Safaa S. Moawad , Mohsen M. Abou-El-Regal , S. A. El-Metwally
{"title":"新型吡啶嘧啶和环膜吡啶类似物的设计、合成和生物学评价","authors":"Safaa S. Moawad , Mohsen M. Abou-El-Regal , S. A. El-Metwally","doi":"10.1080/00397911.2024.2429148","DOIUrl":null,"url":null,"abstract":"<div><div>The important pharmacological and medicinal facts concerning chromenopyridopyrimidine and pyridopyrimidine compounds motivated us to condense our efforts into constructing novel derivatives with valuable biological properties. A series of new chromenopyridopyrimidine <strong>2</strong>–<strong>4</strong> and different substituted pyridopyrimidine derivatives <strong>6</strong>–<strong>9</strong> and <strong>13</strong> were synthesized in one pot three components base-catalyzed reaction of aminothiouracil <strong>1</strong> with various aldehydes and different active methylene compounds. Also, substituted pyridopyrimidines <strong>10</strong> and <strong>11</strong> were synthesized when thiouracil <strong>1</strong> reacted only with cinnamaldehyde and acetyl acetone. The synthesized compounds’ structure was verified by microanalysis and spectral data, the biological studies demonstrated antibacterial and antifungal activities against <em>E. coli</em>, <em>Pseudomonas aeruginosa</em>, <em>S. aureus</em>, and <em>C. albicans</em>.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 1","pages":"Pages 65-75"},"PeriodicalIF":1.8000,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis and biological assessment of novel pyridopyrimidine and chromenopyridopyrimidine analogues\",\"authors\":\"Safaa S. Moawad , Mohsen M. Abou-El-Regal , S. A. El-Metwally\",\"doi\":\"10.1080/00397911.2024.2429148\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>The important pharmacological and medicinal facts concerning chromenopyridopyrimidine and pyridopyrimidine compounds motivated us to condense our efforts into constructing novel derivatives with valuable biological properties. A series of new chromenopyridopyrimidine <strong>2</strong>–<strong>4</strong> and different substituted pyridopyrimidine derivatives <strong>6</strong>–<strong>9</strong> and <strong>13</strong> were synthesized in one pot three components base-catalyzed reaction of aminothiouracil <strong>1</strong> with various aldehydes and different active methylene compounds. Also, substituted pyridopyrimidines <strong>10</strong> and <strong>11</strong> were synthesized when thiouracil <strong>1</strong> reacted only with cinnamaldehyde and acetyl acetone. The synthesized compounds’ structure was verified by microanalysis and spectral data, the biological studies demonstrated antibacterial and antifungal activities against <em>E. coli</em>, <em>Pseudomonas aeruginosa</em>, <em>S. aureus</em>, and <em>C. albicans</em>.</div></div>\",\"PeriodicalId\":22119,\"journal\":{\"name\":\"Synthetic Communications\",\"volume\":\"55 1\",\"pages\":\"Pages 65-75\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2025-01-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Synthetic Communications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S0039791124001358\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Synthetic Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S0039791124001358","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Design, synthesis and biological assessment of novel pyridopyrimidine and chromenopyridopyrimidine analogues
The important pharmacological and medicinal facts concerning chromenopyridopyrimidine and pyridopyrimidine compounds motivated us to condense our efforts into constructing novel derivatives with valuable biological properties. A series of new chromenopyridopyrimidine 2–4 and different substituted pyridopyrimidine derivatives 6–9 and 13 were synthesized in one pot three components base-catalyzed reaction of aminothiouracil 1 with various aldehydes and different active methylene compounds. Also, substituted pyridopyrimidines 10 and 11 were synthesized when thiouracil 1 reacted only with cinnamaldehyde and acetyl acetone. The synthesized compounds’ structure was verified by microanalysis and spectral data, the biological studies demonstrated antibacterial and antifungal activities against E. coli, Pseudomonas aeruginosa, S. aureus, and C. albicans.
期刊介绍:
Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.