ПЕРСПЕКТИВИ ТІАЗОЛЬНИХ ГЕТЕРОЦИКЛІВ ЯК ІННОВАЦІЙНИХ ПРОТИЗАПАЛЬНИХ АГЕНТІВ: ЛІТЕРАТУРНИЙ ОГЛЯД
DOI:
https://doi.org/10.11603/2312-0967.2026.2.15980Ключові слова:
тіазольні гетероцикли, протизапальна активність, структурно-активнісні залежності, протизапальні засобиАнотація
Мета роботи. Систематизація сучасних літературних даних щодо протизапальної дії гетероциклічних сполук на основі тіазолу, з акцентом на їхню класифікацію, механізми дії, структурно-активнісні залежності, включно з мультифункціональними підходами та "prodrug" (з англ. – "проліки") –концепціями.
Матеріали і методи. Інформаційно-аналітичну основу роботи сформовано шляхом систематизованого пошуку наукових публікацій у міжнародних базах даних Scopus, Web of Science Core Collection, PubMed/MEDLINE та Google Scholar за період 2011–2026 рр. із пріоритетом досліджень на останні 5 років. До аналізу включали повнотекстові оригінальні дослідження з кількісною оцінкою протизапальної активності тіазоловмісних похідних. Узагальнення здійснювали із застосуванням системного, порівняльного та контент-аналізу для встановлення закономірностей «структура-активність» і визначення перспектив структурної оптимізації тіазоловмісних сполук.
Результати й обговорення. Тіазольні гетероцикли займають провідне місце в сучасному хімічному дизайні завдяки своїй структурній гнучкості, високій біологічній активності та можливості багатофункціональної модифікації. Враховуючи глобальне зростання поширеності запальних захворювань, а також обмеження традиційних нестероїдних протизапальних препаратів (НПЗП) через побічні ефекти та резистентність, виникає нагальна потреба у нових протизапальних агентах з підвищеним терапевтичним індексом. У цьому огляді систематизовано сучасні дані щодо класифікації тіазольних сполук з протизапальною активністю, їхніх механізмів дії, а також результатів доклінічних досліджень in vitro (з лат. - "у склі"). Особлива увага приділена перспективам оптимізації молекул через мультифункціональні підходи, "prodrug"-стратегії та гібридизацію фармакофорів.
Висновки. Сформульовано ключові виклики та перспективні напрямки створення потенційних протизапальних агентів на основі тіазольного ядра, включно з необхідністю стандартизації методів оцінки, впровадження комп’ютерного моделювання та ШI (штучний інтелект)-дизайну. Цей огляд створює наукову основу для подальшого розвитку тіазольних протизапальних агентів та їх інтеграції у сучасну фармакотерапію.
Посилання
Chavda VP, Feehan J, Apostolopoulos V. Inflammation: The cause of all diseases. Cells 2024; 13(22):1906. https://doi.org/10.3390/cells13221906 DOI: https://doi.org/10.3390/cells13221906
Del Buono M, Abbate A, Toldo S. Interplay of inflammation, oxidative stress and cardiovascular disease in rheumatoid arthritis. Heart 2018; 104(24):1991-2. https://doi.org/10.1136/heartjnl-2018-313313 DOI: https://doi.org/10.1136/heartjnl-2018-313313
Zhang W, Xiazo D, Mao Q, Xia H. Role of neuroinflammation in neurodegeneration development. Signal Transduct Target Ther. 2023; 8:267. https://doi.org/10.1038/s41392-023-01486-5 DOI: https://doi.org/10.1038/s41392-023-01486-5
Zhang X, Donnan PT, Bell S, Guthrie B. Non-steroidal anti-inflammatory drug induced acute kidney injury in the community dwelling general population and people with chronic kidney disease: systematic review and meta-analysis. BMC Nephrol. 2017; 18:256. https://doi.org/10.1186/s12882-017-0673-8 DOI: https://doi.org/10.1186/s12882-017-0673-8
