A one-pot synthesis of indole-appended heterocycles as potent anti-inflammatory, analgesic, and CNS depressant agents

Autor:	Shaik Rahber, Mety Sundar, Sasidhar Balappa Somappa, Parveen Rajesab, Jaiprakash S. Biradar
Rok vydání:	2015
Předmět:	Indole test medicine.drug_class Stereochemistry One-pot synthesis General Chemistry Carbon-13 NMR Pyrazole Anti-inflammatory chemistry.chemical_compound chemistry medicine Proton NMR Potency Isoxazole
Zdroj:	Monatshefte für Chemie - Chemical Monthly. 146:2067-2078
ISSN:	1434-4475 0026-9247
DOI:	10.1007/s00706-015-1476-x
Popis:	A series of novel 3-[3-(2,5-dichloro-3-thienyl)-substituted-1H-pyrazol-5-yl]-2,5-disubstituted-1H-indoles, 3-[3-(2,5-dichloro-3-thienyl)isoxazol-5-yl]-2,5-disubstituted-1H-indoles, and 4-(2,5-dichloro-3-thienyl)-6-(2,5-disubstituted-1H-indol-3-yl)-substituted pyrimidin-2(5H)-ones were synthesized by means of a one-pot reaction. Structures of all compounds were confirmed by their melting points, elemental analysis, IR, 1H NMR, 13C NMR, and mass spectral data. The novel compounds were evaluated for pharmacological studies and discussed in terms of their structural differences. Among the screened compounds, three show excellent anti-inflammatory activity with maximum inhibition (50.0–59.1 %), i.e. better than the standard drug indomethacin (50.0 %). Four of the compounds revealed highest analgesic potency. In locomotor activity, six compounds exhibited promising results for CNS depressant activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::4e401c6801598113f9d352e4b3db6e2b https://doi.org/10.1007/s00706-015-1476-x Zobrazit plný text záznamu Full text from SpringerLink