Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

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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.

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The effect of celecoxib, a cyclooxygenase-2 inhibitor, in familial adenomatous polyposis.

G Steinbach, P M Lynch, R K Phillips … (2000)

Patients with familial adenomatous polyposis have a nearly 100 percent risk of colorectal cancer. In this disease, the chemopreventive effects of nonsteroidal antiinflammatory drugs may be related to their inhibition of cyclooxygenase-2. We studied the effect of celecoxib, a selective cyclooxygenase-2 inhibitor, on colorectal polyps in patients with familial adenomatous polyposis. In a double-blind, placebo-controlled study, we randomly assigned 77 patients to treatment with celecoxib (100 or 400 mg twice daily) or placebo for six months. Patients underwent endoscopy at the beginning and end of the study. We determined the number and size of polyps from photographs and videotapes; the response to treatment was expressed as the mean percent change from base line. At base line, the mean (+/-SD) number of polyps in focal areas where polyps were counted was 15.5+/-13.4 in the 15 patients assigned to placebo, 11.5+/-8.5 in the 32 patients assigned to 100 mg of celecoxib twice a day, and 12.3+/-8.2 in the 30 patients assigned to 400 mg of celecoxib twice a day (P=0.66 for the comparison among groups). After six months, the patients receiving 400 mg of celecoxib twice a day had a 28.0 percent reduction in the mean number of colorectal polyps (P=0.003 for the comparison with placebo) and a 30.7 percent reduction in the polyp burden (the sum of polyp diameters) (P=0.001), as compared with reductions of 4.5 and 4.9 percent, respectively, in the placebo group. The improvement in the extent of colorectal polyposis in the group receiving 400 mg twice a day was confirmed by a panel of endoscopists who reviewed the videotapes. The reductions in the group receiving 100 mg of celecoxib twice a day were 11.9 percent (P=0.33 for the comparison with placebo) and 14.6 percent (P=0.09), respectively. The incidence of adverse events was similar among the groups. In patients with familial adenomatous polyposis, six months of twice-daily treatment with 400 mg of celecoxib, a cyclooxygenase-2 inhibitor, leads to a significant reduction in the number of colorectal polyps.

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From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.

Santos Fustero, María Sanchez-Roselló, Pablo Del Barrio-Díaz … (2011)

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Review: biologically active pyrazole derivatives

Anam Ansari, Abad Ali, Mohd Asif … (2017)

Nitrogen-containing heterocyclic compounds and their derivatives have historically been invaluable as a source of therapeutic agents. Nitrogen-containing heterocyclic compounds and their derivatives have historically been invaluable as a source of therapeutic agents. Pyrazole, which has two nitrogen atoms and aromatic character, provides diverse functionality and stereochemical complexity in a five-membered ring structure. In the past decade, studies have reported a growing body of data on different pyrazole derivatives and their innumerable physiological and pharmacological activities. In part, such studies attempted to reveal the wide range of drug-like properties of pyrazole derivatives along with their structure–activity relationships in order to create opportunities to harness the full potentials of these compounds. Here, we summarize strategies to synthesize pyrazole derivatives and demonstrate that this class of compounds can be targeted for the discovery of new drugs and can be readily prepared owing to recent advances in synthetic medicinal chemistry.

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Journal

Journal ID (nlm-ta): Molecules

Journal ID (iso-abbrev): Molecules

Journal ID (publisher-id): molecules

Title: Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

Publisher: MDPI

ISSN (Electronic): 1420-3049

Publication date (Electronic): 12 January 2018

Publication date Collection: January 2018

Volume: 23

Issue: 1

Electronic Location Identifier: 134

Affiliations

[1 ]Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10100 Rabat, Morocco; Khalid.karrouchi@ 123456um5s.net.ma (K.K.); yramli76@ 123456yahoo.fr (Y.R.); jataoufik@ 123456hotmail.com (J.T.); ansarmhammed@ 123456gmail.com (M.A.)

[2 ]LCAE, Department of Chemistry, Faculty of Sciences, University Mohamed I, 60000 Oujda, Morocco

[3 ]Physicochemical Service, Drugs Quality Control Laboratory, Division of Drugs and Pharmacy, Ministry of Health, 10100 Rabat, Morocco

[4 ]Department of Chemistry, Faculty of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; faizalaizari@ 123456yahoo.com

Author notes

[* ]Correspondence: s.radi@ 123456ump.ac.ma or radi_smaail@ 123456yahoo.fr (S.R.); yahia@ 123456ksu.edu.sa (Y.N.M.); Tel.: +212-536-500-601 (S.R.)

Author information

Smaail Radi https://orcid.org/0000-0002-5062-6904

Youssef Ramli https://orcid.org/0000-0002-6885-5692

Yahia N. Mabkhot https://orcid.org/0000-0002-5062-6904

Article

Publisher ID: molecules-23-00134

DOI: 10.3390/molecules23010134

PMC ID: 6017056

PubMed ID: 29329257

SO-VID: 2c90a842-4f4d-4a94-9164-73ff7b513d56

License:

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

History

Date received : 22 November 2017

Date accepted : 05 January 2018

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Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

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Most cited references 400

The effect of celecoxib, a cyclooxygenase-2 inhibitor, in familial adenomatous polyposis.

From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.

Review: biologically active pyrazole derivatives

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