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Discovery of novel cage-like heterocyclic hybrids as anti-inflammatory agents through the inhibition of nitrite, PGE2 and TNF-α.
Kumar, Raju Suresh; Antonisamy, Paulrayer; Almansour, Abdulrahman I; Arumugam, Natarajan; Al-Thamili, Dhaifallah M; Kumar, Raju Ranjith; Kim, Ha-Rim; Kwon, Kang-Beom.
Afiliação
  • Kumar RS; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: sraju@ksu.edu.sa.
  • Antonisamy P; Department of Korean Physiology, Wonkwang University School of Korean Medicine, 460 Iksan-daero, Iksan City, Jeonbuk 570-749, Republic of Korea.
  • Almansour AI; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Arumugam N; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Al-Thamili DM; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Kumar RR; Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625 021, Tamil Nadu, India.
  • Kim HR; Department of Korean Physiology, Wonkwang University School of Korean Medicine, 460 Iksan-daero, Iksan City, Jeonbuk 570-749, Republic of Korea.
  • Kwon KB; Department of Korean Physiology, Wonkwang University School of Korean Medicine, 460 Iksan-daero, Iksan City, Jeonbuk 570-749, Republic of Korea.
Bioorg Chem ; 91: 103180, 2019 10.
Article em En | MEDLINE | ID: mdl-31416031
ABSTRACT
Novel cage-like indolizine-acenaphthene-pyridinone heterocyclic hybrids were synthesized in good yields through [bmim]Br mediated tandem 1,3-dipolar cycloaddition-annulation sequence. The anti-inflammatory activity of these hybrids was performed using carrageenan-induced hind paw oedema, croton oil-induced ear oedema and cotton pellet-induced granuloma models. Four of these cage-like heterocyclic hybrids viz. 4b, 4d, 4e and 4j showed substantial anti-inflammatory activities against acute and chronic inflammatory models and also showed significant inhibition of PGE2, TNF-α, and nitrite levels in carrageenan-induced hind paw oedema.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Dinoprostona / Fator de Necrose Tumoral alfa / Edema / Descoberta de Drogas / Granuloma / Compostos Heterocíclicos / Anti-Inflamatórios / Nitritos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Dinoprostona / Fator de Necrose Tumoral alfa / Edema / Descoberta de Drogas / Granuloma / Compostos Heterocíclicos / Anti-Inflamatórios / Nitritos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Ano de publicação: 2019 Tipo de documento: Article