Aim and Objective: We reported in this manuscript, synthesis of novel pyrazolopyrazinothienopyrimidines.
The o-amino-thienopyrazolopyrazine-carbonitrile 4 was used as a versatile precursor for synthesis
of new heterocyclic compounds. Due to development of resistance to the current antimicrobial therapy and
non-steroidal anti-inflammatory drugs (NSAIDs), continues research for more effective agents is interesting.
Hence, the suspected promising biological activities of pyrazolopyrazine compounds persuaded us to study the
anti-microbial and anti-inflammatory activities in comparison with standard drugs.
Materials and Methods: The chemical structures of the newly synthesized compounds were confirmed by
elemental and spectral analyses. Activities of the synthesized compounds against a number of Gram-negative
and Gram-positive bacterial strains were investigated. The fungal strains were obtained from some cases of
human dermatophytosis. The antimicrobial activities were determined according to the Kwon-Chung and
Bennett method. Anti-inflammatory activity was evaluated using carrageenan induced paw edema method.
Results: The antibacterial screening of the synthesized compounds represented that the o-amino-carbonitrile 4
and triazepinone 11 have the highest activity towards E. coli & S. aureus and S. pneumonia. The amino-imino
6 was very effective against E. coli. Ring closure of 6 to triazolopyrimidine 7 increases the antibacterial activity
against E. coli & K. pneumonia, their inhibition zones were higher than ciprofloxacin. Also, the triazolopyrimidines
7 and 10 exhibited high antifungal activity against all tested strains. Compounds 6 and 11 revealed
high antifungal activity against S. racemosum and T. rubrum. The anti-inflammatory activity data indicated
that all the tested compounds 4, 6, 7, 10 & 11 revealed the highest anti-inflammatory effect after 4 hrs. of
Conclusion: we found that most of the examined novel thieno- pyrazolopyrazine compounds exhibited promising
antibacterial, antifungal and anti-inflammatory activities which can be used as potential antibacterial,
antifungal and anti-inflammatory drugs.
Keywords: Thienopyrazolopyrazine, pyrimidine, triazole, triazepine, synthesis, antimicrobial activity, anti-inflammatory activity., Thienopyrazolopyrazine, pyrimidine, triazole, triazepine, synthesis, antimicrobial activity, anti-inflammatory activity.
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