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Synthesis and sar study of diarylpentanoid analogues as new anti-inflammatory agents.
Leong, Sze Wei; Faudzi, Siti Munirah Mohd; Abas, Faridah; Aluwi, Mohd Fadhlizil Fasihi Mohd; Rullah, Kamal; Wai, Lam Kok; Bahari, Mohd Nazri Abdul; Ahmad, Syahida; Tham, Chau Ling; Shaari, Khozirah; Lajis, Nordin H.
Afiliación
  • Leong SW; Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. frederick_leong@hotmail.com.
  • Faudzi SM; Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. munifaudzi@gmail.com.
  • Abas F; Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. faridah_abas@upm.edu.my.
  • Aluwi MF; Drug and Herbal Research Centre Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abd. Aziz, 50300 Kuala Lumpur, Malaysia. fadhfasihi@yahoo.com.
  • Rullah K; Drug and Herbal Research Centre Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abd. Aziz, 50300 Kuala Lumpur, Malaysia. kamalrullah@yahoo.co.id.
  • Wai LK; Drug and Herbal Research Centre Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abd. Aziz, 50300 Kuala Lumpur, Malaysia. david_lam_98@yahoo.com.
  • Bahari MN; Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. nazribahari89@gmail.com.
  • Ahmad S; Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. syahida@upm.edu.my.
  • Tham CL; Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. chauling@upm.edu.my.
  • Shaari K; Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. khozirah@upm.edu.my.
  • Lajis NH; Al-Moalim BinLaden Chair for Scientific Miracles of Prophetic Medicine, Scientific Chairs Unit, Taibah University, P.O. Box 30001, Madinah al Munawarah 41311, Saudi Arabia. nordinlajis@gmail.com.
Molecules ; 19(10): 16058-81, 2014 Oct 09.
Article en En | MEDLINE | ID: mdl-25302700
A series of ninety-seven diarylpentanoid derivatives were synthesized and evaluated for their anti-inflammatory activity through NO suppression assay using interferone gamma (IFN-γ)/lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Twelve compounds (9, 25, 28, 43, 63, 64, 81, 83, 84, 86, 88 and 97) exhibited greater or similar NO inhibitory activity in comparison with curcumin (14.7 ± 0.2 µM), notably compounds 88 and 97, which demonstrated the most significant NO suppression activity with IC50 values of 4.9 ± 0.3 µM and 9.6 ± 0.5 µM, respectively. A structure-activity relationship (SAR) study revealed that the presence of a hydroxyl group in both aromatic rings is critical for bioactivity of these molecules. With the exception of the polyphenolic derivatives, low electron density in ring-A and high electron density in ring-B are important for enhancing NO inhibition. Meanwhile, pharmacophore mapping showed that hydroxyl substituents at both meta- and para-positions of ring-B could be the marker for highly active diarylpentanoid derivatives.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Relación Estructura-Actividad Cuantitativa / Antiinflamatorios Límite: Animals Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Relación Estructura-Actividad Cuantitativa / Antiinflamatorios Límite: Animals Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Suiza