Chemistry is an experimental science, Safety of H-Glu(OBzl)-OH, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 1676-73-9, Name is H-Glu(OBzl)-OH, molecular formula is C12H15NO4, belongs to phthalazine compound. In a document, author is Gao, Cheng-Zhi.
A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 +/- 1.25 nM) and MDA-MB-436 cancer cell (11.62 +/- 2.15 mu M), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer’s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 +/- 0.91 mu M) which was stronger than neostigmine (12.01 +/- 0.45 mu M) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer’s disease.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 1676-73-9, in my other articles. Safety of H-Glu(OBzl)-OH.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem