Abstract
Background: Pyrazole is a bioactive heterocyclic congener with numerous biological and pharmacological functionalities. Due to their multiple prospective applications, developing innovative and novel pyrazoles and analogs, revealing revolutionary methods for synthesizing this nucleus, investigating diverse potencies of that heterocycle, and exploring possible pyrazole applications are becoming increasingly relevant.
Objectives: Pyrazole scaffolds have been proven successful as antimicrobial, anticancer, and antimalarial therapeutics against multiple targets like DNA gyrase, topoisomerase IV, Hsp90, and several kinase enzymes. For this variability in the biotic zone, their moiety has gained the attention of many scientists interested in researching chemical and pharmacological profiles.
Results: The review covers pyrazole scaffolds with a variety of biological functions and attempts to connect the structure-activity relationship. Multiple pyrazole analogs have been produced as lead compounds, and their activities have been evaluated.
Conclusion: The combination of pyrazole with other pharmacophores in a molecule might lead to novel potent therapeutic medicines, which could aid in the development of potent lead compounds.
Keywords: Pyrazole, heterocyclic congener, antimicrobial, anticancer, antimalarial activities, topoisomerase IV.
Graphical Abstract
[http://dx.doi.org/10.1021/cr300176g] [PMID: 23347156]
[http://dx.doi.org/10.1039/C6NJ03181A]
[http://dx.doi.org/10.3390/molecules24213839] [PMID: 31731387]
[http://dx.doi.org/10.3390/molecules25081909] [PMID: 32326131]
[http://dx.doi.org/10.1021/jo051878h] [PMID: 16388628]
[http://dx.doi.org/10.3390/molecules26113103] [PMID: 34067399]
[http://dx.doi.org/10.1021/jm00036a001] [PMID: 8182695]
[http://dx.doi.org/10.22159/ajpcr.2017.v10i12.22065]
[http://dx.doi.org/10.1039/c2gc16425f]
[http://dx.doi.org/10.1016/j.tetlet.2016.06.019]
[http://dx.doi.org/10.1016/j.bmcl.2004.03.013] [PMID: 15109642]
[http://dx.doi.org/10.1016/j.ejmech.2003.11.012] [PMID: 15051169]
[http://dx.doi.org/10.1016/S0968-0896(02)00533-3] [PMID: 12614881]
[http://dx.doi.org/10.2174/1389557511009011014] [PMID: 20540709]
[http://dx.doi.org/10.1016/j.arabjc.2013.05.029]
[http://dx.doi.org/10.3109/14756366.2012.720572] [PMID: 23030043]
[http://dx.doi.org/10.2174/1573407214666180827094725]
[http://dx.doi.org/10.1016/j.bmcl.2007.03.003] [PMID: 17368897]
[http://dx.doi.org/10.1016/j.coph.2008.04.009] [PMID: 18555745]
[http://dx.doi.org/10.1016/j.ejmech.2011.03.045] [PMID: 21489661]
[http://dx.doi.org/10.1016/j.ejmech.2007.08.002] [PMID: 17923171]
[http://dx.doi.org/10.1016/j.ejmech.2009.12.020] [PMID: 20064677]
[http://dx.doi.org/10.1016/j.bmcl.2010.07.019] [PMID: 20724151]
[http://dx.doi.org/10.1016/j.ejmech.2008.09.029] [PMID: 18995932]
[http://dx.doi.org/10.1016/j.jsps.2011.01.005] [PMID: 23960745]
[http://dx.doi.org/10.1016/j.bmcl.2011.03.101] [PMID: 21530247]
[http://dx.doi.org/10.1016/j.ejmech.2011.05.005] [PMID: 21620535]
[http://dx.doi.org/10.1007/s00044-011-9796-9]
[http://dx.doi.org/10.1016/j.ejmech.2011.01.060] [PMID: 21342734]
[http://dx.doi.org/10.1186/2191-2858-1-8] [PMID: 22373408]
