Literature DB >> 26186150

Design and synthesis of some new pyrazolyl-pyrazolines as potential anti-inflammatory, analgesic and antibacterial agents.

Shivapura Viveka1, Prasanna Shama2, Gundibasappa Karikannar Nagaraja3, Shuvankar Ballav4, Savita Kerkar4.   

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.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-inflammatory activity; Antibacterial activity; Drug design; Pyrazolyl-pyrazolines

Mesh:

Substances:

Year:  2015        PMID: 26186150     DOI: 10.1016/j.ejmech.2015.07.002

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  10 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Novel quinolinone-pyrazoline hybrids: synthesis and evaluation of antioxidant and lipoxygenase inhibitory activity.

Authors:  Ioanna Kostopoulou; Antonia Diassakou; Eleni Kavetsou; Eftichia Kritsi; Panagiotis Zoumpoulakis; Eleni Pontiki; Dimitra Hadjipavlou-Litina; Anastasia Detsi
Journal:  Mol Divers       Date:  2020-02-17       Impact factor: 2.943

3.  Synthesis, Spectral Characterization and Fluorescent Assessment of 1,3,5-Triaryl-2-pyrazoline Derivatives: Experimental and Theoretical Studies.

Authors:  Mohammad M Ibrahim; Mahmoud Al-Refai; Khurshid Ayub; Basem F Ali
Journal:  J Fluoresc       Date:  2016-05-24       Impact factor: 2.217

4.  Microwave-assisted synthesis and bioevaluation of new sulfonamides.

Authors:  Halise Inci Gul; Cem Yamali; Fatma Yesilyurt; Hiroshi Sakagami; Kaan Kucukoglu; Ilhami Gulcin; Mustafa Gul; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

5.  Designing, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides.

Authors:  Halise Inci Gul; Ebru Mete; Sakip Emre Eren; Hiroshi Sakagami; Cem Yamali; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-23       Impact factor: 5.051

6.  Synthesis of Anti-Inflammatory Spirostene-Pyrazole Conjugates by a Consecutive Multicomponent Reaction of Diosgenin with Oxalyl Chloride, Arylalkynes and Hydrazines or Hydrazones.

Authors:  Maksim E Mironov; Sergey A Borisov; Tatyana V Rybalova; Dmitry S Baev; Tatyana G Tolstikova; Elvira E Shults
Journal:  Molecules       Date:  2021-12-28       Impact factor: 4.411

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

Authors:  Esraa A Abdelsalam; Amer Ali Abd El-Hafeez; Wagdy M Eldehna; Mahmoud A El Hassab; Hala Mohamed M Marzouk; Mahmoud M Elaasser; Nageh A Abou Taleb; Kamilia M Amin; Hatem A Abdel-Aziz; Pradipta Ghosh; Sherif F Hammad
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

8.  Identification of small molecules that interfere with c-di-GMP signaling and induce dispersal of Pseudomonas aeruginosa biofilms.

Authors:  Jens Bo Andersen; Louise Dahl Hultqvist; Charlotte Uldahl Jansen; Tim Holm Jakobsen; Martin Nilsson; Morten Rybtke; Jesper Uhd; Blaine Gabriel Fritz; Roland Seifert; Jens Berthelsen; Thomas Eiland Nielsen; Katrine Qvortrup; Michael Givskov; Tim Tolker-Nielsen
Journal:  NPJ Biofilms Microbiomes       Date:  2021-07-09       Impact factor: 7.290

9.  Crystal structure of 3,5-dimeth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.

Authors:  Dongsoo Koh
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-09-12

10.  Crystal structure of 3-meth-oxy-2-[5-(naphthalen-1-yl)-4,5-di-hydro-1H-pyrazol-3-yl]phenol.

Authors:  Dongsoo Koh
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-10-07
  10 in total

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