56983-72-3

Upstream product

• 119-36-8 methyl salicylate 
• 70203-02-0 N'-(2-phenyl-2-ethylidene)-2-hydroxybenzohydrazide 
• 936-02-7 2-Hydroxybenzoylhydrazine 
• 106275-60-9 3-salicyloylhydrazono-butyric acid ethyl ester 
• 141-97-9 ethyl acetoacetate 

Downstream Products

• 124524-87-4 1-(2-Hydroxy-benzoyl)-3,4-dimethyl-1H-pyrano[2,3-c]pyrazol-6-one 
• 213010-83-4 2-(2-Hydroxy-benzoyl)-4-[1-(4-methoxy-phenyl)-meth-(Z)-ylidene]-5-methyl-2,4-dihydro-pyrazol-3-one 
• 1218782-86-5 N'-((1-(2-hydroxybenzoyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)methyl)isonicotinohydrazide 
• 1218782-90-1 C₁₇H₁₆N₆O₄ 
• 1218782-89-8 C₁₃H₁₃N₇O₃ 
• 1218782-87-6 C₁₉H₁₇N₃O₆ 
• 1218782-88-7 C₁₈H₁₈N₄O₅S 

Relevant academic research and scientific papers

Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations

COX-2 is an inducible enzyme mediating inflammatory responses. Selective targeting of COX-2 is useful for developing anti-inflammatory agents devoid of ulcerogenic activity. Herein, we report the design and synthesis of a series of pyrazoles and pyrazolo[1,2-a]pyridazines with selective COX-2 inhibitory activity and in vivo anti-inflammatory effect. Both series were accessed through acid-catalyzed ultrasound-assisted reactions. The most active compounds in this study are two novel molecules, 11 and 16, showing promising selectivity and decent IC50 of 16.2 and 20.1?nM, respectively. These compounds were also docked into the crystal structure of COX-2 enzyme (PDB ID: 3LN1) to understand their mode of binding. Finally, Mulliken charges and electrostatic surface potential were calculated for both compound 11 and celecoxib using DFT method to get insights into the molecular determinants of activity of this compound. These results could lead to the development of novel COX-2 inhibitors with improved selectivity.

Synthesis and Biological Evaluation of Some Heterocyclic Compounds from Salicylic Acid Hydrazide

Different heterocyclic compounds were prepared starting from 2-hydroxy benzohydrazide; for example, cyclization of hydrazide hydrazone 3 derived from 2-hydroxybenzohydrazide 2 with acetic anhydride or concentrated sulfuric acid gave 1,3,4-oxadiazole derivatives 4–5. On the other hand, direct cyclization of 2-hydroxy benzohydrazide 2 with one carbon cyclizing agent gave a new derivative of 1,3,4-oxadiazole 7, 8, 9, 10, 11. Heating of hydrazide hydrazone 3 with thioglycolic acid in pyridine gave thiazolidinone 12. When 2-hydroxy benzohydrazide 2 reacted with aliphatic carboxylic acids such as formic acid or acetic acid, it gave the corresponding N-formyl or N-acetyl derivatives 6. Subsequent cyclization of 6 using phosphorous pentasulphide in pyridine gave 1,3,4-thiadiazoles 13. Cyclization of 2-hydroxy benzohydrazide with ethyl acetoacetate gives pyrazolone derivative 14. Finally, when an ethanolic solution of acid hydrazide 2 was treated with ammonium thiocyanate in 35% HCl, it gave the thiosemicarbazide 15. Subsequent treatment of 15 with concentrated sulfuric acid or 10% sodium hydroxide gave 5-amino-1,3,4-thiadiazole 16 and 1,2,4-triazole 17, respectively. The structures of all newly isolated compounds were confirmed using1H NMR, IR spectra, and elemental analyses. The antimicrobial activities for all isolated compounds were examined against different microorganisms.

Synthesis and evaluation of some novel substituted 1,3,4-oxadiazole and pyrazole derivatives for antitubercular activity

A series of 1,3,4-oxadiazole and pyrazole derivatives have been synthesized and evaluated for antitubercular activity. All the structures of the newly synthesized compounds have been supported by IR,1H NMR, MS and CHN analysis. All the compounds have shown promising antitubercular activity when compared with the standard drug Streptomycin.

Fused heterocycles: Synthesis and fungistatic activity of some 1- aroyl/aryloxyaceto-4-aryl-5-cyano-3-methyl 1,4,5,6,7-pentahydropyrazolo[4,5- e]pyridin-6-ones and 1-aroyl/aryloxyaceto-4-aryl-3-methyl- 1,4- dihydropyrazolo[4,5-e]pyrido [ 1,2-α]pyrimidines

A number of 1-aroyl/aryloxyaceto-4-aryl-5-cyano-3-methyl 1,4,5,6,7- pentahydropyrazolo[4,5-e] pyridin-6-ones 3 and 1-aroyl/aryloxyaceto-4-aryl- 3-methyl-1,4-dihydropyrazolo[4,5-e]pyrido[1,2-α]pyrimidines 4 have been prepared by Michael addition between α,β-unsaturated ketones 2 and ethyl cyanoacetate/2-arninopyridine in the presence of ammonium acetate. These compounds have been evaluated for their fungistatic activity against P. oryzae, R. solani, P cubensis and P infestans.

STUDIES ON NITROFURAN HETEROCYCLES. PART III. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SOME N-SUBSTITUTED-3-METHYL-4-(5-NITRO-2-FURFURYLIDENE)-2-PYRAZOLIN-5-ONES

The preparation of fourteen new N-substituted-3-methyl-4-(5-nitro-2-furfurylidene)-2-pyrazolin-5-ones is described. These compounds were evalueted for antibacterial activity against both Gram-positive and Gram-negative bacteria. The results of the screeni

Synthesis of Some N1-Substituted-3,5-Dimethyl Pyrazoles and N1-Substituted-3-Methyl-5-Pyrazolones and Related Compounds as Potential Fungicides

Six N1-aroyl/aryloxyacetyl-3,5-dimethylpyrazoles, ten N1-aroyl/aryloxyacetyl-3-methyl-5-pyrazolones, twenty N1-aroyl/aryloxyacetyl-3-methyl-4-arylideno-2-pyrazoline-5-ones and five 1-aryl-1,1-bis1'aroyl/aryl;o