52507-66-1Relevant academic research and scientific papers
Synthesis of arylfurfural oximes and their biological evaluation
Aslam, Samina,Khakwani, Samia,Jnazeer, Areesha,Shahi, Mehrzadi Jnoureen,Yaqoob, Asma,Shafiq, Hamna,Manazer, Rafia,Nasim, Faizul Hassan,Khan, Misbahul Ain
, p. 1210 - 1214 (2016/04/10)
Various oximes of arylfurfural were prepared and characterized through elemental analysis and spectroscopic techniques (FTIR, 1H NMR, 13C NMR and Mass). Synthesized compounds were tested for their antioxidant, tyrosinase and chemotrypson activities.
Discovery of a potent dihydrooxadiazole series of non-ATP-competitive MK2 (MAPKAPK2) inhibitors
Qin, Jun,Dhondi, Pawan,Huang, Xianhai,Aslanian, Robert,Fossetta, James,Tian, Fang,Lundell, Daniel,Palani, Anandan
supporting information; experimental part, p. 100 - 105 (2012/03/27)
Inhibition of MK2 has been shown to offer advantages over that of p38 MAPK in the development of cures for inflammatory diseases such as arthritis. P38 MAPK knockout in mice was lethal, whereas MK2-null mice demonstrated strong inhibition of disease progression in collagen-induced arthritis and appeared normal and viable. However, it is challenging to develop ATP-competitive MK2 inhibitors due to high ATP binding affinity to the kinase. Non-ATP-competitive MK2 inhibitors interact and bind to the kinase in a mode independent of ATP concentration, which could provide better selectivity and cellular potency. Therefore, it is desirable to identify non-ATP-competitive MK2 inhibitors. Through structure optimization of lead compound 1, a novel series of dihydrooxadiazoles was discovered. Additional structure-activity relationship (SAR) study of this series led to the identification of compound 38 as a non-ATP-competitive MK2 inhibitor with potent enzymatic activity and good cellular potency. The SAR, synthesis, and biological data of dihydrooxadiazole series are discussed.
N-hydroxy-5-phenyl-2-furancarboximidamides useful as cardiotonic agents
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, (2008/06/13)
The present invention involves certain N-hydroxy-5-phenyl-2-furancarboximidamides, pharmaceutical compositions containing such compounds, and methods for increasing the contractile force of cardiac muscle of a mammal which comprises systemically administering such compounds to a mammal.
5-Phenyl-2-furamidines: A new chemical class of potential antidepressants
Pong,Pelosi Jr.,Wessels,Yu,Burns,White,Anthony Jr.,Ellis,Wright,White Jr.
, p. 1411 - 1416 (2007/10/02)
A series of 5-phenyl-2-furamidines has been synthesized and evaluated for antidepressant activities. Substitution in the phenyl ring with a nitro (4) or an amino (12) group in the ortho-position resulted in an increase in antidepressant activity. Both 4 and 12 antagonized tetrabenazine-induced ptosis in rodents and inhibited norepinephrine (noradrenaline) uptake into crude synaptosomes of whole mouse brain at doses or concentrations comparable to those of the tricyclic antidepressants. However, these compounds did not possess the anticholinergic and antihistaminic activities common to tricyclic antidepressants. In addition, they lacked monoamine oxidase inhibitory activity. The 5-phenyl-2-furamidines represent a new chemical class of antidepressants and may be useful for depressive patients who cannot tolerate the compromising side effects of the tricyclic antidepressants and monoamine oxidase inhibitors.
5-PHENYL-2-FURAMIDOXIMES
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, (2008/06/13)
A series of 5-phenyl-2-furamidoximes are useful as antidepressants.
