abhishek,Thanukrishnan, Kannan,Bhojya Naik, Halehatty S.,Maridu, Rajendraswami
, p. 1949 - 1956 (2017/05/29)
Tumor angiogenesis has become an important target for antitumor therapy, with most current therapies aimed at blocking the vascular endothelial growth factor (VEGF) pathway. The VEGF and its receptors have been implicated as key factors in tumor angiogenesis and are major targets in cancer therapy. A series of aryl-modified benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides were synthesized from 2-amino-5,6-dimethoxy benzimidazole and aryl-substituted benzoylamino hetero acids. The new compounds were tested for inhibition of VEGF receptors I and II (VEGFR-1 and VEGFR-2). Compound 6e displayed VEGFR-2 inhibitory activity with a 50% inhibition concentration value as low as 0.020 μM in a homogeneous time-resolved fluorescence enzymatic assay. VEGFR-2 active compounds display good activity against VEGFR-1 as well.
Method of inhibiting the advanced glycosylation of proteins using 1,2-disubstituted-benzimidazoles
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, (2008/06/13)
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, composition is disclosed which comprises 1,2-disubstituted benzimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
NMR studies of N-(benzimidazol-2-yl)pyridinium derivatives: QSAR with the anti-leishmanial activity and their carbon-13 NMR chemical shifts
Alcalde, E,Dinares, I,Frigola, J
, p. 633 - 642 (2007/10/02)
Quantitative structure-activity-relationships between the in vitro anti-leishmanial activity of N-benzimidazolyl-2,4,6-triphenylpyridinium salts 6 and pyridinium benzimidazolate betaines 7 and their 13C-NMR chemical shifts have been studied, in order to ascertain the influence of the benzimidazole substituents upon anti-leishmanial activity.The calculated 13C-chemical shifts allow the selection of a representative subset of compounds.Several new N-benzimidazolylpyridinium derivatives 6 and 7 have been prepared.Among them, 5-methoxy-1-methylbenzimidazole 21 and 6-methoxy-1-methylbenzimidazole 22 derivatives have high anti-leishmanial activity in vitro and compound 22 shows an interesting activity in vivo although host toxicity is present.
