Abstract
Background: Thiazole is a widely studied core structure in heterocyclic chemistry and has proven to be a valuable scaffold in medicinal chemistry. The presence of thiazole in both naturally occurring and synthetic pharmacologically active compounds demonstrates the adaptability of these derivatives.
Methods: The current study attempted to review and compile the contributions of numerous researchers over the last 20 years to the medicinal importance of these scaffolds, with a primary focus on antimalarial activity. The review is based on an extensive search of PubMed, Google Scholar, Elsevier, and other renowned journal sites for a thorough literature survey involving various research and review articles.
Results: A comprehensive review of the antimalarial activity of the thiazole scaffold revealed potential therapeutic targets in Plasmodium species. Furthermore, the correlation of structure-activity-relationship (SAR) studies from various articles suggests that the thiazole ring has therapeutic potential.
Conclusion: This article intends to point researchers in the right direction for developing potential thiazole-based compounds as antimalarial agents in the future.
Graphical Abstract
[http://dx.doi.org/10.3390/microorganisms7060179] [PMID: 31234443]
[http://dx.doi.org/10.1038/s41467-022-30133-w] [PMID: 35562368]
[http://dx.doi.org/10.1186/s12916-020-01710-x] [PMID: 32727467]
[http://dx.doi.org/10.1016/j.ejmech.2014.10.058] [PMID: 25455640]
[http://dx.doi.org/10.1007/s00044-017-1910-1]
[http://dx.doi.org/10.1016/j.jsps.2011.05.003] [PMID: 23960775]
[http://dx.doi.org/10.4103/2394-6555.162452]
[http://dx.doi.org/10.1002/chin.200647175]
[http://dx.doi.org/10.3390/ijms15034142] [PMID: 24608926]
[http://dx.doi.org/10.1186/s12929-014-0107-x] [PMID: 25563361]
[http://dx.doi.org/10.1007/s00044-011-9610-8]
[http://dx.doi.org/10.1155/2015/464379]
[http://dx.doi.org/10.1515/chem-2015-0127]
[http://dx.doi.org/10.1371/journal.pone.0135556] [PMID: 26270335]
[http://dx.doi.org/10.1080/10426500802446181]
[http://dx.doi.org/10.3109/14756366.2011.587418] [PMID: 21657948]
[http://dx.doi.org/10.17311/sciintl.2013.253.260]
[http://dx.doi.org/10.1016/j.ejmech.2015.04.015] [PMID: 25934508]
[http://dx.doi.org/10.1021/acs.joc.8b02655] [PMID: 30458618]
[http://dx.doi.org/10.1134/S1070427208050376]
[http://dx.doi.org/10.1134/S1070363209030311]
[http://dx.doi.org/10.1002/cber.188702002200]
[http://dx.doi.org/10.1002/cber.19100430219]
[http://dx.doi.org/10.1039/jr9470001594] [PMID: 18898853]
[http://dx.doi.org/10.4236/jbm.2020.82007]
[http://dx.doi.org/10.1016/j.ejmech.2018.08.040] [PMID: 30261467]
[http://dx.doi.org/10.1021/bi0117549] [PMID: 11841219]
[http://dx.doi.org/10.1021/jm0155704] [PMID: 11855978]
[http://dx.doi.org/10.1021/cc020119z] [PMID: 12739934]
[http://dx.doi.org/10.1021/jm9911027] [PMID: 10669577]
[http://dx.doi.org/10.1128/AAC.47.8.2584-2589.2003] [PMID: 12878523]
