Bioisosteric hybrids of two anti-inflammatory agents, rutaecarpine and piroxicam

Bubenyák, Máté Dániel and Noszál, Béla and Kóczián, Kristóf and Takács, Mária and Béni, Szabolcs and Hermecz, István and Kökösi, József (2008) Bioisosteric hybrids of two anti-inflammatory agents, rutaecarpine and piroxicam. TETRAHEDRON LETTERS, 49 (40). pp. 5711-5713. ISSN 0040-4039

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Bioisosteric replacements were accomplished by building the structural elements of piroxicam, an antiinflammatory drug, into the pentacyclic system of rutaecarpine, a quinazolinocarboline alkaloid, in order to modify activity and selectivity on COX-isoenzymes. The pentacyclic compounds were synthesized efficiently by employing 1-oxo-9,10,11,12-tetrahydro-4H-pyrido[1,2-b] 1,2-benzothiazine 5,5-dioxide as a key intermediate, and prepared by alternative routes. Condensation of the tricyclic ketone with arylhydrazines and subsequent Fischer-indolization provided the first representatives of new heterocyclic ring systems 3 and 4. Crown Copyright (C) 2008 Published by Elsevier Ltd. All Fights reserved.

Item Type: Article
Subjects: R Medicine / orvostudomány > RM Therapeutics. Pharmacology / terápia, gyógyszertan
R Medicine / orvostudomány > RS Pharmacy and materia medica / gyógyszerészet, gyógyászati eszközök
Depositing User: MTMT SWORD
Date Deposited: 15 Feb 2016 13:01
Last Modified: 15 Feb 2016 13:01

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