title: Synthesis, anti-inflammatory and analgesic evaluation of certain new 3a,4,9,9a-tetrahydro-4,9-benzenobenz[f]isoindole-1,3-diones.
abstract: In an effort to establish new candidates with improved analgesic and anti-inflammatory activities, we reported here the synthesis and in-vivo analgesic and anti-inflammatory evaluation of various series of 2-substituted-3a,4,9,9a-tetrahydro-4,9-benzeno-benz[f]isoindole-1,3-diones: [4-Bromobutoxy] 6, 5-bromopentoxy 7, [4-(4-phenylpiperazin-1-yl)butoxy] 9, [5-(4-phenylpiperazin-1-yl)pentoxy] 10, 2-(2(4)-(4-phenylpiperazin-1-yl)-2-oxoethyl/4-oxobutyl 17, 19, [2(4)-(4-methylpiperazin-1-yl]-2-oxoethyl/4-oxobutyl 20, 22, [2(4)-morpholino-2-oxoethyl/4-oxobutyl] 23, 25, and 2(4)-(piperidin-1-yl)2-oxoethyl/4-oxobutyl) 26 and 28. The newly synthesized compounds were characterized by (IR, (1)H-, (13)C-NMR, and mass spectra). The representative compounds were evaluated as analgesic and anti-inflammatory activities. Compounds 9, 19, 22, 25, and 28 exhibited activities higher than the reference drug.
authors.affiliation: Photochemistry Department (Heterocyclic Unit), National Research Center, Dokki, Giza, Egypt.
authors.forename: A A
authors.initials: AA
authors.lastname: Abu-Hashem
authors.forename: M A
authors.initials: MA
authors.lastname: Gouda
mesh_terms: D000700:Analgesics / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D055808:Drug Discovery; D054833:Isoindoles / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D060172:Morpholinos / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: C568423:3a,4,9,9a-tetrahydro-4,9-benzenobenz(f)isoindole-1,3-dione; D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D054833:Isoindoles; D060172:Morpholinos