Background: From the literature it is known that many derivatives of fused thienopyrimidines and furopyrimidines possess broad spectrum of biological activity.

Objectives: The current studies describe the synthesis and evaluation of antimicrobial activity of some new N-1,3-thiazol-2-ylacetamides of pyrido[3',2':4,5]furo(thieno)[3,2-d]pyrimidines.

Methods: By cyclocondensation of ethyl 1-aminofuro(thieno)[2,3-b]pyridine-2-carboxylates 1with formamide were converted to the pyrido[3',2':4,5]furo(thieno)[3,2-d]pyrimidin-7(8)-ones 2.Alkylation of compound 2 with 2-chloro-N-1,3-thiazol-2-ylacetamide led to the aimed N-1,3-thiazol-2-ylaceta-mides of pyrido[3',2':4,5]furo(thieno)[3,2-d]pyrimidines 3. Starting from compound 2 the relevant S-alkylated derivatives of pyrido[3',2':4,5]furo(thieno)[3,2-d]pyrimidines 6 were also synthesized.

Results: All the compounds showed antibacterial activity to non-resistant strains. Compounds 3a-3m showed antibacterial activity with MIC/MBC at 0.08-2.31 mg/mL/0.11-3.75 mg/mL .The two most active compounds, 3j and 6b, appeared to be more active towards MRSA than the reference drugs. Half of the tested compounds appeared to be equipotent/more potent than ketoconazole and more potent than bifonazole. The docking analysis provided useful information about the interactions occurring between the tested compounds and the different enzymes.

Conclusion: Gram-negative and Gram-positive bacteria and fungi showed different response towards tested compounds, indicating that different substituents may lead to different modes of action or that the metabolism of some bacteria/fungi was better able to overcome the effect of the compounds or adapt to it.

背景：从文献中知道，稠合的噻吩并嘧啶和呋喃并嘧啶的许多衍生物具有广谱的生物活性。

目的：目前的研究描述了一些新的吡啶并[3'，2'：4,5]呋喃（thieno）[3,2-d] N-1,3-噻唑-2-基乙酰胺的合成和抗菌活性评估]嘧啶。

方法：通过将1-氨基呋喃乙酯（噻吩）[2,3-b]吡啶-2-甲酸乙酯与甲酰胺进行环缩合，将吡啶[3'，2'：4,5]呋喃（噻吩）[3,2] -d]嘧啶7（8）-酮2.化合物2与2-氯-N-1,3-噻唑-2-基乙酰胺的烷基化反应生成目标N-1,3-噻唑-2-基乙酰胺吡啶基[3'，2'：4,5]呋喃（硫代）[3,2-d]嘧啶3的合成。从化合物2开始，吡啶基[3'，2'：4,5]的相关S-烷基化衍生物还合成了呋喃（噻吩）[3，2-d]嘧啶6。

结果：所有化合物对非耐药菌株均具有抗菌活性。化合物3a-3m对MIC / MBC的抑菌活性为0.08-2.31 mg / mL / 0.11-3.75 mg / mL。两种活性最高的化合物3j和6b似乎对MRSA的活性高于参考药物。一半的受试化合物似乎等效/比酮康唑更有效，比联苯唑更有效。对接分析提供了有关受试化合物与不同酶之间相互作用的有用信息。

结论：革兰氏阴性和革兰氏阳性细菌和真菌对被测化合物表现出不同的响应，表明不同的取代基可能导致不同的作用方式，或者某些细菌/真菌的代谢能更好地克服化合物或适应它。