39730-36-4Relevant academic research and scientific papers
Synthesis, characterization and antimicrobial screening of 1,3-dione with their metal complexes
Sampal, Sandeep N.,Thakur, Shailendrasingh V.,Rajbhoj, Anjali S.,Gaikwad, Suresh T.
, p. 398 - 402 (2018/01/12)
1-(5-Bromo-2-hydroxyphenyl)-3-(thiophen-2-yl)-propane-1,3-dione and its metal complexes has been synthesized. The functionalized 1,3-dione potentially acts as bidentate ligand and coordinate with the transition metal ions through β-diketo system. The synthesized diketone and their transition metal complexes have been screened for in vitro antibacterial and antifungal activity using Resazurin 96 well plate method. The transition metal complexes showed moderate to excellent antimicrobial activity against all tested bacteria and fungi which constitutes a new group of compounds that can be used as potential metal derived drugs.
Discovery of 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol- 9(2H)-one as a phosphodiesterase-5 inhibitor and its complex crystal structure
Shang, Na-Na,Shao, Yong-Xian,Cai, Ying-Hong,Guan, Matthew,Huang, Manna,Cui, Wenjun,He, Lin,Yu, Yan-Jun,Huang, Lei,Li, Zhe,Bu, Xian-Zhang,Ke, Hengming,Luo, Hai-Bin
, p. 86 - 98 (2014/05/06)
Phosphodiesterase-5 (PDE5) inhibitors have been approved for the treatment of erectile dysfunction and pulmonary hypertension, but enthusiasm on discovery of PDE5 inhibitors continues for their potential new applications. Reported here is discovery of a series of new PDE5 inhibitors by structure-based design, molecular docking, chemical synthesis, and enzymatic characterization. The best compound, 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol-9(2H)-one (57), has an IC50 of 17 nM against the PDE5 catalytic domain and good selectivity over other PDE families. The crystal structure of the PDE5 catalytic domain in complex with 57 was determined at 2 A resolution and showed that 57 occupies the same pocket as other PDE5 inhibitors, but has a different binding pattern in detail. On the basis of the binding pattern of 57, a novel scaffold can be proposed as a candidate of PDE inhibitors.
