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• 1255771-59-5 tert-butyl (5S)-3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carboxylate 
• 98-88-4 benzoyl chloride 
• 159042-12-3 chalcone benzoylhydrazone 
• 613-94-5 benzoic acid hydrazide 
• 94-41-7 benzalacetophenone 
• 614-47-1 1,3-diphenyl-propen-3-one 

Relevant academic research and scientific papers

Synthesis of some new bioactive 1-N-acid hydrazide substituted pyrazolines

A series of 14 new bioactive 1-N-acid hydrazide substituted pyrazolines were synthesized by cyclization of variably substituted chalcones and different acid hydrazides, using acetic acid as a solvent. The chemical structure of the compounds was characteri

N-formylpyrazolines and N-benzoylpyrazolines as novel inhibitors of mammalian cathepsin B and cathepsin H

Cathepsins, intracellular proteases, are known to be involved in a number of physiological processes ranging from degradation of extracellular proteins, prohormone processing, progressions of atherosclerosis, etc. High levels of cathepsins have been indicated in various pathological conditions like arthritis, cancer and other tissue degenerative disorders. One of the reasons attributed to these high levels is decrease in inhibitor concentration. Therefore, the work on the identification of small molecular weight compounds as inhibitors of cysteine proteases is of great therapeutic significance. Exploring this work in the same direction, we here present the synthesis of substituted N-formylpyrazolines and N-benzoylpyrazolines and study these as inhibitors to cysteine proteases. After a preliminary screening of the compounds as inhibitors to cysteine proteases in general, studies were carried out to study their inhibitory effects on cathepsin B and cathepsin H. SAR studies show that N-formylpyrazolines were better inhibitors than N-benzoylpyrazolines. The most potent inhibitors among the two series were nitro substituted compounds 1i and 2i with Ki values of ～1.1 × 10-9 M and 19.5 × 10-8 M for cathepsin B and Ki values of ～5.19 × 10-8 M and 9.8 × 10-7 M for cathepsin H, respectively. Docking experiments showing interaction between N-formylpyrazolines and N-benzoylpyrazolines with enzyme active sites structures also provided useful insights.

N-formylpyrazolines and N-benzoylpyrazolines as novel inhibitors of mammalian cathepsin B and cathepsin H

Cathepsins, intracellular proteases, are known to be involved in a number of physiological processes ranging from degradation of extracellular proteins, prohormone processing, progressions of atherosclerosis, etc. High levels of cathepsins have been indicated in various pathological conditions like arthritis, cancer and other tissue degenerative disorders. One of the reasons attributed to these high levels is decrease in inhibitor concentration. Therefore, the work on the identification of small molecular weight compounds as inhibitors of cysteine proteases is of great therapeutic significance. Exploring this work in the same direction, we here present the synthesis of substituted N-formylpyrazolines and N-benzoylpyrazolines and study these as inhibitors to cysteine proteases. After a preliminary screening of the compounds as inhibitors to cysteine proteases in general, studies were carried out to study their inhibitory effects on cathepsin B and cathepsin H. SAR studies show that N-formylpyrazolines were better inhibitors than N-benzoylpyrazolines. The most potent inhibitors among the two series were nitro substituted compounds 1i and 2i with Kivalues of ～1.1 × 10-9M and 19.5 × 10-8M for cathepsin B and Kivalues of ～5.19 × 10-8M and 9.8 × 10-7M for cathepsin H, respectively. Docking experiments showing interaction between N-formylpyrazolines and N-benzoylpyrazolines with enzyme active sites structures also provided useful insights.

Enantioselective phase-transfer catalysis: Synthesis of pyrazolines

All paired up: Under catalytic phase-transfer conditions the formation of a chiral ion pair between quininium cation 1 and hydrazine anion 2 led to an enantioselective aza-Michael cyclocondensation domino reaction to furnish pyrazolines. A convenient one-pot protocol allowed exchange of the functional group (R1) on the nitrogen atom.

TBD-organocatalysed synthesis of pyrazolines

It was found that TBD, a cheap and commercially available guanidine, easily catalysed the synthesis of biologically important 3,5-diarylpyrazolines from chalcones and acylhydrazines via a selective secondary amine alkylation.

PROCESS FOR PRODUCING NITROGENOUS 5-MEMBERED CYCLIC COMPOUND

A method of the intramolecular and intermolecular cyclization of an N-acylhydrazone for obtaining a pyrazoline skeleton or pyrazolidine skeleton under ordinary conditions with high stereoselectivity and in high yield. An N-acylhydrazone represented by the following formula (I): (wherein R1 and R2 are the same or different and each represents hydrogen or a hydrocarbon group and Ar represents an optionally substituted aromatic hydrocarbon group) is converted to an N-acylpyrazoline derivative with high stereoselectivity in the presence of a Lewis acid catalyst or asymmetric Lewis acid catalyst.