Synthesis and biological evaluation of 3N-substituted-thieno[2,3-d] pyrimidines

Veena K; Shravan. L. Nargund; Shachindra. L. Nargund; J. N. Narendra Sharath Ch; L. V. G. Nargund

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Synthesis and biological evaluation of 3N-substituted-thieno[2,3-d] pyrimidines

机译：3N-取代的噻吩并[2,3-d]嘧啶的合成及生物学评价

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To counteract the resistance produced by microbes there is a need to invent new drugs, which are more safe and effective. In many cases heterocyclic fusion with pyrimidine ring resulted in compounds with wide spectrum of biological activities. Thienopyrimidines, the structural analogues of biogenic purine class, undoubtedly, has high significance in the field of pharmaceutical and biotechnological sciences, with wide spectrum of biological activities. In continuation of our research program to find out bioactive thienopyrimidines, the present work is an effort towards the synthesis, characterisation and evaluation of 3-substituted-thieno[2,3-d]pyrimidine-4-ones for their antibacterial, anti-inflammatory and antioxidant activity. Three compounds (6a, 6d, 7f) were found to possess moderate anti-bacterial activity against both micro-organisms when compared to Procaine penicillin (gram +ve) and Streptomycin (gram –ve). Compounds 6a, 6c and 7a were found to possess good anti-inflammatory activity when compared to Diclofenec sodium. The study regarding anti oxidant activity shown that thienopyrimidines are not anti-oxidants. Further lead optimization should be carried out for the better expected anti-inflammatory or antibacterial activity.

机译：为了抵消微生物产生的抗药性，需要发明更安全有效的新药。在许多情况下，与嘧啶环的杂环融合会产生具有广泛生物活性的化合物。硫代嘧啶，一种生物嘌呤类的结构类似物，无疑在制药和生物技术科学领域具有重要的意义，具有广泛的生物活性。在继续我们的研究计划以发现具有生物活性的噻吩并嘧啶类药物方面，目前的工作是努力合成，表征和评估3-取代的噻吩并[2,3-d]嘧啶-4-酮类化合物的抗菌，消炎作用。和抗氧化活性。与普鲁卡因青霉素（克+ ve）和链霉素（克-ve）相比，发现三种化合物（6a，6d，7f）对两种微生物均具有中等的抗菌活性。与双氯芬酸钠相比，发现化合物6a，6c和7a具有良好的抗炎活性。关于抗氧化剂活性的研究表明，噻吩并嘧啶不是抗氧化剂。为了更好地预期抗炎或抗菌活性，应进行进一步的铅优化。

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《Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry》 |2012年第2期|共6页
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Veena K; Shravan. L. Nargund; Shachindra. L. Nargund; J. N. Narendra Sharath Ch; L. V. G. Nargund;
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Synthesis and biological evaluation of 3N-substituted-thieno[2,3-d] pyrimidines

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