![]() ![]() Chalcone-thiazole hybrids: rational design, synthesis and lead identification against 5-lipoxygenase. 5-lipoxygenase metabolic contributions to NSAID-Induced organ toxicity. Opposing roles of LTB 4 and PGE 2 in regulating the inflammasome-dependent scorpion venom-induced mortality. Zoccal KF, Sorgi CA, Hori JI, Arantes EC, Serezani CH, Zamboni DS. ![]() Nasturtium (Indian cress, Tropaeolum majus nanum) dually blocks the COX and LOX pathway in primary human immune cells. Tran H, Márton, Rita M, Maul R, Baldermann S, Schreiner M. N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study. Biological basis for the cardiovascular consequences of COX-2 inhibition: Therapeutic challenges and opportunities. Synergy of physico-chemical and biological experiments for developing a cyclooxygenase-2 inhibitor. Singh P, Kaur J, Kaur H, Kaur A, Bhatti R. ![]() Synthetically-tailored and nature-derived dual COX-2/5-LOX inhibitors: Structural aspects and SAR. Meshram MA, Bhise UO, Makhal PN, Kaki VR. COX isoforms in the cardiovascular system: understanding the activities of non-steroidal anti-inflammatory drugs. Anti-inflammatory and side effects of cyclooxygenase inhibitors. Synthesis, inhibitory activity and in silico docking of dual COX/5-LOX inhibitors with quinone and resorcinol core. Sisa M, Dvorakova M, Temml V, Jarosova V, Vanek T, Landa P. Dual COX and 5-LOX inhibition by clerodane diterpenes from seeds of Polyalthia longifolia (Sonn.) Thwaites. Nguyen HT, Vu TY, Chandi V, Polimati H, Tatipamula UB. Prevention of thrombosis and vascular inflammation: benefits and limitations of selective or combined COX-1, COX-2 and 5-LOX inhibitors. Inhibition of both COX-1 and COX-2 and resulting decrease in the level of prostaglandins E2 is responsible for non-steroidal anti-inflammatory drug (NSAID) -dependent exacerbation of colitis. Tanaka KI, Suemasu S, Ishihara T, Tasaka Y, Arai Y, Mizushima T. 2-Aryl-3- (2-morpholinoethyl) thiazolidin-4-ones: Synthesis, anti-inflammatory in vivo, cytotoxicity in vitro and molecular docking studies. Gouvea PD, Vasconcellos FA, Berwaldt GA, Fischer G, Sakata RP, Almeida WP. Origin and physiological roles of inflammation. Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2, 5-dione derivatives as multitarget anti-inflammatory agents. Jan MS, Ahmad S, Hussain F, Ahmad A, Mahmood F, Rashid U. Detection of an anti-angina therapeutic module in the effective population treated by a multi-target drug Danhong injection: a randomized trial. Liu J, Li DD, Dong W, Liu YQ, Wang YY, Chen YD. Based on these results, further research into safer and more effective anti-inflammatory drugs might be possible using indole arylamide benzoic acid analogs. As demonstrated by docking studies, 7f and 7n have stronger interactions with key residues in the active pocket of COX-1 or COX-2, which is consistent with the activity results. According to the biological results, compounds 7f and 7n have better inhibitory activities on the production of NO and PGE 2 in LPS-induced RAW 264.7 cell macrophages than celecoxib and indomethacin. Compared to zileuton (IC 50 = 36.46 nM), compound 7f was identified as the most potent 5-LOX inhibitor (IC 50 = 77.37 nM). Furthermore, 7f and 7n exhibited moderate COX-2 inhibitory activity (IC 50 = 537 and 321.5 nM) than celecoxib (IC 50 = 10.04 nM) in vitro, among which 7n had higher COX-2 selectivity activity (selectivity index (COX-1/COX-2) = 7.89) and moderate 5-LOX inhibitory activity (IC 50 = 222.1 nM). ![]() Compounds 7f and 7n showed significant anti-inflammatory activity in a xylene-induced mouse model of auricular edema. In this study, we designed and synthesized a series of novel indole and indazole arylamide benzoic acid analogues as dual COX-2 / 5-LOX inhibitors and evaluated their anti-inflammatory properties in vivo. Compared to classical NSAIDs, the dual COX-2/5-LOX inhibition is an effective strategy for designing compounds with more effective biological activities, fewer side effects, and a broader anti-inflammatory spectrum. The arachidonic acid metabolizing enzymes cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) have been considered to be associated with the occurrence and development of a variety of diseases, including inflammatory. ![]()
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