Oray M, Samra KA, Ebrahimiadib N, Meese H, Foster CS. Long-term side effects of glucocorticoids. Expert Opin Drug Saf. 2016; 15(4):457-65. https://doi.org/10.1517/14740338.2016.1140743 DOI: https://doi.org/10.1517/14740338.2016.1140743
Tapkir AS, Chitlange SS, Bhole RP. Discovery of thiazole based bis heterocyclic system for anti-inflammatory potential. Antiinflamm Antialergy Agents Med Chem. 2017; 16(3):175-92. https://doi.org/10.2174/1871523016666171114165958 DOI: https://doi.org/10.2174/1871523016666171114165958
Tratrat C, Haroun M, Tsolaki E, Petrou A, Gavalas A, Geronikaki A. Thiazole-based chalcone derivatives as potential anti-inflammatory agents: Biological evaluation and molecular modelling. Curr Top Med Chem. 2021; 21(4):257-68. https://doi.org/10.2174/1568026621999201214232458 DOI: https://doi.org/10.2174/1568026621999201214232458
Narasimhamurthy KH, Swaroop TR, Rangappa KS. A review on progress of thiazole derivatives as potential anti-inflammatory agents. Eur J Med Chem Rep. 2024; 12:100225. https://doi.org/10.1016/j.ejmcr.2024.100225 DOI: https://doi.org/10.1016/j.ejmcr.2024.100225
Liaras K, Fesatidou M, Geronikaki A. Thiazoles and thiazolidinones as COX/LOX inhibitors. Molecules 2018; 23(3):685. https://doi.org/10.3390/molecules23030685 DOI: https://doi.org/10.3390/molecules23030685
Jacob PJ, Manju SL. Identification and development of thiazole leads as COX-2/5-LOX inhibitors through in-vitro and in-vivo biological evaluation for anti-inflammatory activity. Bioorg Chem. 2020; 100:103882. https://doi.org/10.1016/j.bioorg.2020.103882 DOI: https://doi.org/10.1016/j.bioorg.2020.103882
Bian M, Ma Q-Q, Wu Y, Du H-H, Guo-Hua G. Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: A review. J Enzyme Inhib Med Chem. 2021; 36(1):2139-59. https://doi.org/10.1080/14756366.2021.1984903 DOI: https://doi.org/10.1080/14756366.2021.1984903
Shou J, Kong X, Wang X, Tang Y, Wang C, Wang M, Zhang L, Liu Y, Fei C, Xue F, Li J, Zhang K. Tizoxanide inhibits inflammation in LPS-activated RAW264.7 macrophages via the suppression of NF-κB and MAPK activation. Inflammation 2019; 42(4):1336-49. https://doi.org/10.1007/s10753-019-00994-3 DOI: https://doi.org/10.1007/s10753-019-00994-3
Cai X, Cai J, Fang L, Xu S, Zhu H, Wu S, Chen Y, Fang S. Design, synthesis and molecular modeling of novel D-ring substituted steroidal 4,5-dihydropyrazole thiazolinone derivatives as anti-inflammatory agents by inhibition of COX-2/iNOS production and down-regulation of NF-κB/MAPKs in LPS-induced RAW264.7 macrophage cells. Eur J Med Chem. 2024; 272:116460. https://doi.org/10.1016/j.ejmech.2024.116460 DOI: https://doi.org/10.1016/j.ejmech.2024.116460
Rosen T, Nagel AA, Rizzi JP, Ives JL, Daffeh JB, Ganong AH, Guarino K, Heym J, McLean S. Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists. J Med Chem. 1990; 33(10):2715-20. https://doi.org/10.1021/jm00172a006 DOI: https://doi.org/10.1021/jm00172a006
Kushwaha P, Pandey S. 1,3-Thiazole derivatives as a promising scaffold in medicinal chemistry: A recent overview. Antiinflamm Antialergy Agents Med Chem. 2023; 22(3):133-63. https://doi.org/10.2174/0118715230276678231102150158 DOI: https://doi.org/10.2174/0118715230276678231102150158
Maghraby MT-E, Abou-Ghadir OMF, Abdel-Moty SG, Ali AY, Salem OIA. Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. Bioorg Med Chem. 2020; 28(7):115403. https://doi.org/10.1016/j.bmc.2020.115403 DOI: https://doi.org/10.1016/j.bmc.2020.115403
