Solid phase synthesis of quinolones

• Published in: Bioorganic & medicinal chemistry letters Vol. 9; no. 14; pp. 1885 - 1888
• Main Authors: Srivastava, Sanjay K., Haq, W., Murthy, P.K., Chauhan, P.M.S.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 19.07.1999; Elsevier
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Biological and medical sciences; Brugia malayi - drug effects; Chemistry, Organic - methods; Filaricides - chemical synthesis; Filaricides - chemistry; Filaricides - pharmacology; Hexanes - chemical synthesis; Hexanes - chemistry; Hexanes - pharmacology; Medical sciences; Octanes - chemical synthesis; Octanes - chemistry; Octanes - pharmacology; Pharmacology. Drug treatments; Quinolones - chemical synthesis; Quinolones - chemistry; Quinolones - pharmacology; Structure-Activity Relationship; Ketoamide; Quinoline derivatives; In vitro; Structure activity relation; Carboxylic acid; Brugia malayi; Parasiticid; Helmintha; Nemathelminthia; Ketoester; Solid phase; Invertebrata; Chemical synthesis; Nematoda; Quinolone derivatives
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(99)00326-1

Solid phase syntheses of ethyl 6-carboxyquinol-4(1H)-one-3-carboxylate (5) and N-substituted 6-carboxyquinol-4(1H)-one-3-carboxamides 7a-d have been described. Antifilarial in vitro activities of 5,7a-d against Brugia malayi have also been delineated. Synthesis of quinolones ( 5,7a-d) has been carried out on solid support and their in vitro antifilarial activity against B. malayi have been delineated.