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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Abstract
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 |
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Subjects: | R Medicine / orvostudomány > RM Therapeutics. Pharmacology / terápia, gyógyszertan R Medicine / orvostudomány > RS Pharmacy and materia medica / gyógyszerészet, gyógyászati eszközök |
SWORD Depositor: | MTMT SWORD |
Depositing User: | MTMT SWORD |
Date Deposited: | 15 Feb 2016 13:01 |
Last Modified: | 15 Feb 2016 13:01 |
URI: | http://real.mtak.hu/id/eprint/33432 |
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