Cancela S, Minini L, Mourglia-Ettlin G, Merlino A, Lavaggi ML, Hernandez P. Novel thiazole-nitrone hybrids as innovative neuroprotective agents with antioxidant and antiapoptotic properties. Results Chem. 2025; 16:102414. https://doi.org/10.1016/j.rechem.2025.102414 DOI: https://doi.org/10.1016/j.rechem.2025.102414
Patil SM, Kamble O, Asgaonkar K, Bhandari S, Chitre T, Rathod V, Bhosale P, Gavali P, Das A. Design and development of pyrazole–thiazole hybrid derivatives as anti-inflammatory and anti-oxidant agents. J Mol Struct. 2026; 1353(2):144688. https://doi.org/10.1016/j.molstruc.2025.144688 DOI: https://doi.org/10.1016/j.molstruc.2025.144688
Arshad MF, Alam A, Alshammari AA, Alhazza MB, Alzimam IM, Alam MdA, Mustafa G, Ansari MdS, Alotaibi AM, Alotaibi AA, Kumar S, Asdaq SMB, Irman M, Deb PK, et al. Thiazole: A versatile standalone moiety contributing to the development of various drugs and biologically active agents. Molecules 2022; 27(13):3994. https://doi.org/10.3390/molecules27133994 DOI: https://doi.org/10.3390/molecules27133994
Kamat V, Santosh R, Poojary B, Nayak SP, Kumar BK, Sankaranarayanan M, Faheem, Khanapure S, Baretto DA, Vootla SK. Pyridine- and thiazole-based hydrazides with promising anti-inflammatory and antimicrobial activities along with their in silico studies. ACS Omega. 2020; 5(39):25228-39. https://doi.org/10.1021/acsomega.0c03386 DOI: https://doi.org/10.1021/acsomega.0c03386
Khidre RE, Radini IAM. Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents. Sci Rep. 2021; 11:7846. https://doi.org/10.1038/s41598-021-86424-7 DOI: https://doi.org/10.1038/s41598-021-86424-7
El-Miligy MMM, Al-Kubeisi AK, Nassra RA, El-Zemity SR, Hazzaa AA. Discovery of new thymol-3,4-disubstituted thiazole hybrids as dual COX-2/5-LOX inhibitors with in vivo proof. J Enzyme Inhib Med Chem. 2024; 39(1):2309171. https://doi.org/10.1080/14756366.2024.2309171 DOI: https://doi.org/10.1080/14756366.2024.2309171
El-Achkar GA, Jouni M, Mrad MF, Hirz T, El Hachem N, Khalaf A, Hammoud S, Fayyad-Kazan H, Eid AA, Badran B, Merhi RA, Hachem A, Hamade E, Habib A. Thiazole derivatives as inhibitors of cyclooxygenases in vitro and in vivo. Eur J Pharmacol. 2015; 750:66-73. https://doi.org/10.1016/j.ejphar.2015.01.008 DOI: https://doi.org/10.1016/j.ejphar.2015.01.008
Hawash M, Jaradat N, Sabobeh R, Abualhasan M, Qaoud MT. New thiazole carboxamide derivatives as COX inhibitors: Design, synthesis, anticancer screening, in silico molecular docking, and ADME profile studies. ACS Omega. 2023; 8(32):29512-26. https://doi.org/10.1021/acsomega.3c03256 DOI: https://doi.org/10.1021/acsomega.3c03256
Staś M, Broda MA, Siodłak D. Thiazole-amino acids: Influence of thiazole ring on conformational properties of amino acid residues. Amino Acids 2021; 53:673-86. https://doi.org/10.1007/s00726-021-02974-0 DOI: https://doi.org/10.1007/s00726-021-02974-0
Cascioferro S, Parrino B, Carbone D, Schilacci D, Giovannetti E, Cirrincione G, Diana P. Thiazoles, their benzofused systems, and thiazolidinone derivatives: Versatile and promising tools to combat antibiotic resistance. J Med Chem. 2020; 63(15):7923-56. https://doi.org/10.1021/acs.jmedchem.9b01245 DOI: https://doi.org/10.1021/acs.jmedchem.9b01245
Seboletswe P, Cele N, Singh P. Thiazolidinone-heterocycle frameworks: A concise review of their pharmacological significance. ChemMedChem. 2023; 18(7):e20220618. https://doi.org/10.1002/cmdc.202200618 DOI: https://doi.org/10.1002/cmdc.202200618
Ghafoori H, Rezaei M, Mohammadi A. Anti-inflammatory effects of novel thiazolidinone derivatives as bioactive heterocycles on RAW264.7 cells. Iran J Allergy Asthma Ammunol. 2017; 16(1):28-38.
