Literature DB >> 29329257

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Khalid Karrouchi1,2,3, Smaail Radi4, Youssef Ramli5, Jamal Taoufik6, Yahia N Mabkhot7, Faiz A Al-Aizari8, M'hammed Ansar9.   

Abstract

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

Entities:  

Keywords:  biological activities; pyrazole derivatives; synthesis

Mesh:

Substances:

Year:  2018        PMID: 29329257      PMCID: PMC6017056          DOI: 10.3390/molecules23010134

Source DB:  PubMed          Journal:  Molecules        ISSN: 1420-3049            Impact factor:   4.411


  303 in total

1.  Novel pyrazole and indazole derivatives: synthesis and evaluation of their anti-proliferative and anti-angiogenic activities.

Authors:  Evangelia Tzanetou; Sandra Liekens; Konstantinos M Kasiotis; Nikolas Fokialakis; Serkos A Haroutounian
Journal:  Arch Pharm (Weinheim)       Date:  2012-06-18       Impact factor: 3.751

2.  Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

Authors:  Dong-Ming Shen; Edward J Brady; Mari R Candelore; Qing Dallas-Yang; Victor D-H Ding; William P Feeney; Guoquiang Jiang; Margaret E McCann; Steve Mock; Sajjad A Qureshi; Richard Saperstein; Xiaolan Shen; Xinchun Tong; Laurie M Tota; Michael J Wright; Xiaodong Yang; Song Zheng; Kevin T Chapman; Bei B Zhang; James R Tata; Emma R Parmee
Journal:  Bioorg Med Chem Lett       Date:  2010-11-21       Impact factor: 2.823

3.  1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.

Authors:  Jiwon Choi; Yunsun Park; Hui Sun Lee; Young Yang; Sukjoon Yoon
Journal:  Bioorg Med Chem       Date:  2010-10-26       Impact factor: 3.641

4.  Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.

Authors:  Alessandro Balbi; Maria Anzaldi; Chiara Macciò; Cinzia Aiello; Mauro Mazzei; Rosaria Gangemi; Patrizio Castagnola; Mariangela Miele; Camillo Rosano; Maurizio Viale
Journal:  Eur J Med Chem       Date:  2011-08-31       Impact factor: 6.514

5.  Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors.

Authors:  Shu-Fu Wang; Yin-Ling Zhu; Ping-Ting Zhu; Jigar A Makawana; Ya-Liang Zhang; Meng-Yue Zhao; Peng-Cheng Lv; Hai-Liang Zhu
Journal:  Bioorg Med Chem       Date:  2014-09-06       Impact factor: 3.641

6.  Novel pyrazole-5-carboxamide and pyrazole-pyrimidine derivatives: synthesis and anticancer activity.

Authors:  Jing Bo Shi; Wen Jian Tang; Xing Bao Qi; Rong Li; Xin Hua Liu
Journal:  Eur J Med Chem       Date:  2014-12-09       Impact factor: 6.514

7.  Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents.

Authors:  Pawan K Sharma; Navneet Chandak; Pawan Kumar; Chetan Sharma; Kamal R Aneja
Journal:  Eur J Med Chem       Date:  2011-02-03       Impact factor: 6.514

8.  Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches.

Authors:  Baptiste Villemagne; Marion Flipo; Nicolas Blondiaux; Céline Crauste; Sandra Malaquin; Florence Leroux; Catherine Piveteau; Vincent Villeret; Priscille Brodin; Bruno O Villoutreix; Olivier Sperandio; Sameh H Soror; Alexandre Wohlkönig; René Wintjens; Benoit Deprez; Alain R Baulard; Nicolas Willand
Journal:  J Med Chem       Date:  2014-05-28       Impact factor: 7.446

9.  Synthesis and antiviral evaluation of some new pyrazole and fused pyrazolopyrimidine derivatives.

Authors:  Aymn E Rashad; Mohamed I Hegab; Randa E Abdel-Megeid; Jehan A Micky; Farouk M E Abdel-Megeid
Journal:  Bioorg Med Chem       Date:  2008-07-02       Impact factor: 3.641

10.  Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues.

