Description
The triazole moiety is present in a large number of FDA-approved drugs, drug candidates, and lead compounds. This heterocycle, for example, is considered as a privileged structure of antifungal compounds that act as P450 enzyme inhibitors.
The following are just a few examples of potential applications
Anticancer
Antibacterial (antitubercular)
Anticonvulsant
Anti-inflammatory
The ChemDiv database contains 4000 unique molecules - various derivatives of 1,2,4-triazoles. We sincerely hope and will be glad if you can choose new objects for your research.
Product Details
Triazole derivatives are used as biologically active substances of various actions, have antibacterial, antipsychotic, hypotensive and antispasmodic activity, stimulate cardiac activity. They are used as ligands in organometallic complexes, as optical brighteners, intermediates for the production of plasticizers, corrosion inhibitors, herbicides (Azaphenidin), catalysts.
1,2,4-triazoles in pharmaceuticals and medicine ]
1,2,4-Triazole hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus.
Ge X, Xu Z.Arch Pharm (Weinheim). 2021 Jan;354(1):e2000223. doi: 10.1002/ardp.202000223. Epub 2020 Sep 28.PMID: 32985011 Review.
Thus, MRSA is an important cause of morbidity and mortality in both hospitals and in the community, creating an urgent demand for the development of novel anti-MRSA candidates. The 1,2,4-triazole nucleus is a bioisostere of amide, ester, and carboxylic …
1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents.
Zhang J, Wang S, Ba Y, Xu Z.Eur J Med Chem. 2019 Jul 15;174:1-8. doi: 10.1016/j.ejmech.2019.04.033. Epub 2019 Apr 16.PMID: 31015103 Review.
This review covers the recent advances of 1,2,4-triazole-quinoline/quinolone hybrids as potential anti-bacterial agents. The structure-activity relationship (SAR) is also discussed for further rational development of 1,2,4-triazoles
Recent Development of 1,2,4-triazole-containing Compounds as Anticancer Agents.
Wen X, Zhou Y, Zeng J, Liu X.Curr Top Med Chem. 2020;20(16):1441-1460. doi: 10.2174/1568026620666200128143230.PMID: 31994462 Review.
1,2,4-Triazole derivatives possess promising in vitro and in vivo anticancer activity, and many anticancer agents such as fluconazole, tebuconazole, triadimefon, and ribavirin bear a 1,2,4-triazole moiety, revealing their po …
Antibacterial activity study of 1,2,4-triazole derivatives.
Gao F, Wang T, Xiao J, Huang G.Eur J Med Chem. 2019 Jul 1;173:274-281. doi: 10.1016/j.ejmech.2019.04.043. Epub 2019 Apr 16.PMID: 31009913 Review.
Antibiotics are commonly used to fight against bacterial infections, but bacteria have already been resistant to almost all antibiotics due to abuse of antibiotics. 1,2,4-Triazole derived compounds possess chemotherapeutic effects including potential a …
1,2,4-Triazole: A Privileged Scaffold for the Development of Potent Antifungal Agents - A Brief Review.
Tratrat C.Curr Top Med Chem. 2020;20(24):2235-2258. doi: 10.2174/1568026620666200704140107.PMID: 32621720 Review.
Despite a large variety of drugs being available to treat invasive candidiasis, only two of them contain a 1,2,4-triazole core, namely Fluconazole and itraconazole, which are efficient in treating infection induced by fungal Candida species. ...Therefo …
Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.
Leenders RGG, Brinch SA, Sowa ST, Amundsen-Isaksen E, Galera-Prat A, Murthy S, Aertssen S, Smits JN, Nieczypor P, Damen E, Wegert A, Nazaré M, Lehtiö L, Waaler J, Krauss S.J Med Chem. 2021 Dec 23;64(24):17936-17949. doi: 10.1021/acs.jmedchem.1c01264. Epub 2021 Dec 8.PMID: 34878777 Free PMC article.
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a plethora of target proteins. ...Based on our 1,2,4-triazole-based lead compound 1 (OM-1700), further structure-activity relat …
Recent advances bioactive 1,2,4-triazole-3-thiones.
Küçükgüzel ŞG, Çıkla-Süzgün P.Eur J Med Chem. 2015 Jun 5;97:830-70. doi: 10.1016/j.ejmech.2014.11.033. Epub 2014 Nov 26.PMID: 25563511 Review.
Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. This review contains various pharmacological activities of 1,2,4-triazole-3-thiones in one place and it is also the milestone …
5-alkylvinyl-1,2,4-triazole nucleosides: Synthesis and biological evaluation.