Hu J, Wang Y, Wei X, Wu X, Chen G, Cao G, Shen X, Zhang X, Tang Q, Liang G, Li X. Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents. Eur J Med Chem. 2013; 64:292-301. https://doi.org/10.1016/j.ejmech.2013.04.010 DOI: https://doi.org/10.1016/j.ejmech.2013.04.010
El-Karim SSA, Mohamed HS, Abdelhameed MF, Amr AE-G, Almehizia AA, Nossier AS. Design, synthesis and molecular docking of new pyrazole-thiazolidinones as potent anti-inflammatory and analgesic agents with TNF-α inhibitory activity. Bioorg Chem. 2021; 111:104827. https://doi.org/10.1016/j.bioorg.2021.104827 DOI: https://doi.org/10.1016/j.bioorg.2021.104827
Faine LA, Rudnicki M, Cesar FA, Heras BL, Bosca L, Souza ES, Hernandes MZ, Galdino SL, Lima MCA, Pitta IR, Abdalla DSP. Anti-inflammatory and antioxidant properties of a new arylidene-thiazolidinedione in macrophages. Curr Med Chem. 2011; 18(22):3351-60. https://doi.org/10.2174/092986711796504600 DOI: https://doi.org/10.2174/092986711796504600
Yadav A, Chawla PA, Wahan SK, Chavla V. Exploring the potential of novel 4-thiazolidinone derivatives as dual anti-inflammatory and antioxidant agents: Synthesis, pharmacological activity and docking analysis. Curr Org Chem. 2025; 29(7):580-90. https://doi.org/10.2174/0113852728301305240828073241 DOI: https://doi.org/10.2174/0113852728301305240828073241
Moraheb R, Al-Omran F, Abdelaziz M, Ibrahim R. Anti-inflammatory and anti-ulcer activities of new fused thiazole derivatives derived from 2-(2-oxo-2H-chromen-3-yl)thiazol-4(5H)-one. Acta Chim Slov. 2017; 64(2):349-64. https://doi.org/10.17344/acsi.2017.3200 DOI: https://doi.org/10.17344/acsi.2017.3200
Chaban T, Matiychuk V, Komarytsya O, Myrko I, Chaban I, Ogurtsov V, Nektegaev I. Anti-inflammatory properties of some novel thiazolo[4,5-b]pyridin-2-ones. Pharmacia. 2020; 67(3):121-7. https://doi.org/10.3897/pharmacia.67.e38969 DOI: https://doi.org/10.3897/pharmacia.67.e38969
Gao D, Jin N, Fu Y, Zhu Y, Wang Y, Wang T, Chen Y, Zhang M, Xiao Q, Huang M, Li Y. Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. Eur J Med Chem. 2021; 216:113333. https://doi.org/10.1016/j.ejmech.2021.113333 DOI: https://doi.org/10.1016/j.ejmech.2021.113333
Kim J, Hong SH, Jeon SH, Park MH, Shin C-G. The novel benzothiazole derivative PB11 induces apoptosis via the PI3K/AKT signaling pathway in human cancer cell lines. Int J Mol Sci. 2021; 22(5):2718. https://doi.org/10.3390/ijms22052718 DOI: https://doi.org/10.3390/ijms22052718
Hegazy ME, Taher ES, Ghiaty AH, Bayoumi AH. Tailored quinoline hybrids as promising COX-2/15-LOX dual inhibitors endowed with diverse safety profile: Design, synthesis, SAR, and histopathological study. Biorg Chem. 2024; 145:107244. https://doi.org/10.1016/j.bioorg.2024.107244 DOI: https://doi.org/10.1016/j.bioorg.2024.107244
Alkorbi F, Alshareef SA, Abdelaziz MA, Omer N, Jame R, Alatawi IS, Ali AM, Omran OA, Bakr RB. Multicomponent reaction for synthesis, molecular docking, and anti-inflammatory evaluation of novel indole-thiazole hybrid derivatives. Mol Divers. 2025; 29(5):3945-56. https://doi.org/10.1007/s11030-024-10969-8 DOI: https://doi.org/10.1007/s11030-024-10969-8
