SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES
Omar, R., Said, M., Ahmed, H., Omar, A., Mahmoud, A. (2004). SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES. EKB Journal Management System, 13(1), 21-28. doi: 10.21608/zjps.2004.177905
Refat Omar; Makarem Said; Hosam El-Din Ahmed; Adel Omar; Ahmed Mahmoud. "SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES". EKB Journal Management System, 13, 1, 2004, 21-28. doi: 10.21608/zjps.2004.177905
Omar, R., Said, M., Ahmed, H., Omar, A., Mahmoud, A. (2004). 'SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES', EKB Journal Management System, 13(1), pp. 21-28. doi: 10.21608/zjps.2004.177905
Omar, R., Said, M., Ahmed, H., Omar, A., Mahmoud, A. SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES. EKB Journal Management System, 2004; 13(1): 21-28. doi: 10.21608/zjps.2004.177905

SYNTHESIS OF CERTAIN CYCLOPENTYLbPYRIDIN-5-ONES OF ANTICIPATED ANTI- INFLAMMATORY, ANTICOAGULANT AND ANTIMICROBIAL ACTIVITIES

Zagazig Journal of Pharmaceutical Sciences
Article 5, Volume 13, Issue 1, June 2004, Page 21-28  XML PDF (3.3 MB)
Document Type: Original Article
DOI: 10.21608/zjps.2004.177905
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Authors
Refat Omar email 1; Makarem Said1; Hosam El-Din Ahmed2; Adel Omar3; Ahmed Mahmoud4
1Organic Chemistry Department, Faculty of Pharmacy, Cairo University,
2Organic Chemistry Department, Faculty of Pharmacy, Suez Canal University
3Clinical Pharmacology Department, Faculty of Medicine, Menofia University
4Microbiology Department, Faculty of Medicine, Menofia University
Abstract
The reaction of quinolinic anhydride (2) with α-(or ɣ-) picoline yielded 6-(2-pyridinyl) cyclopentylbpyridine-5,7-dione (3) or 6-(4- pyridinyl) analogue 4 Compounds 3 and 4 were changed into the chloro derivatives 5 and 6 respectively by using mixture of phosphorus pentachloride and phosphorus oxychloride. The chloro compounds (5 and 6) underwent nucleophilic substitution condensed with different amines to produce compound 7 and 8 respectively. The hydrazino derivatives 7i and 8i respectively were with different aromatic aldehydes to produce 9 and 10 respectively.
Compounds  8g and 10f, which showed a significant antiinflammatory action compared to Indomethacine. Also compounds 8h and 9h were  active as anticoagulant as phenindione. Finally, 9f, and 9c. showed antimicrobial activity especially against Staphlococoue aureus and Escherichica coli.
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