Literature DB >> 19926363

Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives.

Franco Chimenti1, Simone Carradori, Daniela Secci, Adriana Bolasco, Bruna Bizzarri, Paola Chimenti, Arianna Granese, Matilde Yáñez, Francisco Orallo.   

Abstract

A series of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives has been synthesized and assayed for their ability to inhibit the activity of the A and B isoforms of human monoamine oxidase (hMAO). Some of these compounds were endowed with a selective inhibitory activity against hMAO-B in the micromolar range. The most active of the series is the compound 13, N1-thiocarbamoyl-3-(fur-2'-yl)-5-(4'-fluoro-phenyl)-4,5-dihydro-(1H)-pyrazole, with IC(50) 2.75+/-0.81muM value and selectivity ratio of 25, which is the best candidate for further investigations. Copyright 2009 Elsevier Masson SAS. All rights reserved.

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Year:  2009        PMID： 19926363     DOI： 10.1016/j.ejmech.2009.11.003

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


  14 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.  Synthesis, molecular modeling, and in vitro screening of monoamine oxidase inhibitory activities of some novel hydrazone derivatives.

Authors:  Umut Salgin-Gökşen; Nesrin Gökhan-Kelekçi; Samiye Yabanoglu-Çiftci; Kemal Yelekçi; Gülberk Uçar
Journal:  J Neural Transm (Vienna)       Date:  2013-01-18       Impact factor: 3.575

3.  Microwave-assisted green synthesis of 4,5-dihydro-1H-pyrazole-1-carbothioamides in water.

Authors:  Hamid Reza Farmani; Mohammad Hossein Mosslemin; Bahareh Sadeghi
Journal:  Mol Divers       Date:  2018-03-31       Impact factor: 2.943

4.  Evaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives.

Authors:  Umut Salgin-Gökşen; Samiye Yabanoğlu-Çiftçi; Ayşe Ercan; Kemal Yelekçi; Gülberk Uçar; Nesrin Gökhan-Kelekçi
Journal:  J Neural Transm (Vienna)       Date:  2013-01-30       Impact factor: 3.575

5.  Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis.

Authors:  Vishnu Nayak Badavath; İpek Baysal; Gulberk Ucar; Barij Nayan Sinha; Venkatesan Jayaprakash
Journal:  ACS Med Chem Lett       Date:  2015-12-01       Impact factor: 4.345

6.  Study of the antibacterial and antifungal activities of synthetic benzyl bromides, ketones, and corresponding chalcone derivatives.

Authors:  Muhamad Ali K Shakhatreh; Mousa L Al-Smadi; Omar F Khabour; Fatima A Shuaibu; Emad I Hussein; Karem H Alzoubi
Journal:  Drug Des Devel Ther       Date:  2016-11-08       Impact factor: 4.162

7.  2-[3-(4-Chloro-phen-yl)-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thia-zole.

Authors:  Bakr F Abdel-Wahab; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-03-23

8.  5-(4-Fluoro-phen-yl)-3-(4-methyl-phen-yl)-4,5-dihydro-1H-pyrazole-1-carbothio-amide.

Authors:  Bakr F Abdel-Wahab; Hanan A Mohamed; Rizk E Khidre; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-02-16

9.  3-(4-Chloro-phen-yl)-5-(4-fluoro-phen-yl)-4,5-dihydro-1H-pyrazole-1-carbothio-amide.

Authors:  Bakr F Abdel-Wahab; Hanan A Mohamed; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-02-20

10.  2-[5-(4-Fluoro-phen-yl)-3-(4-methyl-phen-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thia-zole.

Authors:  Bakr F Abdel-Wahab; Hanan A Mohamed; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-02-16
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