Synthesis, anti-inflammatory evaluation, and docking studies of some new thiazole derivatives

Deb, Pran Kishore; Kaur, Rajwinder; Chandrasekaran, Balakumar; Bala, Madhu; Gill, Dilshad; Kaki, Venkata Rao; Akkinepalli, Raghuram Rao; Mailavaram, Raghuprasad

doi:10.1007/s00044-013-0861-4

Cited by 47 publications

(13 citation statements)

References 32 publications

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“…This glycocalyx disturbance was avoided by an infusion of antioxidant N ‐acetylcysteine, which suggests that the development of ROS leads to glycocalyx dislocation under the conditions of hyperglycemia. [ 59,60 ]…”

Section: The Egx In the Pathophysiologymentioning

confidence: 99%

A review on the physiological and pathophysiological role of endothelial glycocalyx

Liu

Xuan

et al. 2020

J Biochem & Molecular Tox

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The glycocalyx is a gel‐like layer covering the luminal surface of vascular endothelial cells. It comprises of membrane‐attached proteoglycans, glycosaminoglycan chains, glycoproteins, and adherent plasma proteins. The glycocalyx maintains homeostasis of the vasculature, which includes controlling vascular permeability and microvascular tone, preventing microvascular thrombosis, and regulating leukocyte adhesion. In the past decades, the number of studies on endothelial glycocalyx has steadily grown. Glycocalyx emerged as an essential part of blood vessels involved in multiple physiological functions. Damage to glycocalyx is associated with many types of diseases. The structure and physiology and pathophysiology of the glycocalyx, as well as the clinical effects of glycocalyx degradation, are addressed throughout this study. We strive in particular to define therapeutic approaches for the survival or reparation of the glycocalyx.

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Section: The Egx In the Pathophysiologymentioning

confidence: 99%

A review on the physiological and pathophysiological role of endothelial glycocalyx

Liu

Xuan

et al. 2020

J Biochem & Molecular Tox

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“…Several atempts were made to extensively manipulate the ring system that is fused with the cis-stilbene system to include every possible heterocyclic ring of varying sizes as well as by altering the scafolds of classical NSAIDs to convert them into COX-2 selective inhibitors, but none could successfully reach the market. Recently, a series of thiazole derivatives [21], cycloalkyl/aryl-3,4,5-trimethylgallates [22], thienopyrimidine derivatives [23], 3-alkoxy-4-methanesulfonamido acetophenone derivatives [24] and 8/10-triluoromethyl-substituted-imidazo[1,2-c]quinazolines [25], have been designed, synthesised and reported from our research group in search of compounds with novel scafold as potent anti-inlammatory agents.…”

Section: Progress In the Pursuit Of The Development Of Cyclooxygenasementioning

confidence: 99%

Molecular Basis of Binding Interactions of NSAIDs and Computer-Aided Drug Design Approaches in the Pursuit of the Development of Cyclooxygenase-2 (COX-2) Selective Inhibitors

Deb¹,

Mailabaram²,

Al-Jaidi³

et al. 2017

Nonsteroidal Anti-Inflammatory Drugs

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The nonsteroidal anti-inlammatory drugs (NSAIDs) are important class of therapeutic agents used for the treatment of pain, inlammation and fever. Nonselective inhibition of cyclooxygenase (COX-1 and COX-2) isoenzymes by classical NSAIDs is associated with undesirable side efects such as gastrointestinal (GI) and renal toxicities due to COX-1 inhibition. To circumvent this problem, several COX-2 selective inhibitors were developed with superior GI safety proile. However, the voluntary market withdrawal of potent COX-2 selective inhibitors (rofecoxib and valdecoxib) due to their severe cardiovascular toxicity which is also found to be associated with some of the traditional NSAIDs suggesting the need to relook into the entire class of NSAIDs rather than exclusively victimizing the COX-2 selective inhibitors. Furthermore, the recent evidences for the involvement of COX-2 selective inhibitors in the aetiology of many diseases, such as Alzheimer's disease, Parkinson's disease, diabetes, various cancers and so on, have gained much atention for researchers to design and develop novel COX-2 selective inhibitors with improved pharmacodynamics and pharmacokinetic proile. This chapter is focused on the detailed analysis of molecular basis of binding interactions of various NSAIDs by highlighting the role of crucial amino acid residues at the binding site of cyclooxygenase enzymes (COXs) to be considered for selective inhibition of COX-2 enzyme while emphasising the impact of signiicant CADD strategies employed for designing new potent COX-2 inhibitors with tuned selectivity.

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“…Therefore, a dual COX inhibitory-antibacterial agent with an improved safety profile is necessary for enhanced therapeutic benefits and better patient compliance. Prompted from this requirement lot of studies have been reported [28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43] . As a result, above-mentioned information directed us to synthesize some novel 2-(4-substitutedmethylphenyl)propionic acid derivatives and investigate their inhibitory activity against COX-1, COX-2 enzymes and various microbial strains.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents

Gençer

Çevik

Çavuşoğlu

et al. 2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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A series of 2-(4-substitutedmethylphenyl)propionic acid derivatives (6a-6m) were synthesized, characterized and evaluated for cyclooxygenase (COX) enzyme inhibitory and antimicrobial activity. Test compounds that exhibited good COX inhibition and antibacterial activity were further screened for their cytotoxicity and genotoxicity. Compounds 6h and 6l showed better COX-1 and COX-2 inhibition when compared to ibuprofen. Inhibition potency of these compounds against COX-2 was very close to that of nimesulide. The compounds 6d, 6h, 6l and 6m displayed promising antibacterial property when compared to chloramphenicol. However, the compound 6l was emerged as the best dual COX inhibitory-antibacterial agent in this study. The ADME prediction of the compounds revealed that they may have a good pharmacokinetic profile. Docking results of the compounds 6h and 6l with COX-1 (PDB ID: 1EQG) also exhibited a strong binding profile. ARTICLE HISTORY

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Synthesis, anti-inflammatory evaluation, and docking studies of some new thiazole derivatives

Cited by 47 publications

References 32 publications

A review on the physiological and pathophysiological role of endothelial glycocalyx

A review on the physiological and pathophysiological role of endothelial glycocalyx

Molecular Basis of Binding Interactions of NSAIDs and Computer-Aided Drug Design Approaches in the Pursuit of the Development of Cyclooxygenase-2 (COX-2) Selective Inhibitors

Design, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents

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