Synthesis of some thiazolyl and thiadiazolyl derivatives of 4(3H)-quinazolinone as anti-inflammatory-antimicrobial agents
- Authors
- Bekhit A.A.; Habib N.S.; Park J.Y.
- Issue Date
- Jan-2004
- Publisher
- Societa Editoriale Farmaceutica
- Keywords
- 4(3H)-Quinazolinone; Anti-inflammatory and antimicrobial activities; Thiadiazole; Thiazole; Ulcerogenic effects
- Citation
- Bollettino Chimico Farmaceutico, v.143, no.1, pp 34 - 39
- Pages
- 6
- Journal Title
- Bollettino Chimico Farmaceutico
- Volume
- 143
- Number
- 1
- Start Page
- 34
- End Page
- 39
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/16103
- ISSN
- 0006-6648
- Abstract
- This paper describes the synthesis of four series of 4(3H)-quinazolinone derivatives. The first series was prepared by cyclization of the intermediate 3-aryl-2-substituted thiocarbamoylhydrazonomethyl-4(3H)-quinazolinones 2a,b with ethyl bromoacetate to afford the corresponding thiazolidinonyl derivatives 3a,b. The second series were prepared by the cyclization of the intermediate 2a,b with phenacyl bromide or 4-substituted phenacyl bromide giving rise to thiazolinyl derivatives 4a-f Furthermore, the thiazolidinonyl derivatives 5a,b were obtained by reaction of the intermediate 2a,b with thioglycolic acid. On the other hand, heating the intermediate 2a,b with, acetic anhydride afforded the corresponding thiadiazolinyl derivatives 6a,b. Some of the synthesized compounds showed promising anti-inflammatory activities.
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