Literature DB >> 18783947

Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities.

H N Hafez1, A B A El-Gazzar.   

Abstract

Two series of 5-ethyl-2-amino-3-pyrazolyl-4-methylthiophenecarboxylate and 2-thioxo-N(3)-aminothieno[2,3-d]pyrimidines were prepared from 3,5-diethyl-2-amino-4-methylthio-phenecaboxylate and evaluated as anti-inflammatory, analgesic and ulcerogenic activities. Among the compounds studied, compounds which containing the substituted hydrazide at C-3 position 7, 16, and 17a showed more potent anti-inflammatory and analgesic activities than the standard drug (Indomethacin and Aspirin), along without ulcerogenity. While compounds 2, 5, 9, 10, and 11c showed moderate activities. Some of the newly synthesized compounds have good to excellent antimicrobial activity.

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Year:  2008        PMID: 18783947     DOI: 10.1016/j.bmcl.2008.08.071

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Tau as a therapeutic target in neurodegenerative disease.

Authors:  Diana S Himmelstein; Sarah M Ward; Jody K Lancia; Kristina R Patterson; Lester I Binder
Journal:  Pharmacol Ther       Date:  2012-07-10       Impact factor: 12.310

2.  2-Amino-4,5,6,7-tetra-hydro-benzo[b]thio-phene-3-carbonitrile.

Authors:  Willams L Silva; Maria do Carmo A de Lima; Suely L Galdino; Ivan R Pitta; Carlos A De Simone
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-11-02

3.  Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidine derivatives.

Authors:  Mohamed A M Abdel Reheim; Safaa M Baker
Journal:  Chem Cent J       Date:  2017-11-02       Impact factor: 4.215

4.  Antimicrobial Activity of Some Novel Armed Thiophene Derivatives and Petra/Osiris/Molinspiration (POM) Analyses.

Authors:  Yahia Nasser Mabkhot; Fatima Alatibi; Nahed Nasser E El-Sayed; Salim Al-Showiman; Nabila Abdelshafy Kheder; Abdul Wadood; Abdur Rauf; Saud Bawazeer; Taibi Ben Hadda
Journal:  Molecules       Date:  2016-02-17       Impact factor: 4.411

5.  Molecular design, synthesis and in vitro biological evaluation of thienopyrimidine-hydroxamic acids as chimeric kinase HDAC inhibitors: a challenging approach to combat cancer.

Authors:  Mona M Abdel-Atty; Nahla A Farag; Rabah A T Serya; Khaled A M Abouzid; Samar Mowafy
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

6.  Pyrazole carbohydrazide derivatives of pharmaceutical interest.

Authors:  Luiza Rosaria Sousa Dias; Raquel Rocha Silva Salvador
Journal:  Pharmaceuticals (Basel)       Date:  2012-03-16
  6 in total

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