Exceedingly facile one-pot protocols to the synthesis of pyrimido annulated analogues of carbazolo condensed azepinones and their evaluation for analgesic activity
| Autor: | M. Agrawal, S. Jain, S. Sharma, J. Dwivedi, D. Kishore |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: | |
| Zdroj: | Bulletin of the Chemical Society of Ethiopia, Vol 31, Iss 1, Pp 93-105 (2017) |
| Druh dokumentu: | article |
| ISSN: | 1011-3924 1726-801X |
| DOI: | 10.4314/bcse.v31i1.8 |
| Popis: | Extremely simple protocols based on the reactivity of corresponding oxoketenedithioacetal (4), 2-(dimethylaminomethylene) ketone (5), β-oxoenolether (6) and α,β-unsaturated ketone (7) derivatives of 7-ethyl-3, 4-dihydroazepino[3,2-b]carbazol-2,5(1H,7H)-dione (3) have been developed to provide an easy access to their pyrimido annulated analogues (8-15) of medicinal interest. The key compound 3 from which, the synthesis proceeded has been realized in two steps from the commercial 3-amino-9-ethyl carbazole (1) on its reaction in the first step with ethyl succinyl chloride followed by cyclocondensation of the resulting ester 2 with PPA. The selected synthesized compounds were screened for in-vivo analgesic activity using acetic acid induced writhing model in mice. Among them, compound 13was found to be most active and found comparable to standard aspirin. |
| Databáze: | Directory of Open Access Journals |
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