57077-20-0Relevant academic research and scientific papers
Synthesis and evaluation of new 1,5-diaryl-3-[4-(methylsulfonyl)phenyl]-4,5-dihydro-1 H-pyrazole derivatives as potential antidepressant agents
?zdemir, Ahmet,Altintop, Mehlika Dilek,Kaplancikli, Zafer Asim,Can, ?zgür Devrim,?zkay, ümide Demir,Turan-Zitouni, Gülhan
, p. 2668 - 2684 (2015)
In an effort to develop potent antidepressant agents, new pyrazoline derivatives 2a-s were synthesized and evaluated for their antidepressant-like activity by tail suspension test (TST) and modified forced swimming test (MFST). The effects of the compound
Design, synthesis and biological evaluation of new 1,3-diphenyl-3-(Phenylamino)propan-1-ones as selective cyclooxygenase (COX-2) inhibitors
Farzaneh, Shabnam,Shahhosseini, Soraya,Arefi, Hadi,Esfahanizadeh, Marjan,Zarghi, Afshin,Daraei, Bahram
, p. 652 - 659 (2018/11/21)
Background: Prostaglandins are a family of eicosanoids biosynthesized from arachi-donic acid through cyclooxygenase (COX) pathway. Two isoforms of COX are well established: COX-1, COX-2. Evidence supports the notion that cyclooxygenase-2, plays a crucial role in some pathological conditions such as inflammation and cancer. Objective: A new group of 1,3-diphenyl-3-(phenylamino)propan-1-ones was designed and synthesized to investigate for their COX-2 inhibitory activity and inhibition of platelet aggregation. Method: Docking study was performed using AutoDock vina software. In vitro COX-1 and COX-2 isozyme inhibition studies were accomplished to obtain structure activity relationship data. The in vitro antiplatelet aggregation activity was determined by turbidimetric procedure. Results: In vitro COX inhibition assay showed that except compound 8c, all derivatives were selective COX-2 inhibitors with IC50 values in the potent 0.20-0.35 μM range with high COX-2 selectivity indexes (SI). Molecular modeling and docking studies indicated that synthesized compounds had a binding similar to that of the known inhibitor SC-558 and the SO2 Me group was inserted into the COX-2 secondary pocket (Val523, Phe518, Ile517, Arg513 and His90) and C=O of the central α, β-unsaturated-carbonyl moiety was oriented toward the entrance to the COX-2 binding site (Tyr355 and Arg120). Conclusion: The 1,3-diphenyl-3-(phenylamino)propan-1-ones are novel COX-2 inhibitors with good COX-2 inhibitory and low affinity for COX-1 isoenzyme. Also our results demonstrated that majority of these compounds inhibited AA-induced platelet aggregation.
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2- pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors
Fioravanti, Rossella,Bolasco, Adriana,Manna, Fedele,Rossi, Francesca,Orallo, Francisco,Ortuso, Francesco,Alcaro, Stefano,Cirilli, Roberto
supporting information; experimental part, p. 6135 - 6138 (2011/01/12)
Eighteen new 1-N-substituted-3,5-diphenyl-2-pyrazoline derivatives have been synthesized and cyclooxygenase (COX-1 and COX-2) inhibitory activities have been evaluated. The results of these biological assays showed that all of new derivatives are not endowed with improved anti-inflammatory activity against COX-1, but some of them showed a good activity against COX-2. To evaluate the binding mode of the most significative compounds (2d, 2f, 2g and 2k) docking studies were carried out. These studies confirmed biological data, in fact these compounds were able to fit into the active site of COX-2.
