新型杂环结构的合成与生物活性：[1,3]噻嗪并[2,3-i]嘌呤、噻唑并[3,2-c][1,2,3]三唑并[4,5-e]嘧啶和[1,2,3]三唑并[4',5':4,5]嘧啶并[6,1-b][1,3]噻嗪
Synthesis and biological activity of new heterocyclic structures: [1,3]thiazino[2,3-i]purine, thiazolo[3,2-c] [1,2,3]triazolo[4,5-e]pyrimidine and [1,2,3]triazolo [4', 5': 4,5] pyrimido[6,1-b][1,3]thiazine.
作者信息
Rinaldi M, Pecorari P, Costantino L, Provvisionato A, Malagoli M, Cermelli C
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Modena, Italy.
出版信息
Farmaco. 1992 Oct;47(10):1315-22.
Some derivatives of thiazolo[3,2-c]pyrimidine, pyrimido[6,1-b][1,3]thiazine, thiazolo[2,3-i]purine, [1,3]thiazino[2,3-i]purine, thiazolo[3,2-c][1,2,3]triazolo[4,5-e]pyrimidine and [1,2,3]triazolo[4',5':4,5]pyrimido[6,1-b][1,3]thiazine were prepared. The compounds were tested for antimicrobial and antimycotic activity on a number of strains, namely, Escherichia coli, Proteus vulgaris, P. mirabilis, Pseudomonas aeruginosa, Salmonella sp., Staphylococcus aureus, Streptococcus faecalis, Bacillus subtilis, Sarcina lutea, Candida albicans, Aspergillus sp., and for antiviral activity on Herpes simplex virus, Type 1 (HSV-1), Vesicular stomatitis virus (VSV) and Coxsackievirus B5 (CoxB5). The compounds proved to be devoid of activity against viruses, mycetes and gram-negative bacteria, while some of them exhibited a modest activity against gram-positive bacterial strains.
制备了噻唑并[3,2 - c]嘧啶、嘧啶并[6,1 - b][1,3]噻嗪、噻唑并[2,3 - i]嘌呤、[1,3]噻嗪并[2,3 - i]嘌呤、噻唑并[3,2 - c][1,2,3]三唑并[4,5 - e]嘧啶和[1,2,3]三唑并[4',5':4,5]嘧啶并[6,1 - b][1,3]噻嗪的一些衍生物。对这些化合物在多种菌株上进行了抗微生物和抗真菌活性测试，这些菌株包括大肠杆菌、普通变形杆菌、奇异变形杆菌、铜绿假单胞菌、沙门氏菌属、金黄色葡萄球菌、粪肠球菌、枯草芽孢杆菌、藤黄八叠球菌、白色念珠菌、曲霉属，还对其在1型单纯疱疹病毒（HSV - 1）、水疱性口炎病毒（VSV）和柯萨奇病毒B5（CoxB5）上进行了抗病毒活性测试。结果证明这些化合物对病毒、霉菌和革兰氏阴性菌无活性，而其中一些对革兰氏阳性菌菌株表现出一定活性。
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