Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.

https://pubs.rsc.org/en/Content/ArticlePDF/2015/CC/C4CC09495F

Combining silver- and organocatalysis: an enantioselective sequential catalytic approach towards pyrano-annulated pyrazoles

An organocatalyzed diastereo- and enantioselective cascade aza-Michael/Michael addition of 2-tosylaminoenones to unsaturated pyrazolones has been developed to afford novel chiral spiropyrazolone tetrahydroquinolines containing three contiguous stereocenters. This cascade reaction proceeded well with 2 mol% chiral bifunctional tertiary amine squaramide catalyst to give the desired products in excellent yields (up to 99%) with excellent diastereoselectivity (up to >25:1 diastereomeric ratio) and high enantioselectivity (up to 91% enantiomeric excess).

Organocatalyzed cascade aza-Michael/Michael addition for the asymmetric construction of highly functionalized spiropyrazolone tetrahydroquinolines.

Antimicrobial activities of 1-phenyl-3-methyl-4-trichloroacetyl-pyrazolone: Experimental, DFT studies, and molecular docking investigation

An efficient chiral squaramide-catalysed enantioselective Michael addition of pyrazolin-5-ones to nitroalkenes has been developed. This reaction afforded the chiral pyrazol-3-ol derivatives in high to excellent yields (up to >99%) with high enantioselectivities (up to 94% ee) for most substrates under very low catalyst loading (0.25 mol%). This catalytic asymmetric reaction provides valuable and easy access to chiral pyrazol-3-ol derivatives, which possess potential pharmaceutical activity.

/pdf/squaramide-catalysed-enantioselective-michael-addition-of-1cnumwldh2.pdf

Squaramide-catalysed enantioselective Michael addition of pyrazolin-5-ones to nitroalkenes

Chemistry of Pyrazolinones and their Applications

A Versatile Synthesis, PM3‐Semiempirical, Antibacterial, and Antitumor Evaluation of Some Bioactive Pyrazoles

Fourteen novel compounds incorporating pyrazolone or pyrazole moieties are synthesized and characterized, including quantum mechanical molecular orbital calculations.

Hamada G. El-Gohary

Papers

Chemistry of Pyrazolinones and their Applications

A Versatile Synthesis, PM3‐Semiempirical, Antibacterial, and Antitumor Evaluation of Some Bioactive Pyrazoles

A Versatile Synthesis, PM3‐Semiempirical, Antibacterial, and Antitumor Evaluation of Some Bioactive Pyrazoles.