Authors:  Jonathan M Large; Simon A Osborne; Ela Smiljanic-Hurley; Keith H Ansell; Hayley M Jones; Debra L Taylor; Barbara Clough; Judith L Green; Anthony A Holder
Journal:  Bioorg Med Chem Lett       Date:  2013-08-11       Impact factor: 2.823

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  54 in total

1.  Davis-Beirut Reaction: Diverse Chemistries of Highly Reactive Nitroso Intermediates in Heterocycle Synthesis.

Authors:  Jie S Zhu; Makhluf J Haddadin; Mark J Kurth
Journal:  Acc Chem Res       Date:  2019-07-22       Impact factor: 22.384

2.  Synthesis and evaluation of tetrahydropyrazolopyridine inhibitors of anion exchange protein SLC26A4 (pendrin).

Authors:  Jie S Zhu; Julia Y Lu; Joseph-Anthony Tan; Amber A Rivera; Puay-Wah Phuan; Marina E Shatskikh; Jung-Ho Son; Peter M Haggie; Alan S Verkman; Mark J Kurth
Journal:  Bioorg Med Chem Lett       Date:  2019-07-03       Impact factor: 2.823

Review 3.  Synthesis of Biologically Active Molecules through Multicomponent Reactions.

Authors:  Daniel Insuasty; Juan Castillo; Diana Becerra; Hugo Rojas; Rodrigo Abonia
Journal:  Molecules       Date:  2020-01-24       Impact factor: 4.411

Review 4.  Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011-2020): Current Status and Future Prospects.

Authors:  Mohammed I El-Gamal; Seyed-Omar Zaraei; Moustafa M Madkour; Hanan S Anbar
Journal:  Molecules       Date:  2022-01-05       Impact factor: 4.411

5.  Multicomponent Pyrazole Synthesis from Alkynes, Nitriles, and Titanium Imido Complexes via Oxidatively Induced N-N Bond Coupling.

Authors:  Adam J Pearce; Robin P Harkins; Benjamin R Reiner; Alexander C Wotal; Rachel J Dunscomb; Ian A Tonks
Journal:  J Am Chem Soc       Date:  2020-02-20       Impact factor: 15.419

6.  Novel Copper(II) Complex with a 4-Acylpyrazolone Derivative and Coligand Induce Apoptosis in Liver Cancer Cells.

Authors:  Marhaba Nurmamat; Haili Yan; Ru Wang; Huixin Zhao; Yanhong Li; Xiaojing Wang; Kaidirye Nurmaimaiti; Tamasha Kurmanjiang; Difang Luo; Jumagul Baodi; Guancheng Xu; Jinyu Li
Journal:  ACS Med Chem Lett       Date:  2021-02-26       Impact factor: 4.345

7.  Novel Pyran-Linked Phthalazinone-Pyrazole Hybrids: Synthesis, Cytotoxicity Evaluation, Molecular Modeling, and Descriptor Studies.

Authors:  M Shaheer Malik; Basim H Asghar; Riyaz Syed; Reem I Alsantali; Moataz Morad; Hatem M Altass; Ziad Moussa; Ismail I Althagafi; Rabab S Jassas; Saleh A Ahmed
Journal:  Front Chem       Date:  2021-05-24       Impact factor: 5.221

8.  Novel pyrazoles as potent growth inhibitors of staphylococci, enterococci and Acinetobacter baumannii bacteria.

Authors:  Ibrahim Alkhaibari; Hansa Raj Kc; Duminduni H Angappulige; David Gilmore; Mohammad A Alam
Journal:  Future Med Chem       Date:  2021-12-08       Impact factor: 3.808

Review 9.  Functional Pyrazolo[1,5-a]pyrimidines: Current Approaches in Synthetic Transformations and Uses As an Antitumor Scaffold.

Authors:  Andres Arias-Gómez; Andrés Godoy; Jaime Portilla
Journal:  Molecules       Date:  2021-05-05       Impact factor: 4.411

Review 10.  Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations.

Authors:  Rafael Fernades Costa; Larissa Córdova Turones; Keilah Valéria Naves Cavalcante; Ismael Aureliano Rosa Júnior; Carlos Henrique Xavier; Lucimar Pinheiro Rosseto; Hamilton Barbosa Napolitano; Patrícia Ferreira da Silva Castro; Marcos Luiz Ferreira Neto; Gustavo Mota Galvão; Ricardo Menegatti; Gustavo Rodrigues Pedrino; Elson Alves Costa; José Luis Rodrigues Martins; James Oluwagbamigbe Fajemiroye
Journal:  Front Pharmacol       Date:  2021-05-10       Impact factor: 5.810

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