Haroun M, Petrou A, Tratrat C, Kolokotroni A, Fesatidou M, Zagaliotis P, Gavalas A, Venugolapa KN, Sreeharsha N, Nair AB, Elsewedy HS, Geronikaki A. Discovery of 5-methylthiazole-thiazolidinone conjugates as potential anti-inflammatory agents: Molecular target identification and in silico studies. Molecules. 2022; 27(23):8137. https://doi.org/10.3390/molecules27238137 DOI: https://doi.org/10.3390/molecules27238137
Hawash M, Jaradat N, Abualhasan M, Şüküroğlu MK, Qaoud MT, Kahraman DC, Daraghmeh H, Maslamani L, Sawafta M, Ratrout A, Issa L. Design, synthesis, molecular docking studies and biological evaluation of thiazole carboxamide derivatives as COX inhibitors. BMC Chem. 2023; 17(1):11. https://doi.org/10.1186/s13065-023-00924-3 DOI: https://doi.org/10.1186/s13065-023-00924-3
Sinha S, Sravanthi TV, Yuvaraj S, Manju SL, Doble M. 2-Amino-4-aryl thiazole: A promising scaffold identified as a potent 5-LOX inhibitor. RSC Adv. 2016; 6(13):19271-9. https://doi.org/10.1039/C5RA28187C DOI: https://doi.org/10.1039/C5RA28187C
Oniga SD, Pacureanu L, Stoica CI, Palage MD, Craciun A, Rusu LR, Crisan E-L, Araniciu C. COX inhibition profile and molecular docking studies of some 2-(trimethoxyphenyl)-thiazoles. Molecules. 2017; 22(9):1507. https://doi.org/10.3390/molecules22091507 DOI: https://doi.org/10.3390/molecules22091507
Mahnashi MH, Rashid U, Almasoudi HH, Nahari MH, Ahmad I, Binshaya AS, Abdulaziz O, Alsuwat MA, Jan MS, Sadiq A. Modification of 4-(4-chlorothiophen-2-yl)thiazol-2-amine derivatives for the treatment of analgesia and inflammation: Synthesis and in vitro, in vivo, and in silico studies. Front Pharmacol. 2024; 15:1366695. https://doi.org/10.3389/fphar.2024.1366695 DOI: https://doi.org/10.3389/fphar.2024.1366695
Giri RS, Thaker HM, Giordano T, Williams J, Rogers D, Sudersanam V, Vasu KK. Design, synthesis and characterization of novel 2-(2,4-disubstituted-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-κB and AP-1 mediated transcription activation and as potential anti-inflammatory agents. Eur J Med Chem. 2009; 44(5):2184-9. https://doi.org/10.1016/j.ejmech.2008.10.031 DOI: https://doi.org/10.1016/j.ejmech.2008.10.031
Üremiş MM, Üremiş N, Ceylan M, Türköz Y. Anticancer and anti-inflammatory effects of benzothiazole derivatives targeting NF-κB/COX-2/iNOS in a hepatocellular carcinoma cell line. Turk J Pharm Sci. 2025; 22(3):207-16. https://doi.org/10.4274/tjps.galenos.2025.49840. DOI: https://doi.org/10.4274/tjps.galenos.2025.49840
Góral I, Wichur T, Sługocka E, Godyń J, Szałaj N, Zaręba P, Głuch-Lutwin M, Mordyl B, Panek D, Więckowska A. Connecting GSK-3β inhibitory activity with IKK-β or ROCK-1 inhibition to target tau aggregation and neuroinflammation in Alzheimer’s disease–discovery, in vitro and in cellulo activity of thiazole-based inhibitors. Molecules. 2024; 29(11):2616. https://doi.org/10.3390/molecules29112616 DOI: https://doi.org/10.3390/molecules29112616
Tian T, Liu K, Kang Z, Liu H, Li T, Zhang X, Akhtar M, Li F, Lin L. Thiazolo-pyrones as potential anti-inflammatory agents. Eur J Pharmacol. 2025; 1004:178030. https://doi.org/10.1016/j.ejphar.2025.178030 DOI: https://doi.org/10.1016/j.ejphar.2025.178030
Ebaid MS, Ibrahim HAA, Kassem AF, Sabt A. Recent studies on protein kinase signaling inhibitors based on thiazoles: Review to date. RSC Adv. 2024; 14(50):36989-7018. https://doi.org/10.1039/d4ra05601a DOI: https://doi.org/10.1039/D4RA05601A
