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Abstract
A series of novel 4-(3,5-dimethyl-1H-pyrazol-1-yl)-2-substituted phenyl/Heterocyclic Thieno[2,3-d] Pyrimidine (8 a-j) derivatives were synthesized by a facile Five-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The structures of the final compounds were confirmed by IR, NMR, EI-MS. The final compounds were screened for their anti-bacterial activity against Bacillus subtilis and Staphylocouccus aureus from Gram positive group of bacteria and Escherichia coli and Klebsiella pneumonia from Gram negative group of bacteria and antifungal activity against Candida albicans and Aspergillus flavus. Anti-bacterial and anti-fungal activities were Evaluated and compared with the standard drugs Such as Amoxicillin and Ketoconazole. From anti-bacterial and antifungal activity screening results, it has been observed that compounds 8i, 8h, 8e and 8j possess good activity.
Highlights
Pyrimidine has always been a unique interesting Heterocyclic moiety for the medicinal chemists; an exhaustive research has been done on the pyrimidines that led to the discovery and introduction of several drugs into the market
Since last four decades research has been focused on the design and synthesis of novel thieno pyrimidines as medicinal agents, a large number of reports have been documented on thieno pyrimidines as they found to exhibit a variety of biological activities such as antimicrobial, anti-inflammatory, bronchodilatory activity, inhibition of Phospodiesterases, tyrosine kinase and VEGFR kinase
The reaction sequences Employed for synthesis of title compounds are shown in
Summary
Pyrimidine has always been a unique interesting Heterocyclic moiety for the medicinal chemists; an exhaustive research has been done on the pyrimidines that led to the discovery and introduction of several drugs into the market. Fused Pyrimidines have been attracted a considerable interest in medicinal chemistry research due to their versatility and a broad bioactive potential. Thieno pyrimidine is among those fused pyrimidines found to have a wide variety of pharmacological and biological applications. Since last four decades research has been focused on the design and synthesis of novel thieno pyrimidines as medicinal agents, a large number of reports have been documented on thieno pyrimidines as they found to exhibit a variety of biological activities such as antimicrobial, anti-inflammatory, bronchodilatory activity, inhibition of Phospodiesterases, tyrosine kinase and VEGFR kinase. As a bio isoster to Purines, thieno[2,3-d] pyrimidines were found to exhibit numerous biological activities probably due to the interaction with various physiological elements
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