Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies

2021 ◽  
Author(s):  
Xi Wang ◽  
Yuanxun Wang ◽  
Xuemin Li ◽  
Zhenyang Yu ◽  
Chun Song ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Sar Studies ◽  
Structure Activity

This review summarizes versatile nitrile-containing drugs in the following aspects: target, mechanism of action and their structure activity relationship, and categorizes these drugs based on their target diseases.

scholarly journals Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 230
Author(s):  
Daniela Pereira ◽  
Madalena Pinto ◽  
Marta Correia-da-Silva ◽  
Honorina Cidade
Keyword(s):  
Click Chemistry ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Triazole Ring ◽  
Pharmacokinetic Profile ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Antifouling Activity ◽  
Sar Studies ◽  
Structure Activity

As a result of the biological activities of natural flavonoids, several synthetic strategies aiming to obtain analogues with improved potency and/or pharmacokinetic profile have been developed. Since the triazole ring has been associated with several biological activities and metabolic stability, hybridization with a 1,2,3-triazole ring has been increasingly reported over the last years. The feasible synthesis through copper (I) catalyzed azide-alkyne cycloaddition (CuAAC) has allowed the accomplishment of several hybrids. Since 2017, almost 700 flavonoid hybrids conjugated with 1,2,3-triazole, including chalcones, flavones, flavanones and flavonols, among others, with antitumor, antimicrobial, antidiabetic, neuroprotective, anti-inflammatory, antioxidant, and antifouling activity have been reported. This review compiles the biological activities recently described for these hybrids, highlighting the mechanism of action and structure–activity relationship (SAR) studies.

scholarly journals Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure–activity relationship (SAR) studies

2016 ◽  
Vol 111 ◽  
pp. 138-159 ◽  
Author(s):  
Andrea Nuzzi ◽  
Annalisa Fiasella ◽  
Jose Antonio Ortega ◽  
Chiara Pagliuca ◽  
Stefano Ponzano ◽  
...  
Keyword(s):  
Acid Ester ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Carbamic Acid ◽  
Sar Studies ◽  
Structure Activity

Structure–activity relationship of novel low-generation dendrimers for gene delivery

2018 ◽  
Vol 16 (42) ◽  
pp. 7833-7842 ◽  
Author(s):  
Yong-Guang Gao ◽  
Xiao Lin ◽  
Kai Dang ◽  
Shan-Feng Jiang ◽  
Ye Tian ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Sar Studies ◽  
Structure Activity ◽  
Gene Vectors ◽  
Relationship Of

Structure–activity relationship (SAR) studies are very critical to design ideal gene vectors for gene delivery.

scholarly journals Progress on lamellarins

MedChemComm ◽  
2011 ◽  
Vol 2 (8) ◽  
pp. 689-697 ◽  
Author(s):  
Daniel Pla ◽  
Fernando Albericio ◽  
Mercedes Álvarez
Keyword(s):  
Mechanism Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

The latest developments towards the synthesis of lamellarins, their structure–activity relationship and advances in the mechanism of action are described.

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