Recent advancements in the development of bioactive pyrazoline derivatives

被引:118
作者
Nehra, Bhupender [1 ]
Rulhania, Sandeep [1 ]
Jaswal, Shalini [1 ]
Kumar, Bhupinder [1 ]
Singh, Gurpreet [1 ]
Monga, Vikramdeep [1 ]
机构
[1] ISF Coll Pharm, Dept Pharmaceut Chem, GT Rd, Moga 142001, Punjab, India
关键词
Pyrazoline; SAR; Anticancer; Antimicrobial; MAO inhibitors; hCA inhibitors; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; ANTICONVULSANT ACTIVITIES; POTENTIAL ANTIMALARIAL; ANTIMICROBIAL ACTIVITY; INHIBITORY-ACTIVITIES; ANTIFUNGAL ACTIVITY; TK INHIBITORS; DESIGN; ANTIBACTERIAL;
D O I
10.1016/j.ejmech.2020.112666
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Pyrazolines remain privileged heterocycles in drug discovery. 2-Pyrazoline scaffold has been proven as a ubiquitous motif which is present in a number of pharmacologically important drug molecules such as antipyrine, ramifenazone, ibipinabant, axitinib etc. They have been widely explored by the scientific community and are reported to possess wide spectrum of biological activities. For combating unprecedented diseases and worldwide increasing drug resistance, 2-pyrazoline has been tackled as a fascinating pharmacophore to generate new molecules with improved potency and lesser toxicity along with desired pharmacokinetic profile. This review aims to summarizes various recent advancements in the medicinal chemistry of pyrazoline based compounds with the following objectives: (1) To represent inclusive data on pyrazoline based marketed drugs as well as therapeutic candidates undergoing preclinical and clinical developments; (2) To discuss recent advances in the medicinal chemistry of pyrazoline derivatives with their numerous biological significances for the eradication of various diseases; (3) Summarizes structureactivity relationships (SAR) including in silico and mechanistic studies to afford ideas for the design and development of novel compounds with desired therapeutic implications. (C) 2020 Elsevier Masson SAS. All rights reserved.
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页数:34
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