[http://dx.doi.org/10.1073/pnas.0404037101] [PMID: 15492221]
[http://dx.doi.org/10.2174/1386207053328219] [PMID: 15720197]
[http://dx.doi.org/10.1128/AAC.47.8.2590-2597.2003] [PMID: 12878524]
[http://dx.doi.org/10.1128/AAC.47.8.2598-2605.2003] [PMID: 12878525]
[http://dx.doi.org/10.1126/science.1067236] [PMID: 11847346]
[http://dx.doi.org/10.1021/jm0492608] [PMID: 15887971]
[http://dx.doi.org/10.1128/AAC.49.9.3631-3639.2005] [PMID: 16127032]
[http://dx.doi.org/10.1016/j.jchromb.2005.03.022] [PMID: 15866496]
[http://dx.doi.org/10.1086/425584] [PMID: 15529265]
[http://dx.doi.org/10.1128/AAC.00840-06] [PMID: 17088482]
[http://dx.doi.org/10.1017/S0031182004006031] [PMID: 15552398]
[http://dx.doi.org/10.1007/s00044-005-0126-y]
[http://dx.doi.org/10.1021/jm0606241] [PMID: 16854088]
[http://dx.doi.org/10.1016/j.bmc.2006.08.035] [PMID: 16971131]
[http://dx.doi.org/10.1016/j.bmcl.2006.11.067] [PMID: 17189694]
[http://dx.doi.org/10.1042/BJ20070692] [PMID: 17714074]
[http://dx.doi.org/10.1021/np700718p] [PMID: 18543965]
[http://dx.doi.org/10.1021/jm061257w] [PMID: 17477517]
[http://dx.doi.org/10.1021/np0605790] [PMID: 17328572]
[http://dx.doi.org/10.1128/AAC.00439-08] [PMID: 18644969]
[http://dx.doi.org/10.1186/1471-2164-9-513] [PMID: 18973684]
[http://dx.doi.org/10.1007/s00044-008-9089-0]
[http://dx.doi.org/10.1021/np800118g] [PMID: 18558743]
[http://dx.doi.org/10.1021/np800409z] [PMID: 18973386]
[http://dx.doi.org/10.1007/s11030-009-9141-0] [PMID: 19347595]
[http://dx.doi.org/10.1016/j.bmcl.2009.03.026] [PMID: 19339178]
[http://dx.doi.org/10.1016/j.bmc.2010.03.058] [PMID: 20403703]
[http://dx.doi.org/10.1002/cmdc.201000097] [PMID: 20540062]
[http://dx.doi.org/10.1039/c0sc00125b]
[http://dx.doi.org/10.1002/cmdc.200900427] [PMID: 19943278]
[http://dx.doi.org/10.1021/jm201108k] [PMID: 21966980]
[http://dx.doi.org/10.1016/j.bmc.2011.06.025] [PMID: 21723734]
[http://dx.doi.org/10.1039/c1md00129a]
[http://dx.doi.org/10.1016/j.bmcl.2011.04.090] [PMID: 21570837]
[http://dx.doi.org/10.1016/j.ejmech.2012.07.034] [PMID: 22889559]
[http://dx.doi.org/10.1016/j.ejmech.2012.07.018] [PMID: 22871486]
[http://dx.doi.org/10.1371/journal.pone.0037171] [PMID: 22629364]
[http://dx.doi.org/10.1039/c2md20136d]
[http://dx.doi.org/10.1016/j.bmcl.2012.06.010] [PMID: 22749280]
[http://dx.doi.org/10.4155/fmc.12.176] [PMID: 23234550]
[http://dx.doi.org/10.1016/j.bmcl.2012.06.028] [PMID: 22765903]
[http://dx.doi.org/10.1111/j.1476-5381.2012.01966.x] [PMID: 22471905]
[http://dx.doi.org/10.1007/s00044-014-0997-x]
[http://dx.doi.org/10.1016/j.bmcl.2013.12.022] [PMID: 24373723]
[http://dx.doi.org/10.3109/14756366.2012.710848] [PMID: 22957722]
[http://dx.doi.org/10.1016/j.ejmech.2013.04.061] [PMID: 23727539]
[http://dx.doi.org/10.1021/jm400279y] [PMID: 23927599]
[http://dx.doi.org/10.1016/j.bmcl.2014.09.071] [PMID: 25316314]
[http://dx.doi.org/10.1016/j.ejmech.2014.06.022] [PMID: 24956553]
[http://dx.doi.org/10.1016/j.ejps.2013.11.001] [PMID: 24231338]
