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      Microwave-Assisted Synthesis of some Novel Azoles and Azolopyrimidines as Antimicrobial Agents

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          Abstract

          In this study, new derivatives of pyrazole, isoxazole, pyrazolylthiazole, and azolopyrimidine having a thiophene ring were synthesized under microwave irradiation. Their pharmacological activity toward bacteria and fungi inhibition was screened and compared to the references Chloramphenicol and Trimethoprim/ sulphamethoxazole. The antimicrobial results of the investigated compounds revealed promising results and some derivatives have activities similar to the references used.

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          Synthesis of heterocycles. Part II. New routes to acetylthiadiazolines and alkylazothiazoles

          N. F. Eweiss, A. Osman (1980)
          Article 0 comments Cited 42 times – based on 0 reviews     Review now
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            Synthesis of some thiazolyl-pyrazoline derivatives and preliminary investigation of their hypotensive activity.

            G Turan-Zitouni (2000)
            Some 1-(4-arylthiazol-2-yl)-3,5-diaryl-2-pyrazoline derivatives were synthesized by reacting 1-thiocarbamoyl-3,5-diaryl-2-pyrazoline derivatives with phenacetylbromide in ethanol. The structural elucidation of the compounds were performed by IR, 1H-NMR and Mass spectral data and elemental analyses. The hypotensive activities of 13 compounds were evaluated by using the tail-cuff method. All examined compounds showed appreciable hypotensive activities. Clonidine was used as reference substance in the pharmacological evaluation.
            Article 0 comments Cited 29 times – based on 0 reviews     Review now
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              Synthesis, biological evaluation and molecular modeling study of pyrazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.

              Ashish Kumar Tewari, Ved Singh, Pratima Yadav … (2014)
              A novel series of pyrazole derivatives were synthesized and evaluated in vivo for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Among all compounds, 5a, and 5b showed comparable anti-inflammatory activity to Nimesulide, the standard drug taken for the studies. In silico (docking) studies were carried out to investigate the theoretical binding mode of the compounds to target the cyclooxygenase (COX-2) using Autodock 4.2.
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                Author and article information

                Contributors
                Panayiotis A. Koutentis: Role: Academic Editor
                Derek J. McPhee: Role: Academic Editor
                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): 23 February 2017
                Publication date Collection: March 2017
                Volume: 22
                Issue: 3
                Electronic Location Identifier: 346
                Affiliations
                [1 ]Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt; s.m.gomha@ 123456gmail.com (S.M.G.); amaaniq21@ 123456yahoo.com (A.M.G.M.)
                [2 ]Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah-Al-mukkarramah 21514, Saudi Arabia
                [3 ]Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh-11451, Saudi Arabia
                [4 ]Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah B.O. 208203, Saudi Arabia, mohiem@ 123456yahoo.com
                Author notes
                [* ]Correspondence: thoraya-f@ 123456hotmail.com (T.A.F.); yahia@ 123456ksu.edu.sa (Y.N.M.); Tel.: +20-1006-745-618 (T.A.F.); +966-11-467-5898 (Y.N.M.); Fax: +966-11-467-5992 (Y.N.M.)
                Article
                Publisher ID: molecules-22-00346
                DOI: 10.3390/molecules22030346
                PMC ID: 6155381
                PubMed ID: 28241500
                SO-VID: fe04a4c4-e53c-4985-9dcc-b1df110331d5
                Copyright © © 2017 by the authors.
                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 : 01 January 2017
                Date accepted : 21 February 2017
                Categories
                Subject: Article

                Keywords: thiophenes,pyrazoles,thiazoles,antimicrobial activity,microwave irradiation
                Data availability:
                Keywords: thiophenes, pyrazoles, thiazoles, antimicrobial activity, microwave irradiation

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