Cover Picture: Design, Synthesis, and Structure-Activity Relationship Analysis of Thiazolo[3,2-a ]pyrimidine Derivatives with Anti-inflammatory Activity in Acute Lung Injury (ChemMedChem 13/2017)

ChemMedChem ◽  
2017 ◽  
Vol 12 (13) ◽  
pp. 1013-1013
Author(s):  
Lingfeng Chen ◽  
Yiyi Jin ◽  
Weitao Fu ◽  
Siyang Xiao ◽  
Chen Feng ◽  
...  
Keyword(s):  
Acute Lung Injury ◽  
Lung Injury ◽  
Structure Activity Relationship ◽  
Inflammatory Activity ◽  
Activity Relationship ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Relationship Analysis ◽  
Structure Activity ◽  
Anti Inflammatory

scholarly journals Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

2021 ◽  
Vol 14 (7) ◽  
pp. 663
Author(s):  
Ravichandran Veerasamy ◽  
Anitha Roy ◽  
Rohini Karunakaran ◽  
Harish Rajak
Keyword(s):  
Cannabinoid Receptors ◽  
Transient Receptor Potential ◽  
Structure Activity Relationship ◽  
Inflammatory Activity ◽  
Activity Relationship ◽  
Transient Receptor Potential Vanilloid ◽  
Relationship Analysis ◽  
Structure Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

A significant number of the anti-inflammatory drugs currently in use are becoming obsolete. These are exceptionally hazardous for long-term use because of their possible unfavourable impacts. Subsequently, in the ebb-and-flow decade, analysts and researchers are engaged in developing new anti-inflammatory drugs, and many such agents are in the later phases of clinical trials. Molecules with heterocyclic nuclei are similar to various natural antecedents, thus acquiring immense consideration from scientific experts and researchers. The arguably most adaptable heterocyclic cores are benzimidazoles containing nitrogen in a bicyclic scaffold. Numerous benzimidazole drugs are broadly used in the treatment of numerous diseases, showing promising therapeutic potential. Benzimidazole derivatives exert anti-inflammatory effects mainly by interacting with transient receptor potential vanilloid-1, cannabinoid receptors, bradykinin receptors, specific cytokines, 5-lipoxygenase activating protein and cyclooxygenase. Literature on structure–activity relationship (SAR) and investigations of benzimidazoles highlight that the substituent’s tendency and position on the benzimidazole ring significantly contribute to the anti-inflammatory activity. Reported SAR analyses indicate that substitution at the N1, C2, C5 and C6 positions of the benzimidazole scaffold greatly influence the anti-inflammatory activity. For example, benzimidazole substituted with anacardic acid on C2 inhibits COX-2, and 5-carboxamide or sulfamoyl or sulfonyl benzimidazole antagonises the cannabinoid receptor, whereas the C2 diarylamine and C3 carboxamide substitution of the benzimidazole scaffold result in antagonism of the bradykinin receptor. In this review, we examine the insights regarding the SARs of anti-inflammatory benzimidazole compounds, which will be helpful for researchers in designing and developing potential anti-inflammatory drugs to target inflammation-promoting enzymes.

Sign in / Sign up

Export Citation Format

Share Document