Suppr超能文献

新型杂环结构。噻唑并[3,2 - a][1,2,5]噻二唑并[3,4 - d]嘧啶和[1,2,5]噻二唑并[3',4':4,5]嘧啶并[2,1 - b][1,3]噻嗪。生物学测定。

New heterocyclic structures. thiazolo[3,2-a][1,2,5] thiadiazolo[3,4-d]pyrimidine and [1,2,5]thiadiazolo[3',4':4,5] pyrimido[2,1-b][1,3]thiazine. biological assays.

作者信息

Rinaldi M, Pecorari P, Cermelli C, Malagoli M

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Modena, Italy.

出版信息

Farmaco. 1993 Mar;48(3):427-33.

PMID:8323673
Abstract

6,7-Dihydro-9H-thiazolo[3,2-a][1,2,5]thiadiazolo [3,4-d]pyrimidin-9-one, 7,8-dihydro-6H,10H-[1,2,5]thiadiazolo[3',4':4,5]pyrimido [2,1-b][1,3]thiazin-10-one and its 3-methyl derivative were prepared by reacting 6,7-diamino-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-one, 7,8-diamino-3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one or its 3-methyl derivative with N-thionylaniline. A reaction mechanism is proposed. The compounds and the sodium salts of (7-amino-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-on-6-yl)sulfamic acid, (8-amino-3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-on-7-yl) sulfamic acid and its 3-methyl derivative were tested for antimicrobial and antimycotic activity on a number of strains, namely: E. Coli, Proteus mirabilis, P. vulgaris, Pseudomonas aeruginosa, Salmonella spp, Staphylococcus spp, Streptococcus faecalis, Bacillus subtilis, Sarcina lutea, Candida albicans, and for antiviral activity on Herpes simplex virus type 1 and Vescicular stomatitis virus. None of the compounds showed antiviral activity or exhibited biological activity against gram-negative, gram-positive bacteria or against mycetes.

摘要

通过使6,7-二氨基-2,3-二氢-5H-噻唑并[3,2-a]嘧啶-5-酮、7,8-二氨基-3,4-二氢-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮或其3-甲基衍生物与N-硫代苯胺反应,制备了6,7-二氢-9H-噻唑并[3,2-a][1,2,5]噻二唑并[3,4-d]嘧啶-9-酮、7,8-二氢-6H,10H-[1,2,5]噻二唑并[3',4':4,5]嘧啶并[2,1-b][1,3]噻嗪-10-酮及其3-甲基衍生物。提出了一种反应机理。测试了(7-氨基-2,3-二氢-5H-噻唑并[3,2-a]嘧啶-5-酮-6-基)氨基磺酸、(8-氨基-3,4-二氢-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮-7-基)氨基磺酸及其3-甲基衍生物的化合物和钠盐对多种菌株的抗微生物和抗真菌活性,这些菌株包括:大肠杆菌、奇异变形杆菌、普通变形杆菌、铜绿假单胞菌、沙门氏菌属、葡萄球菌属、粪肠球菌、枯草芽孢杆菌、藤黄八叠球菌、白色念珠菌,以及对1型单纯疱疹病毒和水疱性口炎病毒的抗病毒活性。这些化合物均未显示出抗病毒活性,也未表现出对革兰氏阴性菌、革兰氏阳性菌或真菌的生物活性。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验