ChemInform Abstract: NEW ANALGESIC‐ANTI‐INFLAMMATORY DRUGS, 1‐OXO‐2‐SUBSTITUTED ISOINDOLINE DERIVATIVES

Abstract

Auf den in den Formeln wiedergegebenen Wegen wurden nach bekannten Verfahren die l‐Oxo‐isoindolin‐Derivate (XIV), (XX), (XXI) und (XXII) sowie davon abgeleitete Carbonamide, ‐ester, ‐hydrazide und ‐oxime synthetisiert, deren entzündungshemmende und analgetische Eigenschaften untersucht wurden.

Response of pathological ischaemic muscle pain to analgesics.

“…One of the most thoroughly investigated methods, the submaximum-effort tourniquet technique (Smith & Beecher 1969) gave results which however could not be confirmed by others (Moore, Weissman, Thomas & Whitman, 1971; Adler & Lomazzi, 1974;Adler Gervasi, Holzer & Hermeler, (1974). Taking into account these conflicting results, pathological ischaemic pain was used to study analgesic activity of two non-steroidal antiinflammatory drugs, indoprofen (Nannini, Giraldi, Molgora, Biasoli, Spinelli, Logemann, Dradi, Zanni, Buttinoni & Tommasini, 1973;Buttinoni, Cuttica, Franceschini, Mandelli, Orsini, Passerini, Turba & Tommasini, 1973) and ibuprofen (Lewis, 1975;Martindale, 1977) given orally in single doses, compared with placebo. Ibuprofen has been already examined as an analgesic in a non arthritic disorder i.e.…”

Synthesis of Phosphonic Acids Possessing Isoindolin-1-one Moiety: Unexpected Acid-Catalyzed C-P-Bond Cleavage

“…activity. The isoindolin-1-one fragment is present in synthetic (indoprofen-anti-inflammatory agent 5 ) as well as in naturally occuring compounds, in particular in alkaloids (i.e., lennoxamine, nuevamine 6 ). One of the most interesting and recent methods for the synthesis of isoindolin-1-ones is the dehydrative aromatization of epoxyisoindolones, which are the products of the reaction between aminomethylfuranes and acylating dienophiles (e.g., maleic anhydride).…”

Non-steroidal anti-inflammatory drugs. III. Structure of indoprofen: 2-[4-(1-oxo-2-isoindolinyl)phenyl]propionic acid

“…The rotation of the carboxyl group out of the plane of the adjacent phenyl ring seems to be connected with anti-inflammatory activity and is similar to that found in other 2-phenylpropionic acids. Nannini et al (1973) that have antiinflammatory activity. Buttinoni et al (1973) established its pharmacological profile as a non-steroidal anti-inflammatory agent.…”