Literature DB >> 32795767

Recent advancements in the development of bioactive pyrazoline derivatives.

Bhupender Nehra1, Sandeep Rulhania1, Shalini Jaswal1, Bhupinder Kumar1, Gurpreet Singh1, Vikramdeep Monga2.   

Abstract

Pyrazolines remain privileged heterocycles in drug discovery. 2-Pyrazoline scaffold has been proven as a ubiquitous motif which is present in a number of pharmacologically important drug molecules such as antipyrine, ramifenazone, ibipinabant, axitinib etc. They have been widely explored by the scientific community and are reported to possess wide spectrum of biological activities. For combating unprecedented diseases and worldwide increasing drug resistance, 2-pyrazoline has been tackled as a fascinating pharmacophore to generate new molecules with improved potency and lesser toxicity along with desired pharmacokinetic profile. This review aims to summarizes various recent advancements in the medicinal chemistry of pyrazoline based compounds with the following objectives: (1) To represent inclusive data on pyrazoline based marketed drugs as well as therapeutic candidates undergoing preclinical and clinical developments; (2) To discuss recent advances in the medicinal chemistry of pyrazoline derivatives with their numerous biological significances for the eradication of various diseases; (3) Summarizes structure-activity relationships (SAR) including in silico and mechanistic studies to afford ideas for the design and development of novel compounds with desired therapeutic implications.
Copyright © 2020 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anticancer; Antimicrobial; MAO inhibitors; Pyrazoline; SAR; hCA inhibitors

Mesh:

Substances:

Year:  2020        PMID: 32795767     DOI: 10.1016/j.ejmech.2020.112666

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


  6 in total

1.  Design and Synthesis of Carbothioamide/Carboxamide-Based Pyrazoline Analogs as Potential Anticancer Agents: Apoptosis, Molecular Docking, ADME Assay, and DNA Binding Studies.

Authors:  Manish Rana; Md Imam Faizan; Sajad Hussain Dar; Tanveer Ahmad
Journal:  ACS Omega       Date:  2022-06-23

2.  Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights.

Authors:  Tarfah Al-Warhi; Ahmed M El Kerdawy; Mohamed A Said; Amgad Albohy; Zainab M Elsayed; Nada Aljaeed; Eslam B Elkaeed; Wagdy M Eldehna; Hatem A Abdel-Aziz; Miral A Abdelmoaz
Journal:  Drug Des Devel Ther       Date:  2022-05-16       Impact factor: 4.319

3.  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

4.  Copper-Mediated Decarboxylative Coupling of 3-Indoleacetic Acids with Pyrazolones.

Authors:  Kangmei Wen; Yinrong Wu; Jiewen Chen; Jie Shi; Mulin Zheng; Xingang Yao; Xiaodong Tang
Journal:  ACS Omega       Date:  2022-02-02

5.  Synthesis and Evaluation of 1,3,5-Triaryl-2-Pyrazoline Derivatives as Potent Dual Inhibitors of Urease and α-Glucosidase Together with Their Cytotoxic, Molecular Modeling and Drug-Likeness Studies.

Authors:  Rabia Mehmood; Amina Sadiq; Reem I Alsantali; Ehsan Ullah Mughal; Meshari A Alsharif; Nafeesa Naeem; Asif Javid; Munirah M Al-Rooqi; Gul-E-Saba Chaudhry; Saleh A Ahmed
Journal:  ACS Omega       Date:  2022-01-20

6.  Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)-s-triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades.

Authors:  Ihab Shawish; Assem Barakat; Ali Aldalbahi; Azizah M Malebari; Mohamed S Nafie; Adnan A Bekhit; Amgad Albohy; Alamgir Khan; Zaheer Ul-Haq; Matti Haukka; Beatriz G de la Torre; Fernando Albericio; Ayman El-Faham
Journal:  ACS Omega       Date:  2022-07-07
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.