Ge L, Hu Q, Shi M, Yang H, Zhu G. Design and discovery of novel thiazole derivatives as potential MMP inhibitors to protect against acute lung injury in sepsis rats via attenuation of inflammation and apoptotic oxidative stress. RSC Adv. 2017; 7:32909-22. https://doi.org/10.1039/C7RA03511J DOI: https://doi.org/10.1039/C7RA03511J
Patil KR, Mahajan UB, Unger BS, Goyal SN, Belemkar S, Surana SJ, Ojha S, Patil CR. Animal models of inflammation for screening of anti-inflammatory drugs: Implications for the discovery and development of phytopharmaceuticals. Int J Mol Sci. 2019; 20(18):4367. https://doi.org/10.3390/ijms20184367 DOI: https://doi.org/10.3390/ijms20184367
Manful CF, Fordjour E, Ikumoinein E, Abbey L, Thomas R. Therapeutic strategies targeting oxidative stress and inflammation: A narrative review. BioChem. 2025; 5(4):35. https://doi.org/10.3390/biochem5040035 DOI: https://doi.org/10.3390/biochem5040035
Jaishree V, Ramdas N, Sachin J, Ramesh B. In vitro antioxidant properties of new thiazole derivatives. J Saudi Chem Soc. 2012; 16(4):371-6. https://doi.org/10.1016/j.jscs.2011.02.007 DOI: https://doi.org/10.1016/j.jscs.2011.02.007
Koshelev VN, Primerova OV, Vorobyev SV, Stupnikova AS, Ivanova LV. Synthesis and antioxidant activity of novel thiazole and thiazolidinone derivatives with phenolic fragments. Appl Sci. 2023; 13(24):13112. https://doi.org/10.3390/app132413112 DOI: https://doi.org/10.3390/app132413112
Keshta AT, Ashour HKh. Substituted thiazole derivatives provide corrective anti-tumour and anti-oxidant activities against Ehrlich ascites carcinoma. Dokl Biochem Biophys. 2023; 510(1):123-31. https://doi.org/10.1134/S1607672922600270 DOI: https://doi.org/10.1134/S1607672922600270
Zhong R, Miao L, Zhang H, Tan L, Zhao Y, Tu Y, Prieto A, Simal-Gandara J, Chen L, He C, Cao H. Anti-inflammatory activity of flavonols via inhibiting MAPK and NF-κB signaling pathways in RAW264.7 macrophages. Curr Res Food Sci. 2022; 5:1176-84. https://doi.org/10.1016/j.crfs.2022.07.007 DOI: https://doi.org/10.1016/j.crfs.2022.07.007
Wang M, Xiao Y, Miao J, Zhang X, Liu M, Zhu L, Liu H, Shen X, Wang J, Xie B, Wang D. Oxidative stress and inflammation: Drivers of tumorigenesis and therapeutic opportunities. Antioxidants. 2025; 14(6):735. https://doi.org/10.3390/antiox14060735 DOI: https://doi.org/10.3390/antiox14060735
Sağlık BN, Osmaniye D, Levent S, Çevik UA, Çavuşoğlu BK, Yusuf Özkay Y, Kaplancikli ZA. Design, synthesis and biological assessment of new selective COX-2 inhibitors including methyl sulfonyl moiety. Eur J Med Chem. 2021; 209:112918. https://doi.org/10.1016/j.ejmech.2020.112918 DOI: https://doi.org/10.1016/j.ejmech.2020.112918
Liu M, Yokomizo T. The role of leukotrienes in allergic diseases. Allergol Int. 2015; 64(1):17-26. https://doi.org/10.1016/j.alit.2014.09.001 DOI: https://doi.org/10.1016/j.alit.2014.09.001
Kim ME, Le JS. Advances in the regulation of inflammatory mediators in nitric oxide synthase: Implications for disease modulation and therapeutic approaches. Int J Mol Sci. 2025; 26(3):1204. https://doi.org/10.3390/ijms26031204 DOI: https://doi.org/10.3390/ijms26031204
