20050-82-2Relevant academic research and scientific papers
Combatting AMR: A molecular approach to the discovery of potent and non-toxic rhenium complexes active against C. albicans-MRSA co-infection
Crochet, Aurélien,Pavic, Aleksandar,Radakovic, Natasa,Roch, Paul,Sovari, Sara Nasiri,Zobi, Fabio
supporting information, (2021/09/28)
Antimicrobial resistance (AMR) is a major emerging threat to public health, causing serious issues in the successful prevention and treatment of persistent diseases. While the problem escalates, lack of financial incentive has lead major pharmaceutical co
7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor
Xiao, Zhangping,Chen, Deng,Song, Shanshan,Van Der Vlag, Ramon,Van Der Wouden, Petra E.,Van Merkerk, Ronald,Cool, Robbert H.,Hirsch, Anna K. H.,Melgert, Barbro N.,Quax, Wim J.,Poelarends, Gerrit J.,Dekker, Frank J.
, p. 11920 - 11933 (2020/11/26)
Macrophage migration inhibitory factor (MIF) is a cytokine with key roles in inflammation and cancer, which qualifies it as a potential drug target. Apart from its cytokine activity, MIF also harbors enzyme activity for keto-enol tautomerization. MIF enzymatic activity has been used for identification of MIF binding molecules that also interfere with its biological activity. However, MIF tautomerase activity assays are troubled by irregularities, thus creating a need for alternative methods. In this study, we identified a 7-hydroxycoumarin fluorophore with high affinity for the MIF tautomerase active site (Ki = 18 ± 1 nM) that binds with concomitant quenching of its fluorescence. This property enabled development of a novel competition-based assay format to quantify MIF binding. We also demonstrated that the 7-hydroxycoumarin fluorophore interfered with the MIF-CD74 interaction and inhibited proliferation of A549 cells. Thus, we provide a high-affinity MIF binder as a novel tool to advance MIF-oriented research.
Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds
Jalili-Baleh, Leili,Forootanfar, Hamid,Kü?ükk?l?n?, Tuba Tüylü,Nadri, Hamid,Abdolahi, Zahra,Ameri, Alieh,Jafari, Mandana,Ayazgok, Beyza,Baeeri, Maryam,Rahimifard, Mahban,Abbas Bukhari, Syed Nasir,Abdollahi, Mohammad,Ganjali, Mohammad Reza,Emami, Saeed,Khoobi, Mehdi,Foroumadi, Alireza
, p. 600 - 614 (2018/06/26)
A novel series of coumarin-lipoic acid conjugates were synthesized via cycloaddition click reaction to find out new multi-target-directed ligands (MTDLs) for treatment of Alzheimer's disease (AD). All of synthesized compounds were screened for neuroprotec
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents
Montanari, Serena,Scalvini, Laura,Bartolini, Manuela,Belluti, Federica,Gobbi, Silvia,Andrisano, Vincenza,Ligresti, Alessia,Di Marzo, Vincenzo,Rivara, Silvia,Mor, Marco,Bisi, Alessandra,Rampa, Angela
supporting information, p. 6387 - 6406 (2016/07/26)
The modulation of the endocannabinoid system is emerging as a viable avenue for the treatment of neurodegeneration, being involved in neuroprotective and anti-inflammatory processes. In particular, indirectly enhancing endocannabinoid signaling to therapeutic levels through FAAH inhibition might be beneficial for neurodegenerative disorders such as Alzheimer's disease, effectively preventing or slowing the progression of the disease. Hence, in the search for a more effective treatment for Alzheimer's disease, in this paper, the multitarget-directed ligand paradigm was applied to the design of carbamates able to simultaneously target the recently proposed endocannabinoid system and the classic cholinesterase system, and achieve effective dual FAAH/cholinesterase inhibitors. Among the two series of synthesized compounds, while some derivatives proved to be extremely potent on a single target, compounds 9 and 19 were identified as effective dual FAAH/ChE inhibitors, with well-balanced nanomolar activities. Thus, 9 and 19 might be considered as new promising candidates for Alzheimer's disease treatment.
Modified coumarins. 29. Synthesis of structural analogs of natural 6-arylfuro[3,2-g]chromen-7-ones
Garazd,Garazd,Ogorodniichuk,Khilya
experimental part, p. 158 - 163 (2009/12/06)
3-Substituted 6-arylfuro[3,2-g]chromen-7-ones, structural analogs of natural furocoumarins, were synthesized by linear annelation of a furan fragment to a 3-arylcoumarin system.
Synthesis and binding affinity of 3-aryl-7-hydroxycoumarins to human α and β estrogen receptors
Kirkiacharian,Lormier,Resche-Rigon,Bouchoux,Cérède
, p. 51 - 56 (2007/10/03)
The synthesis of a set of substituted 3-aryl-7-hydroxycoumarins was performed. The study of the relations between their structure and their relative binding affinity (RBA) to human α and β estrogen receptors was achieved.
