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      Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1 H) Pyridones

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          Abstract

          Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1 H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC 50 = 0.17 mM).

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          Strategies for treating idiopathic pulmonary fibrosis.

          Philippe Bois (2010)
          Idiopathic pulmonary fibrosis (IPF) is the most common and most lethal diffuse fibrosing lung disease, with a mortality rate that exceeds that of many cancers. Recently, there have been many clinical trials of novel therapies for IPF. The results have mostly been disappointing, although two treatment approaches have shown some efficacy. This Review describes the difficulties of treating IPF and the approaches that have been tried or are in development, and concludes with suggestions of future therapeutic targets and strategies.
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            The immunology of fibrosis: innate and adaptive responses.

            Georg Wick, Aleksandar Backovic, Evelyn Rabensteiner … (2010)
            Fibrosis is an important health problem, and its pathogenetic principles are still largely unknown. It can develop either spontaneously, or, more frequently, as a consequence of various underlying diseases. Irrespective of the primary cause, however, fibrotic tissue is always infiltrated by mononuclear immune cells. In most instances the reason for the attraction of these cells to fibrotic tissue and their proliferation remains to be determined; however their cytokine profile shows clear-cut proinflammatory and profibrotic characteristics. In this review, we discuss the innate and adaptive immune reactions associated with the development of fibrosis and the molecular basis of the profibrotic mechanisms taking place in systemic sclerosis (scleroderma), arteriosclerosis and peri-silicone mammary implant fibrosis. Copyright 2009 Elsevier Ltd. All rights reserved.
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              Glycosides in medicine: "The role of glycosidic residue in biological activity".

              Vladimír Křen, Ludmila Martinkova (2001)
              Numbers of biologically active compounds are glycosides. Sometimes, the glycosidic residue is crucial for their activity, in other cases glycosylation only improves pharmacokinetic parameters. Recent developments in molecular glycobiology brought better understanding to the aglycone vs. glycoside activities, and made possible to develop new, more active or more effective glycodrugs based on these findings - very illustrative recent example is the story of vancomycin. This paper deals with an array of glycosidic compounds currently used in medicine but also with biological activity of some glycosidic metabolites of the known drugs. It involves glycosides of vitamins, polyphenolic glycosides (flavonoids), alkaloid glycosides, glycosides in the group of antibiotics, glycopeptides, cardiac glycosides, steroid and terpenoid glycosides etc. The physiological role of the glycosyl and structure-activity relations (SAR) in the glycosidic moiety (-ies) are discussed.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 17 January 2012
                Publication date Collection: January 2012
                Volume: 17
                Issue: 1
                Pages: 884-896
                Affiliations
                [1 ]State Key Laboratory of Natural and Biomimetic Drug, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
                [2 ]Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
                [3 ]Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha, Hunan 410013, China
                [4 ]Division of Nephrology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
                Author notes
                [* ] Authors to whom correspondence should be addressed; Email: zjli@ 123456bjmu.edu.cn ; Tel.: +86-10-8280-1714; Fax: +86-10-8280-5496.
                Article
                Publisher ID: molecules-17-00884
                DOI: 10.3390/molecules17010884
                PMC ID: 6269014
                PubMed ID: 22252504
                SO-VID: f43be086-90fe-4b30-8dcb-de7176569a5f
                Copyright © © 2012 by the authors; licensee MDPI, Basel, Switzerland.
                License:

                This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 16 November 2011
                Date revision received : 10 January 2012
                Date accepted : 12 January 2012
                Categories
                Subject: Article

                Keywords: antifibrotic,pirfenidone,fluorofenidone,carbohydrate modified,glucose
                Data availability:
                Keywords: antifibrotic, pirfenidone, fluorofenidone, carbohydrate modified, glucose

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