Fang S, Huang X, Cai F, Qiu G, Lin F, Cai X. Design, synthesis and molecular docking of novel D-ring substituted steroidal 4,5-dihydropyrazole thiazole derivatives that act as iNOS/COX-2 inhibitors with potent anti-inflammatory activity against LPS-induced RAW264.7 macrophage cells. J Steroid Biochem Mol Biol. 2024; 240:106478. https://doi.org/10.1016/j.jsbmb.2024.106478 DOI: https://doi.org/10.1016/j.jsbmb.2024.106478
Facchin BM, Dos Reis GO, Vieira GN, Mohr ETB, da Rosa JS, Kretzer IF, Demarchi IG, Dalmarco EM. Inflammatory biomarkers on an LPS-induced RAW 264.7 cell model: a systematic review and meta-analysis. Inflamm Res. 2022; 71(7-8):741-58. https://doi.org/10.1007/s00011-022-01584-0 DOI: https://doi.org/10.1007/s00011-022-01584-0
Efeoglu C, Taskin S, Selcuk O, Celik B, Tumkaya E, Ece A, Sari H, Seferoglu Z, Ayaz F, Nural Y. Synthesis, anti-inflammatory activity, inverse molecular docking, and acid dissociation constants of new naphthoquinone-thiazole hybrids. Bioorg Med Chem. 2023; 95:117510. https://doi.org/10.1016/j.bmc.2023.117510 DOI: https://doi.org/10.1016/j.bmc.2023.117510
Bhol NK, Bhanjadeo MM, Singh AK, Dash UC, Ojha RR, Majhi S, Duttaray AK, Jena AB. The interplay between cytokines, inflammation, and antioxidants: mechanistic insights and therapeutic potentials of various antioxidants and anti-cytokine compound. Biomed Pharmacoter. 2024; 178:117177. https://doi.org/10.1016/j.biopha.2024.117177 DOI: https://doi.org/10.1016/j.biopha.2024.117177
Lin H-F, Jiang Y-C, Chen Z-W, Zheng L-L. Design, synthesis, and anti-inflammatory activity of indole-2-formamide benzimidazole[2,1-b]thiazole derivative. RSC Adv. 2024; 14:16349-57. https://doi.org/10.1039/D4RA00557K DOI: https://doi.org/10.1039/D4RA00557K
Mittal M, Siddiqui MR, Tran K, Reddy SP, Malik AB. Reactive oxygen species in inflammation and tissue injury. Antioxid Redox Signal. 2014; 20(7):1126-67. https://doi.org/10.1089/ars.2012.5149 DOI: https://doi.org/10.1089/ars.2012.5149
Bansal A, Bali A, Balaini A. Synthesis and evaluation of substituted aryl thiazoles with antioxidant potential as gastro-sparing anti-inflammatory agents. Lett Drug Des Discov. 2020; 17(12):1566-78. https://doi.org/10.2174/1570180817999200706005247 DOI: https://doi.org/10.2174/1570180817999200706005247
Leng SX, McElhaney JE, Walston JD, Xie D, Fedarko NS, Kuchel GA. ELISA and multiplex technologies for cytokine measurement in inflammation and aging research. J Gerontol A Biol Sci Med Sci. 2008; 63(8):879-84. https://doi.org/10.1093/gerona/63.8.879 DOI: https://doi.org/10.1093/gerona/63.8.879
Liou C-J, Len W-B, Wu S-J, Lin C-F, Wu X-L, Huang W-C. Casticin inhibits COX-2 and iNOS expression via suppression of NF-κB and MAPK signaling in lipopolysaccharide-stimulated mouse macrophages. J Ethnopharmacol. 2014; 158:310-6. https://doi.org/10.1016/j.jep.2014.10.046 DOI: https://doi.org/10.1016/j.jep.2014.10.046
Yan Z, Wang Y, Song Y, Ma Y, An Y, Wen R, Wang N, Huang Y, Wu X. Phenethylferulate as a natural inhibitor of inflammation in LPS-stimulated RAW 264.7 macrophages: Focus on NF-κB, Akt and MAPK signaling pathways. BMC Complement Med Ther. 2023; 23:398. https://doi.org/10.1186/s12906-023-04234-y DOI: https://doi.org/10.1186/s12906-023-04234-y
