361340-57-0Relevant academic research and scientific papers
Sedinafine derivatives of the microwave-assisted method for preparing
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, (2016/12/07)
The invention discloses a microwave-assisted synthesis method of sildenafil derivatives, which mainly comprises the following steps: by using 2-alkoxybenzoic acid and 4-amino-1-methyl-3-n-propyl-1H-pyrazolyl-5-formamide as initial raw materials, carrying out amidation, cyclization, mononitration, nitro reduction, guanidylation and the like to obtain the sildenafil derivatives. The method greatly shortens the reaction time, enhances the reaction efficiency, has the advantages of high yield and high purity, is simple to operate and easy to control, and is beneficial to industrial production of sildenafil analogs.
Synthesis and phosphodiesterase 5 inhibitory activity of new 5-phenyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one derivatives containing an N-acylamido group on a phenyl ring
Kim, Dae-Kee,Ryu, Do Hyun,Lee, Namkyu,Lee, Ju Young,Kim, Jae-Sun,Lee, Sukho,Choi, Jin-Young,Ryu, Je-Ho,Kim, Nam-Ho,Im, Guang-Jin,Choi, Won-Son,Kim, Tae-Kon
, p. 1895 - 1899 (2007/10/03)
New sildenafil analogues with an N-acylamido group at the 5′-position of the phenyl ring, 6a-e, were prepared from the readily available starting compound 2 in four straightforward steps. Enzyme assays demonstrated that all the target compounds 6a-e showed higher PDE5 inhibitory activities than sildenafil. It was observed that the PDE5 inhibitory activity was enhanced as the chain length of R group increased, but introduction of the branched alkyl groups such as isopropyl (6d) and cyclohexyl (6e) resulted in the drop of potency compared with 6c. In particular the N-butyrylamido derivative 6c exhibited the highest PDE5 inhibitory activity, and was about 6-fold more potent than sildenafil. However, all the compounds exhibited somewhat weak selectivity (1-3-fold) over PDE6, indicating that the compounds 6a-e have intrinsically lower selectivity than sildenafil. Copyright
