Structural optimization of pyrazolopyridine derivative 2, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library, was carried out successfully. The process of discovery of new orally active PDE4 inhibitors, which are expected to possess therapeutic potential, is presented and their structure-activity relationships are discussed.
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| http://dx.doi.org/10.1016/j.bmcl.2003.10.025 | DOI Listing |
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Prevalence of fungal colonization among patients with psoriasis in difficult-to-treat areas: impact of apremilast on mycotic burden and clinical outcomes.
Front Immunol
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Department of Experimental Medicine, University of Rome "Tor Vergata", Rome, Italy.
Introduction: Fungi, including , may be a trigger or exacerbate psoriasis, especially in difficult to treat (DTT) areas, through the activation of IL-17/23 axis.
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Rationale for phosphodiesterase-4 inhibition as a treatment strategy for interstitial lung diseases associated with rheumatic diseases.
RMD Open
December 2024
David Geffen School of Medicine, University of California Los Angeles, Los Angeles, California, USA.
Interstitial lung disease (ILD) associated with rheumatoid arthritis or with connective tissue diseases such as systemic sclerosis can be collectively named systemic autoimmune rheumatic disease-associated ILDs (SARD-ILDs) or rheumatic musculoskeletal disorder-associated ILDs. SARD-ILDs result in substantial morbidity and mortality, and there is a high medical need for effective therapies that target both fibrotic and inflammatory pathways in SARD-ILD. Phosphodiesterase 4 (PDE4) hydrolyses cyclic AMP, which regulates multiple pathways involved in inflammatory processes.
View Article and Find Full Text PDFInhibition of phosphodiesterases 1 and 4 prevents myofibroblast transformation in Peyronie's disease.
BJU Int
December 2024
Fibrosis Research Group, Medical Technology Research Centre, Anglia Ruskin University, Chelmsford, UK.
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Hamad Medical Corporation, Al Rayyan Road, Doha, 3050, Qatar. Electronic address:
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