[http://dx.doi.org/10.1039/C4MD00135D]
[http://dx.doi.org/10.4269/ajtmh.13-0565] [PMID: 25184829]
[http://dx.doi.org/10.1016/j.ejmech.2015.02.038] [PMID: 25768697]
[http://dx.doi.org/10.1016/j.ejmech.2015.05.043] [PMID: 26057222]
[http://dx.doi.org/10.1080/1062936X.2014.984628] [PMID: 25567142]
[http://dx.doi.org/10.1002/aoc.3299]
[http://dx.doi.org/10.1128/AAC.04294-14] [PMID: 25779576]
[http://dx.doi.org/10.1021/jm501127s] [PMID: 25580811]
[http://dx.doi.org/10.1016/j.bmcl.2016.07.010] [PMID: 27432764]
[http://dx.doi.org/10.1007/s00044-016-1714-8]
[http://dx.doi.org/10.1128/AAC.01575-15] [PMID: 27139466]
[http://dx.doi.org/10.1016/j.bmcl.2016.05.039] [PMID: 27212070]
[http://dx.doi.org/10.1186/s12936-017-1832-x] [PMID: 28049519]
[http://dx.doi.org/10.1016/j.fjps.2016.09.004]
[http://dx.doi.org/10.1016/j.bmc.2017.07.057] [PMID: 28789907]
[http://dx.doi.org/10.1007/s11164-017-2985-5]
[http://dx.doi.org/10.1016/j.ejmech.2017.11.053] [PMID: 29197733]
[http://dx.doi.org/10.1016/j.ejmech.2018.11.067] [PMID: 30530172]
[http://dx.doi.org/10.1016/j.exppara.2018.01.015] [PMID: 29355497]
[http://dx.doi.org/10.1016/j.molstruc.2018.11.025]
[http://dx.doi.org/10.2174/1570178615666180425120039]
[http://dx.doi.org/10.1016/j.bmcl.2018.08.028] [PMID: 30174152]
[http://dx.doi.org/10.1002/ardp.201900351] [PMID: 32187709]
[http://dx.doi.org/10.1016/j.ejps.2019.105015] [PMID: 31344442]
[http://dx.doi.org/10.1021/acs.jmedchem.9b01099] [PMID: 31566384]
[http://dx.doi.org/10.1038/s41598-019-42801-x] [PMID: 31065005]
[http://dx.doi.org/10.1016/j.pharep.2019.04.006] [PMID: 31351317]
[http://dx.doi.org/10.1016/j.ejps.2020.105382] [PMID: 32470575]
[http://dx.doi.org/10.1002/ardp.201900079] [PMID: 31602690]
[http://dx.doi.org/10.1016/j.bmc.2020.115758] [PMID: 33007559]
[http://dx.doi.org/10.2174/1573407215666190308154139]
[http://dx.doi.org/10.1016/j.mtchem.2020.100335]
[http://dx.doi.org/10.33263/LIANBS101.18461855]
[http://dx.doi.org/10.1002/cmdc.202000331] [PMID: 32813331]
[http://dx.doi.org/10.3389/fmolb.2020.00105] [PMID: 32582763]
[http://dx.doi.org/10.7124/bc.000A20]
[http://dx.doi.org/10.3390/md18030167] [PMID: 32197482]
[http://dx.doi.org/10.1002/cmdc.202000399] [PMID: 32929894]
[http://dx.doi.org/10.1080/08927022.2021.1935926]
[http://dx.doi.org/10.3390/ijms22115659] [PMID: 34073419]
[http://dx.doi.org/10.1016/j.bmcl.2021.127978] [PMID: 33766764]
[http://dx.doi.org/10.1016/j.molstruc.2017.10.077]
[http://dx.doi.org/10.1002/cmdc.202100067] [PMID: 33844432]
[http://dx.doi.org/10.1007/s00044-021-02843-1] [PMID: 35106047]
[http://dx.doi.org/10.55522/jmpas.V11I2.2470]
[http://dx.doi.org/10.47750/pnr.2023.14.03.247]
[http://dx.doi.org/10.1016/j.exppara.2023.108498] [PMID: 36907541]
[http://dx.doi.org/10.2174/1389557523666230726142459] [PMID: 37496137]
[http://dx.doi.org/10.1080/00397911.2020.1854787]
[http://dx.doi.org/10.2174/1570163814666170725114159] [PMID: 28745209]