» Articles » PMID: 26186150

Design and Synthesis of Some New Pyrazolyl-pyrazolines As Potential Anti-inflammatory, Analgesic and Antibacterial Agents

Overview
Journal Eur J Med Chem
Specialty Chemistry
Date 2015 Jul 18
PMID 26186150
Citations 16
Authors
Affiliations
Soon will be listed here.
Abstract

In the present study, an efficient synthesis of some new substituted pyrazoline derivatives linked to a substituted pyrazole scaffold was performed by a multistep reaction sequences and compounds were screened for their anti-inflammatory, analgesic and antibacterial activities. The preliminary results revealed that the N-acylated (5e, 5h) and nitro substituted N-phenyl (6f) pyrazolyl-pyrazolines derivatives exhibited a very promising anti-inflammatory activity whereas 5h, 6f were interesting analgesic agents. The compounds with halo substituted phenyl group at C-3 of the pyrazoline ring (4a, 5g, 5h, 6a and 6b) were found to be active against clinical bacterial pathogens with MIC in the range of 0.2-0.4 mg/mL. Compound containing N-propionyl pyrazolyl-pyrazoline (5h) could be identified as the most active member within this study with a dual anti-inflammatory and antibacterial profile. Taken together, this study has led to the development of promising compounds.

Citing Articles

A new polyazomethine-based pyrazole moiety and its reinforced nanocomposites @ ZnO for antimicrobial applications.

Hakami A, Alorfi H, Farghaly T, Hussein M Des Monomers Polym. 2024; 27(1):1-20.

PMID: 38756722 PMC: 11097710. DOI: 10.1080/15685551.2024.2352897.


[3+2]-Cycloaddition of Nitrile Imines to Parabanic Acid Derivatives-An Approach to Novel Spiroimidazolidinediones.

Kuznetsova J, Tkachenko V, Petrovskaya L, Filkina M, Shybanov D, Grishin Y Int J Mol Sci. 2024; 25(1).

PMID: 38203188 PMC: 10778941. DOI: 10.3390/ijms25010018.


2-[5-(2,3-Di-meth-oxy-naphthalen-1-yl)-4,5-di-hydro-1-pyrazol-3-yl]-3-meth-oxy-phenol.

Sung J IUCrdata. 2023; 8(Pt 8):x230668.

PMID: 37693784 PMC: 10483541. DOI: 10.1107/S2414314623006685.


Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies.

Machado V, Cenci A, Teixeira K, Sens L, Tizziani T, Nunes R RSC Med Chem. 2022; 13(12):1644-1656.

PMID: 36561075 PMC: 9749939. DOI: 10.1039/d2md00262k.


Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with antitumor activity towards non-small lung cancer.

Abdelsalam E, Abd El-Hafeez A, Eldehna W, El Hassab M, Marzouk H, Elaasser M J Enzyme Inhib Med Chem. 2022; 37(1):2265-2282.

PMID: 36000167 PMC: 9415638. DOI: 10.1080/14756366.2022.2104841.