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...
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Veröffentlicht in: | Bioorganic & medicinal chemistry 2008-10, Vol.18 (19), p.5222-5227 |
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Sprache: | eng |
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Zusammenfassung: | 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.
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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ISSN: | 0960-894X 0968-0896 1464-3405 1464-3391 |
DOI: | 10.1016/j.bmcl.2008.08.071 |