Synthetic inhibitors of interleukin-6 I: 2,3,7,8-tetrahydro-4-aryl-1H-cyclopent [e] imidazo [1,2-a]- pyridin-5(6H)-one and related compounds

Tagat, Jayaram R.; Nazareno, Dennis V.; McCombie, Stuart W.; Barton, Beverly E.; Shortall, Jennifer; Jackson, James R.

doi:10.1016/0960-894x(95)00362-w

Cited by 4 publications

(1 citation statement)

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“…As IL-6 participates in various cellular and physiological responses during the inflammatory reaction [21], IL-6 inhibitors can be used in treatment of psychiatric disorders, Alzheimer's disease, diabetes, cancer, depression SAR and QSAR in Environmental Research 885 and rheumatoid arthritis [22][23][24]. Small compounds that are identified as IL-6 inhibitors (Figure 2) include nitrogen-containing benzophenones [25], β-chloro-vinyl chalcones [26,27], 4-styryl-coumarin derivatives [28], derivatives of N-aryl urea [29], methoxylated chalcones [30], thalidomide analogues [31], pyrazolo [3,4-b]pyridines [32], 3,5-diaryl pyridines and meta-terphenyls [33], 2,2-bisaminomethylated aurone analogues [34], pyrazole chalcones [35] and pyridine-5(6H)-one analogues [36]. Tocilizumab, an anti-interleukin-6 receptor antibody, has been approved for the treatment of rheumatoid arthritis, Castleman's disease and juvenile idiopathic arthritis [37].…”

Section: Introductionmentioning

confidence: 99%

Cytokines in terms of QSAR. Review, evaluation and comparative studies

Konstantinidou

Hadjipavlou‐Litina

2013

SAR and QSAR in Environmental Research

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Cytokines represent a class of chemical factors that act as mediators in the complex biological response of inflammation, potentially implicated in various diseases. Therefore, selective inhibition or antagonism of cytokines is a target of anti-inflammatory drug design. The QSAR (Quantitative Structure-Activity Relationships) analysis presented here attempts to identify the structural features and physicochemical properties that are significant for cytokine antagonists or inhibitors and in particular of i) interleukin-5 (IL-5), ii) interleukin-6 (IL-6) and iii) of the chemotactic cytokine (chemokine) interleukin-8 (IL-8). Firstly, a historical aspect of the limited published QSARs is discussed and then a 2D-QSAR analysis was carried out for 26 data sets of compounds using the C-QSAR program of Biobyte. In six cases hydrophobicity appeared to be important. Steric factors in the form of overall molar refractivity (CMR), molar refractivity of the substituent (MR), molar volume (MgVol), Taft's Es constant and the sterimol parameters B1 and B5 have a significant impact on biological activity in most of the derived equations whereas electronic parameters as σp, σm or Σσ appeared in five cases.

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