Anti-inflammatory agent design

Caribbean coral Pseudopterogorgia elisabethae discovered by Fenical et al. [47], Pseudopterosin E, Fig. (3) is the one with the best pharmacological profile, combining low toxicity and potent antiinflammatory activity. In human neutrophils, pseudopterosin E inhibits degranulation and formation of Ieukotrienes [2], In 1991, phase I clinical trials were initiated with pseudopterosin E as a topical anti-inflammatory agent. Recently, novel anti-inflammatory natural products have been isolated from this Caribbean soft coral [48,49], Japanese researchers reported the isolation of a group of compounds designated helioporins A-E, which are related to the pseudopterosins [1],... 

Functionalized oxadiazoles have received considerable attention in the pharmaceutical industry as heterocyclic amide and ester isosteres [95]. Oxadiazoles have been employed in the design of biologically active templates, e. g. core structures for muscarinic agonists, kinase inhibitors, anti-inflammatory agents, histamine H3 antagonists, monoaminic oxidase inhibitors, etc. 

Designing appropriate polymer-drug linkers for orally administered conjugates is another challenge. Peptidyl sequences tailored for site-specific cleavage by brush border enzymes, i.e., at the enterocyte smface (263), were explored, and also azo hnkers for colon-specific, e.g., of anti-inflammatory agents like aminosalicyfic acid (264). 

Sharma R N, Xavier F P, Vasu K K, Chaturvedi S C, PanchoU S S. S5mthesis of 4-Ben-zyl-l,3-thiazole derivatives as potential anti-inflammatory agents An Analogue-based Drug Design Approach, J Enz Inhib Med Chem. 2009. p. 890 - 897. DOI 10.1080/14756360802519558... 

Rajan S, Hardik G, Thaker M, Tony G, Kamala K. V. Design, synthesis and characterization of novel 2-(2,4-disubstituted-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-kB and AP-1 mediated transcription activation and as potential anti-inflammatory agents, Eur. J. Med. Chem. 2009. p. 2184 - 2189. DOI 10.1016/i.ejmech.2008.10.031... 

In contrast to bioinert materials, which are designed to prevent any interaction with the surrounding medium, bioactive materials come in contact with the environment as they trigger a specific material-tissue interaction such as EC proliferation or release drugs such as anticoagulation or anti-inflammatory agents [1,11,75]. 

Pyrimidinopyridones Design and synthesis of a novel class of FMS inhibitors as potential anti-inflammatory agents... 

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