74620-48-7Relevant articles and documents
Discovery of pyridoindole derivatives as potential inhibitors for phosphodiesterase 5A: in silico and in?vivo studies
Mali, Dipak P.,Gaikwad, Dinanath T.,Bhatia, Manish S.,Bhatia, Neela M.
, (2021/05/27)
The aim of this work was to synthesise derivatives from identified plant based pyridoindole lead scaffold, and to assess phosphodiesterase 5A inhibitory potential by in silico and in?vivo. Pyridoindole derivatives were synthesised by using six-stage reactor. In silico screening was carried out by grip-based docking methodology. In step-I, tryptophan as a starting material was reacted with different aldehydes and ketones to obtain 11 molecules. In step-II, obtained molecules were reacted with ethanol and benzyl alcohols to obtain D1 to D22 derivatives. In silico investigation resulted in best three molecules D12, D4 and D8 with promising BE score. Oral acute toxicity study of selected molecules resulted in LD50 value 500 mg/kg in rats. The result of in?vivo antihypertensive study shown that molecule D12 was found to be the best antihypertensive lead molecule. This study could be a best platform to tailor novel biomolecules for inhibiting phosphodiesterase 5A enzyme in hypertension management.
Synthesis and anti-leishmanial activity of 1-aryl-β-carboline derivatives against Leishmania donovani
Gohil, Vikrantsinh M.,Brahmbhatt, Keyur G.,Loiseau, Philippe M.,Bhutani, Kamlesh K.
supporting information; experimental part, p. 3905 - 3907 (2012/07/03)
β-carbolines from various natural and synthetic sources have been known to show diverse biological activities. As a part of our current ongoing project to search for potent natural product-derived anti-leishmanial compounds, we have synthesized a series of substituted 1-aryl-β-carboline derivatives. A total of 22 compounds were synthesized and tested in vitro against Leishmania donovani, out of which 6 compounds (4, 5, 10, 11, 19 and 22) showed notably more activity than the standard miltefosine (IC50 12.07 ± 0.82 μM), with compound 4 being the most potent (IC 50 2.16 ± 0.26 μM).
β-Carbolines as specific inhibitors of cyclin-dependent kinases
Song, Yongcheng,Wang, Jian,Teng, Su Fern,Kesuma, Djohan,Deng, Yu,Duan, Jinao,Wang, Jerry H.,Qi, Robert Zhong,Sim, Mui Mui
, p. 1129 - 1132 (2007/10/03)
Harmine (3), 7-fluoro-1-methyl β-carboline (35) and 1-(5-methyl-imidazol-4-yl) β-carboline (41) were potent and specific inhibitors of cyclin-dependent kinases. The degree of aromaticity of the tricyclic ring and the positioning of substituents are important for inhibitory activity. While most β-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) β-carbolines.