Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

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Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-Inflammatory and Analgesic Agents. Synthesis and in Vitro and in Vivo Biological Evaluation

Journal of Medicinal Chemistry ◽

10.1021/jm901269y ◽

2010 ◽

Vol 53 (2) ◽

pp. 723-733 ◽

Cited By ~ 33

Author(s):

Mariangela Biava ◽

Giulio C. Porretta ◽

Giovanna Poce ◽

Claudio Battilocchio ◽

Fabrizio Manetti ◽

...

Keyword(s):

Biological Evaluation ◽

Analgesic Agents ◽

Anti Inflammatory ◽

Derivatives Of

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PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i6.17343 ◽

2017 ◽

Vol 10 (6) ◽

pp. 237 ◽

Cited By ~ 1

Author(s):

Ishwar Bhat K ◽

Abhishek Kumar

Keyword(s):

Acetic Acid ◽

Cytotoxic Activity ◽

Glacial Acetic Acid ◽

Antimalarial Activity ◽

Biological Activities ◽

Cytotoxic Agents ◽

Pyrimidine Derivatives ◽

Pharmacological Activities ◽

Anti Inflammatory ◽

Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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