Abstract
This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. The IC50 for nitric oxide inhibition, PGE2 inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity.
Highlights
IntroductionInflammation participates in vital pathological and physiological processes like infection and wound healing [1]
Inflammation is one of the most important and complicated defense mechanisms
The synthesis of the final target compounds 1a–i, 2a–i, 3a–h, and 4a–h was achieved by theadopting synthetic strategy in Scheme
Summary
Inflammation participates in vital pathological and physiological processes like infection and wound healing [1]. As a result of tissue damage, many chemical intermediates are released in the damaged area. The chemical intermediates (such as E, L, and P-selectin and chemokines) initiate activation and migration of white blood cells to the damaged area. Inflammation can be acute, occurring as part of a healing process, or chronic inflammation, which arises from the over response of the immune system and can lead to tissue damage. Chronic inflammation contributes to several physiological disorders such as neurodegenerative diseases [6], cancer [7], inflammatory bowel disease [8], and arteriosclerosis [9]
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