2016
DOI: 10.1002/wnan.1427
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Challenges to develop novel anti‐inflammatory and analgesic drugs

Abstract: Chronic inflammatory diseases and persistent pain of different origin represent common medical, social, and economic burden, and their pharmacotherapy is still an unresolved issue. Therefore, there is a great and urgent need to develop anti-inflammatory and analgesic agents with novel mechanisms of action, but it is a very challenging task. The main problem is the relatively large translational gap between the preclinical experimental data and the clinical results due to characteristics of the models, difficul… Show more

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Cited by 24 publications
(20 citation statements)
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References 263 publications
(454 reference statements)
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“…The importance of these results is highlighted by the fact that neuropathic pain is very resistant to conventional analgesics: the effect of opioids and NSAIDs is almost absent in neuropathic conditions [27,[57][58][59]. Adjuvant analgesics (e.g., antiepileptics, antidepressants) might have limited effects in certain cases, but they could exert several serious adverse effects [60].…”
Section: Discussionmentioning
confidence: 99%
“…The importance of these results is highlighted by the fact that neuropathic pain is very resistant to conventional analgesics: the effect of opioids and NSAIDs is almost absent in neuropathic conditions [27,[57][58][59]. Adjuvant analgesics (e.g., antiepileptics, antidepressants) might have limited effects in certain cases, but they could exert several serious adverse effects [60].…”
Section: Discussionmentioning
confidence: 99%
“…There is a strong proof-of-concept that SST 4 is a unique novel drug target for neuropathic pain, which could be also valuable to treat depression as a common comorbidity [ 8 , 9 , 22 , 23 , 24 ]. Non-peptide SST 4 agonists have recently come in the focus of interest of pharma industry [ 25 ].…”
Section: Introductionmentioning
confidence: 99%
“…Based on the methodology of purposeful search of NSAIDs an effective method for the synthesis of 6-spirofused 10-R-3-aryl-6,7-dihydro-2H- [1,2,4]triazino [2,3-c] quinazolin-2-ones (a promising class of anti-inflammatory agents) was proposed. Structural features of the synthesized compounds, as well as their 1 H, 13 C NMR spectroscopy and mass spectrometry data were discussed.…”
Section: соNclusionsmentioning
confidence: 99%
“…Advances in molecular biology in the last decades allowed to characterize every stage of this process and made it possible to form a number of approaches of the creation of this drug group. 3,4 Thus, the main trends in the creation of innovational drugs include the development of С5a receptor antagonists, inhibitors of interleukin converting enzyme and tumor necrosis factor inhibitors, p38 MAP kinase inhibitors, inhibitors of matrix metalloproteinase, etc. Undoubtedly, the mentioned strategy with the use of de novo methodology (molecular docking) and X-ray analysis of the macromolecules active-site has significantly changed the direction of the synthetic work aimed at creating the drugs for correcting the inflammation.…”
Section: Introductionmentioning
confidence: 99%
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