Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities.
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.
Hafez
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Photochemistry Department, Heterocyclic and Nucleoside Unit, National Research Centre, Dokki, Giza 12622, Egypt. hendnagah2000@yahoo.com
El-Gazzar
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D000528:Alternaria / Q000187:drug effects; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D001241:Aspirin / Q000494:pharmacology; D001409:Bacillus cereus / Q000187:drug effects; D005670:Fusarium / Q000187:drug effects; D007213:Indomethacin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012485:Salmonella typhi / Q000187:drug effects; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C532459:5-ethyl-2-amino-3(4-methyl-1,3-thiazol-2-yl)carbohydrazide-4-methylthiophene-carboxylate; C532457:5-ethyl-2-amino-3-(N-hydroxymethylene-carbohydrazide)-4-methylthiophene-carboxylate; C532458:5-ethyl-2-amino-3-carbonylthiosemicarbazide-4-methylthiophenecarboxylate; D000700:Analgesics; D000890:Anti-Infective Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011743:Pyrimidines; D013876:Thiophenes; D001241:Aspirin; D007213:Indomethacin