Abstract
Several new thieno[2,3-d] Pyrimidine derivatives 3-Substituted phenyl-5-(thiophen-2-yl) thieno[3,2-e] [1,2,4] triazolo[4,3-c] pyrimidine 7(a-j), were synthesized starting from thieno[2,3-d] pyrimidine-2,4-diol (1). The characterization of the newly synthesized compounds was established by IR, 1H NMR, 13C NMR and Mass Spectral analysis. 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. Antibacterial and anti-fungal activities were Evaluated and compared with the standard drugs. From anti-bacterial and anti-fungal activity screening results, it has been observed that compounds 8i, 8j, 8e 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 thienopyrimidines 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, antiinflammatory, bronchodilatory activity, inhibition of Phospo diesterases, tyrosine kinase and VEGFR kinase
The fusion may occur in three different orientations that results in three important types of thieno pyrimidines namely; Thieno[2,3-d] Pyrimidine (a), thieno[3,2-d] Pyrimidine (b) and thieno[3,4-d] pyrimidine (c) (Figure 1)
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. Since last four decades research has been focused on the design and synthesis of novel thienopyrimidines 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, antiinflammatory, bronchodilatory activity, inhibition of Phospo diesterases, 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. Thieno pyrimidine is a bi cyclic heterocyclic compound consists of a five membered thiophene ring is fused to a six membered hetero cylic ring with two nitrogen atoms. There exist three possible types of fusion of thiophene to pyrimidines ring results in corresponding isomeric thienopyrimidines namely; thieno [2,3-d] pyrimidines, thieno[3,4-d] pyrimidines and thieno[3,2-d] pyrimidines
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