Yue L, Luo J, Zhao C, Zhao J, Ye J, He K, Zou J. Oleanane triterpenoids with C-14 carboxyl group from Astilbe grandis inhibited LPS-induced macrophages activation by suppressing the NF-κB signaling pathway. Front Pharmacol. 2024; 15:1413876. https://doi.org/10.3389/fphar.2024.1413876 DOI: https://doi.org/10.3389/fphar.2024.1413876
Kim E-A, Choi J, Han AR, Choi SY, Hahn H-G, Cho S-W. Anti-oxidative and anti-inflammatory effects of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride on glutamate-induced neurotoxicity in rat brain. NeuroToxicology. 2013; 38:106-14. https://doi.org/10.1016/j.neuro.2013.07.001 DOI: https://doi.org/10.1016/j.neuro.2013.07.001
Hussain F, Tahir A, Rehman HM, Wu Y, Shah M, Rashid U. Promising thiazolidinedione-thiazole based multi-target and neuroprotective hybrids for Alzheimer's disease: Design, synthesis, in-vitro, in-vivo and in-silico studies. Eur J Med Chem. 2025; 287:117327. https://doi.org/10.1016/j.ejmech.2025.117327 DOI: https://doi.org/10.1016/j.ejmech.2025.117327
Hawash M. Thiazole derivatives as modulators of GluA2 AMPA receptors: Potent allosteric effects and neuroprotective potential. Biomolecules. 2023; 13(12):1694. https://doi.org/10.3390/biom13121694 DOI: https://doi.org/10.3390/biom13121694
Islam S, Ahmed MdMS, Islam MA, Hossain N, Chowdhury MA. Advances in nanoparticles in targeted drug delivery – A review. Results Surf Interfaces. 2025; 19:100529. https://doi.org/10.1016/j.rsurfi.2025.100529 DOI: https://doi.org/10.1016/j.rsurfi.2025.100529
Cai N, Gao X, Yang L, Li W, Sun W, Zhang S, Zhao J, Qu J, Zhou Y. Discovery of novel NSAID hybrids as cPLA2/COX-2 dual inhibitors alleviating rheumatoid arthritis via inhibiting p38 MAPK pathway. Eur J Med Chem. 2024; 267:116176. https://doi.org/10.1016/j.ejmech.2024.116176 DOI: https://doi.org/10.1016/j.ejmech.2024.116176
Kumari L, Choudhari Y, Patel P, Gupta GD, Singh D, Rosenholm JM, Bansal KK, Kurmi BD. Advancement in solubilization approaches: A step towards bioavailability enhancement of poorly soluble drugs. Life. 2023; 13(5):1099. https://doi.org/10.3390/life13051099 DOI: https://doi.org/10.3390/life13051099
Arnott JA, Planey SL. The influence of lipophilicity in drug discovery and design. Expert Opin Drug Discov. 2012; 7(10):863-75. https://doi.org/10.1517/17460441.2012.714363 DOI: https://doi.org/10.1517/17460441.2012.714363
Gajula SNR, Nadimpalli N, Sonti R. Drug metabolic stability in early drug discovery to develop potential lead compounds. Drug Metab Rev. 2021; 53(3):459-77. https://doi.org/10.1080/03602532.2021.1970178 DOI: https://doi.org/10.1080/03602532.2021.1970178
Meanwell NA. The influence of bioisosteres in drug design: Tactical applications to address developability problems. Tactics Contemp Drug Des. 2014; 9:283-381. https://doi.org/10.1007/7355_2013_29 DOI: https://doi.org/10.1007/7355_2013_29
Bukke SPN, Venkatesh C, Rajanna SB, Saraswathi TS, Kusuma PK, Goruntla N, Balasuramanyam N, Munishamireddy S. Solid lipid nanocarriers for drug delivery: design innovations and characterization strategies – a comprehensive review. Discov Appl Sci. 2024; 6:279. https://doi.org/10.1007/s42452-024-05897-z DOI: https://doi.org/10.1007/s42452-024-05897-z
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