132991-79-8Relevant academic research and scientific papers
Synthesis, in silico docking experiments of new 2-pyrrolidinone derivatives and study of their anti-inflammatory activity
Moutevelis-Minakakis, Panagiota,Papavassilopoulou, Eleni,Michas, George,Georgikopoulou, Kalliopi,Ragoussi, Maria-Eleni,Neophytou, Niki,Zoumpoulakis, Panagiotis,Mavromoustakos, Thomas,Hadjipavlou-Litina, Dimitra
experimental part, p. 2888 - 2902 (2011/06/17)
A new class of 2-pyrrolidinone derivatives was designed, synthesized, and tested for their antioxidant and anti-inflammatory activities. The compounds were evaluated for their inhibitory activity against LOX. The most potent among them, 14d [IC50 0.08 (±0.005) mM], and 14e [IC50 0.0705 (±0.003) mM], were also tested in vivo. The compound 14d induced equipotent inhibition against rat paw edema, which is very close to the effect produced by the commonly used standard, namely indomethacin (47%). The LOX inhibitory activity of the compound 14e proceeds in parallel to the % inhibitory value of lipid peroxidation meaning that this LOX inhibitory activity is supported by the lipid peroxidation inhibition. The molecular features that govern their bioactivity were explored through in silico docking experiments. The results showed that acidic moieties must be placed in certain distance and orientation in the active site of LOX enzyme in order to productively exhibit inhibitory activity. In addition, the 2-pyrrolidinone template significantly contributes in the inhibitory properties of the new compounds.
Design and synthesis of novel antihypertensive drugs
Moutevelis-Minakakis,Gianni,Stougiannou,Zoumpoulakis,Zoga,Vlahakos,Iliodromitis,Mavromoustakos
, p. 1737 - 1740 (2007/10/03)
AT1 antagonists constitute a new generation of drugs for the treatment of hypertension and are designed and synthesized to mimic the C-terminal segment of Angiotensin II (Ang II) and to block its binding action on AT1 receptor. For this reason, the conformational analysis of Ang II and its derivatives as well as the AT1 antagonists belonging to SARTANs class of molecules were studied. Such studies offer the possibility to reveal the stereoelectronic factors responsible for bioactivity of AT1 antagonists and to design and synthesize new analogues with better pharmacological and financial profiles. An example of a novel synthetic non-peptide molecule is given which mimics the His6-Pro7-Phe8 part of Ang II and is based on the (S)-pyroglutamic acid.
Peptide Mimetics of Thyrotropin-Releasing Hormone Based on a Cyclohexane Framework: Design, Synthesis, and Cognition-Enhancing Properties
Olson, Gary L.,Cheung, Ho-Chuen,Chiang, Elliot,Madison, Vincent S.,Sepinwall, Jerry,et al.
, p. 2866 - 2879 (2007/10/02)
The design and synthesis of peptide mimetics of thyrotropin-releasing hormone (TRH) in which the peptide backbone is entirely replaced by a cyclohexane framework are described.The cis-1,3,5-trisubstituted ring was expected to permit key pharmacophoric gro
