Discovery of a Series of 5-benzylidene-1, 3-thiazolidine-2, 4-dione-linked Chalcone Hybrids as a Novel Class of 5-Lipoxygenase (5-LO) Inhibitors

    Published on:March 2018
    Journal of Young Pharmacists, 2018; 10(2):241-242
    Letter to the editor | doi:10.5530/jyp.2018.10.53
    Authors:

    Vasudeva Rao Avupati1*, Yuawa Rani2, Ashwinder Singh3

    1Pharmaceutical Chemistry Division, School of Pharmacy, International Medical University, 126, Jln Jalil Perkasa 19, Bukit Jalil, Wilayah Persekutuan, Kuala Lumpur, MALAYSIA.

    2Pharmacology Division, Faculty of Pharmacy, Asia Metropolitan University, G-8 Jalan Kemacahaya 11, Taman Kemacahaya, Cheras, Selangor, MALAYSIA.

    3Pharmaceutical Chemistry Division, Faculty of Pharmacy, Asia Metropolitan University, G-8 Jalan Kemacahaya 11, Taman Kemacahaya, Cheras, Selangor, MALAYSIA.

    Abstract:

    Sir,

    In mammals, lipoxygenases (LOXs) are enzymes containing iron that are biological targets for essential fatty acids. These fatty acids are eicosanoids, derived from arachidonic acid, play important roles in implication and development of multifactorial inflammatory diseases.1 The 5-Lipoxygenase (5-LO) catalyses two-step reaction that is from arachidonic acid to leukotriene A4 (LTA4). In the first step, oxidation of arachidonic acid to an unstable reactive intermediate 5-hydroperoxyeicosatetraenoic acid (5-HPETE), followed by in the second step, dehydration of 5-HPETE to form LTA4. These reactions are initially leading to the biosynthesis of various classes of leukotrienes and plays a significant role in regulating leukotriene production. 5-LO has progressed its role through multiple mechanisms by its function, structure, cofactors, and the other regulatory mechanisms controlling its expression.2 Based on these functions, lipoxygenases were identified as potential drug-target associated with pathogenesis of inflammatory diseases.3 Read more. . . .

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