66382-08-9Relevant academic research and scientific papers
Facile alkylation of 4-nitrobenzotriazole and its platelet aggregation inhibitory activity
Singh, Dhandeep,Silakari, Om
, p. 5260 - 5267 (2017/10/05)
We explored the facile alkylation of 4-nitrobenzotriazole under basic conditions and the synthesized derivatives were tested for their potential ADP induced platelet aggregation inhibition activity in comparison with standard drug ticagrelor (selective P2Y12 inhibitor). The nitro group at 4-position is highly activating toward alkylation reactions (under strong basic conditions) and resulted in formation of degradation product like 3-nitrobenzene-1,2-diamine which make isolation of alkyl products very difficult. We optimized the reaction under mild basic condition (potassium carbonate and DMF) which is devoid of any degradation product. This is perhaps the first report of 4-nitrobenzotriazole derivatives possessing platelet aggregation inhibitory activity. Generally activity increases with increase in length of alkyl chain and 1-alkyl positional isomers were found to be more potent than 2-alkyl isomers. The benzoyl derivative was found to be the most potent [compound 22; (4-Nitro-1H-benzotriazol-1-yl)(phenyl)methanone; IC50 = 0.65 ± 0.10 mM] which may be attributed to electronegative oxygen atom and aromatic ring. Benzyl derivatives [compound 20; 1-Benzyl-4-nitro-1H-benzotriazole; IC50 = 0.81 ± 0.08 mM, compound 21; 2-Benzyl-4-nitro-2H-benzotriazole; IC50 = 0.82 ± 0.19 mM] and sulfonyl derivative [compound 23; 1-[(4-Methylphenyl)sulfonyl]-4-nitro-1H-benzotriazole; IC50 = 0.82 ± 0.19 mM] are also found to be highly active. Furthermore, all compounds possess P2Y12 binding affinity as confirmed by VASP/P2Y12 phosphorylation assay.
Synthesis and anti-mycobacterial activities of triazoloquinolones
Carta, Antonio,Palomba, Michele,Briguglio, Irene,Corona, Paola,Piras, Sandra,Jabes, Daniela,Guglierame, Paola,Molicotti, Paola,Zanetti, Stefania
experimental part, p. 320 - 326 (2011/02/26)
A number of quinolone derivatives have been reported to possess anti-mycobacterial activity. Generally. Mycobacterium tuberculosis isolates expressing resistance to both isoniazid and rifampin are susceptible to fluoroquinolones. Benzotriazole is a hetero
1H- and 2H-Benzotriazoles
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, (2008/06/13)
This invention relates to novel 1H- and 2H-benzotriazoles. These benzotriazoles are useful as herbicidal agents for the control of undesirable broadleaf weeds and grass weeds and may be applied to the foliage of undesirable plants or to soil containing seeds of said undesirable plants in order to obtain the control thereof.