[http://dx.doi.org/10.2174/1871520621666210811105344] [PMID: 34382529]
[http://dx.doi.org/10.3322/caac.21208] [PMID: 24399786]
[http://dx.doi.org/10.1016/j.bioorg.2019.102944] [PMID: 31051400]
[http://dx.doi.org/10.3322/caac.20107] [PMID: 21296855]
[http://dx.doi.org/10.1021/cr900019j] [PMID: 19422222]
[http://dx.doi.org/10.1016/j.bbamcr.2006.10.001] [PMID: 17126425]
[http://dx.doi.org/10.2174/1568009033481787] [PMID: 14529386]
[http://dx.doi.org/10.1016/j.bmcl.2005.08.091] [PMID: 16213716]
[http://dx.doi.org/10.1016/j.ejmech.2010.09.054] [PMID: 20950898]
[http://dx.doi.org/10.1038/nature03097] [PMID: 15549093]
[http://dx.doi.org/10.1038/nrc1296] [PMID: 14993903]
[http://dx.doi.org/10.1021/jm061247v] [PMID: 17352464]
[http://dx.doi.org/10.1016/j.bmcl.2010.12.038] [PMID: 21536432]
[http://dx.doi.org/10.1016/j.bmcl.2007.05.041] [PMID: 17540560]
[http://dx.doi.org/10.1016/j.bmcl.2007.11.074] [PMID: 18055206]
[http://dx.doi.org/10.1016/j.ejmech.2011.08.014] [PMID: 21920636]
[http://dx.doi.org/10.1016/j.bmc.2010.05.034] [PMID: 20627597]
[http://dx.doi.org/10.1016/j.bmc.2009.09.004] [PMID: 19773174]
[http://dx.doi.org/10.1016/j.bmc.2008.10.066] [PMID: 19013820]
[http://dx.doi.org/10.1016/j.ejmech.2008.01.021] [PMID: 18313806]
[http://dx.doi.org/10.1016/j.ejmech.2009.12.039] [PMID: 20097456]
[http://dx.doi.org/10.1016/j.ejmech.2010.07.064] [PMID: 20728965]
[http://dx.doi.org/10.1016/j.bmc.2010.06.046] [PMID: 20638287]
[http://dx.doi.org/10.1007/s00044-011-9563-y]
[http://dx.doi.org/10.1016/j.jinorgbio.2011.09.021] [PMID: 22104300]
[http://dx.doi.org/10.1016/j.ejmech.2018.01.082] [PMID: 29499486]
[http://dx.doi.org/10.1016/j.bmcl.2011.03.037] [PMID: 21493068]
[http://dx.doi.org/10.1021/jm201108k] [PMID: 21966980]
[http://dx.doi.org/10.1021/ci100039k] [PMID: 20426475]
[http://dx.doi.org/10.1016/j.bmcl.2010.05.069] [PMID: 20576433]
[http://dx.doi.org/10.1016/j.bmc.2007.12.054] [PMID: 18194869]
[http://dx.doi.org/10.1016/j.bmcl.2005.10.033] [PMID: 16257205]
[http://dx.doi.org/10.1080/00397910500334561]
[http://dx.doi.org/10.1016/j.ejmech.2013.04.043] [PMID: 23831694]
[http://dx.doi.org/10.1016/j.bmcl.2012.11.024] [PMID: 23228471]
[http://dx.doi.org/10.1016/j.jfluchem.2014.08.017]
[http://dx.doi.org/10.1155/2014/329681]
[http://dx.doi.org/10.1016/j.ejmech.2015.09.021] [PMID: 26408817]
[http://dx.doi.org/10.4067/S0717-97072020000104746]
[http://dx.doi.org/10.3390/molecules23010134] [PMID: 29329257]
[http://dx.doi.org/10.3389/fchem.2019.00917] [PMID: 32039146]
[http://dx.doi.org/10.1016/j.ejmech.2021.113281] [PMID: 33611192]
[http://dx.doi.org/10.1016/j.molstruc.2021.131937]
[http://dx.doi.org/10.1155/2021/5691982]
[http://dx.doi.org/10.1016/j.bioorg.2018.03.002] [PMID: 29571113]
[http://dx.doi.org/10.1016/j.bioorg.2020.103798] [PMID: 32247112]
[http://dx.doi.org/10.1021/cr400270z] [PMID: 24873489]
[http://dx.doi.org/10.1016/j.ejmech.2016.07.034] [PMID: 27474918]
[http://dx.doi.org/10.1021/acs.jmedchem.6b00065] [PMID: 27115835]
[http://dx.doi.org/10.1016/j.bioorg.2018.06.017] [PMID: 29986185]
[http://dx.doi.org/10.3390/antibiotics10081002] [PMID: 34439052]
[http://dx.doi.org/10.3390/molecules25122758]