Catalytic Enantioselective Intramolecular Aza‐Michael Addition to α,β‐Unsaturated Esters
A general method for accessing enantioenriched saturated N‐heterocycles via a catalytic enantioselective intramolecular aza‐Michael reaction to α,β‐unsaturated esters is described. A superbasic bifunctional iminophosphorane (BIMP) catalyst was key to enabling reactivity of the high pKa sulfonamide pronucleophile, whilst delivering good to excellent ...
Evan G. W. Rutter +5 more
wiley +2 more sources
(4Z)-4-[(2E)-1-Hydroxy-3-(4-methoxyphenyl)prop-2-enylidene]-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one
The title compound, C20H18N2O4, is a chalcone derivative of pyrazole. The pyrazole ring is inclined at a dihedral angle of 19.29 (12)° to the methoxyphenyl ring mean plane, and by 1.19 (13)° to the phenyl ring.
Mukhtar-ul-Hassan +4 more
doaj +1 more source
Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor [PDF]
L-glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a fundamental role in the control of motor function, cognition and mood.
Grove, Simon J .A. +4 more
core +1 more source
Dizajniranje i sinteza novih derivata tiofenkarbohidrazida, tienopirazola i tienopirimidina s antioksidativnim i antitumorskim djelovanjem [PDF]
2-Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene-3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5-amino-4-(3,5-dimethyl-1H-pyrazole-1 ...
A. El-Gazzar +24 more
core +3 more sources
Synthesis, X-Ray Analysis, Anticancer Activity, Computational, and in Silico Studies of New Thiophene Pyrazole Conjugates. [PDF]
Two new thiophene–pyrazole derivatives, 8a and 8b, were synthesized from thiophene 3 precursor and fully characterized. The structure of 8a was confirmed by single‐crystal X‐ray diffraction, which revealed a nonplanar conformation stabilized by NH···O hydrogen bonding and weak intermolecular contacts.
Muhsinah AB +3 more
europepmc +2 more sources
A novel di-Mannich derivative of curcumin pyrazole, 2-[(2,6-dimethyl morpholin-4-yl)methyl]-4-[(E)-2-{3-[(E)-2-{3-[(2,6-dimethylmorpholin-4-yl)methyl]-4-hydroxy-5-methoxyphenyl}ethenyl]-1H-pyrazol-5-yl}ethenyl]-6-methoxyphenol (2), has been synthesized ...
Joko Untung +2 more
doaj +1 more source
The 1H-pyrazole-3-carboxylic acid 2 was converted in good yield (69%) into the corresponding 1H-pyrazole-3-carboxamide 5 via reaction of the acid chloride 3 with 2,3- diaminopyridine (4).
Elif Demir +2 more
doaj +1 more source
Bisdemethoxycurcumin and Its Cyclized Pyrazole Analogue Differentially Disrupt Lipopolysaccharide Signalling in Human Monocyte-Derived Macrophages [PDF]
open11noSeveral studies suggest that curcumin and related compounds possess antioxidant and anti-inflammatory properties including modulation of lipopolysaccharide- (LPS-) mediated signalling in macrophage cell models. We here investigated the effects of
core +1 more source
Biopharmaceutical Profiling of New Antitumor Pyrazole Derivatives [PDF]
Several new pyrazole derivatives have demonstrated promising antiproliferative and cytotoxic effects, but their poor solubility raised concerns over possible biopharmaceutical limitations. In order to improve their pharmaceutical potential we performed the biopharmaceutical profiling for nine pyrazole compounds using in vitro and computational methods.
Valentina Anuta +3 more
openaire +3 more sources
Sonodynamic therapy (SDT) is a non-invasive therapeutic modality in cancer treatment that combines low-intensity ultrasound (US) and sonosensitizers. Tumor cells are destroyed through the synergistic effects of ultrasound and a chemical sonosensitizer ...
Katarzyna Sowa-Kasprzak +5 more
doaj +1 more source