Prutkov AN, Chudinov MV, Matveev AV, Grebenkina LE, Akimov MG, Berezovskaya YV.Nucleosides Nucleotides Nucleic Acids. 2020;39(7):943-963. doi: 10.1080/15257770.2020.1723624. Epub 2020 Mar 4.PMID: 32126895
The most active substances of the row contain coplanar with the 1,2,4-triazole ring aromatic substituent which is connected by a rigid ethynyl bond. ...We decided to study the antitumor activity of ribavirin analogues with alkyl/aryl vinyl substituents …
Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review.
Kaur R, Dwivedi AR, Kumar B, Kumar V.Anticancer Agents Med Chem. 2016;16(4):465-89. doi: 10.2174/1871520615666150819121106.PMID: 26286663 Review.
1,2,4-triazole is an important nucleus present in a large number of compounds. ...A large number of 1,2,4-triazole derivatives are reported to possess a wide range of bioactivities including anti-cancer activity. ...
4-Alkyl-1,2,4-triazole-3-thione analogues as metallo-beta-lactamase inhibitors.
Gavara L, Legru A, Verdirosa F, Sevaille L, Nauton L, Corsica G, Mercuri PS, Sannio F, Feller G, Coulon R, De Luca F, Cerboni G, Tanfoni S, Chelini G, Galleni M, Docquier JD, Hernandez JF.Bioorg Chem. 2021 Aug;113:105024. doi: 10.1016/j.bioorg.2021.105024. Epub 2021 May 26.PMID: 34116340
This result confirmed the importance of a carboxylic function on the 4-substituent of 1,2,4-triazole-3-thione heterocycle. As observed in previous series, active compounds also preferentially contained phenyl, 2-hydroxy-5-methoxyphenyl, n …
Library Composition
1,2,3-triazole (vicinal triazole, osotriazole) and symmetrical 1,2,4-triazole are two isomeric triazoles. Unsubstituted or C-substituted triazoles can exist in two tautomeric forms
Publications
Keri, Rangappa S.; Patil, Siddappa A.; Budagumpi, Srinivasa; Nagaraja, Bhari Mallanna (2015). "Triazole: A Promising Antitubercular Agent". Chemical Biology & Drug Design. 86 (4): 410–423.
Kaur, Ramandeep; Ranjan Dwivedi, Ashish; Kumar, Bhupinder; Kumar, Vinod (2016). "Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review". Anti-Cancer Agents in Medicinal Chemistry. 16 (4): 465–489.
1,2,4-Triazole hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus. Ge X, Xu Z.Arch Pharm (Weinheim). 2021 Jan;354(1):e2000223.
1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents. Zhang J, Wang S, Ba Y, Xu Z.Eur J Med Chem. 2019 Jul 15;174:1-8.
Recent Development of 1,2,4-triazole-containing Compounds as Anticancer Agents. Wen X, Zhou Y, Zeng J, Liu X.Curr Top Med Chem. 2020;20(16):1441-1460.
Antibacterial activity study of 1,2,4-triazole derivatives. Gao F, Wang T, Xiao J, Huang G.Eur J Med Chem. 2019 Jul 1;173:274-281.
1,2,4-Triazole: A Privileged Scaffold for the Development of Potent Antifungal Agents - A Brief Review. Tratrat C.Curr Top Med Chem. 2020;20(24):2235-2258.
Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. Leenders RGG, Brinch SA, Sowa ST, Amundsen-Isaksen E, Galera-Prat A, Murthy S, Aertssen S, Smits JN, Nieczypor P, Damen E,
Wegert A, Nazaré M, Lehtiö L, Waaler J, Krauss S.J Med Chem. 2021 Dec 23;64(24):17936-17949.
Recent advances bioactive 1,2,4-triazole-3-thiones. Küçükgüzel ŞG, Çıkla-Süzgün P.Eur J Med Chem. 2015 Jun 5;97:830-70.
5-alkylvinyl-1,2,4-triazole nucleosides: Synthesis and biological evaluation. Prutkov AN, Chudinov MV, Matveev AV, Grebenkina LE, Akimov MG, Berezovskaya YV.Nucleosides Nucleotides Nucleic Acids. 2020;39(7):943-963.
Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review. Kaur R, Dwivedi AR, Kumar B, Kumar V.Anticancer Agents Med Chem. 2016;16(4):465-89.
4-Alkyl-1,2,4-triazole-3-thione analogues as metallo-beta-lactamase inhibitors. Gavara L, Legru A, Verdirosa F, Sevaille L, Nauton L, Corsica G, Mercuri PS, Sannio F, Feller G, Coulon R, De Luca F, Cerboni G, Tanfoni S, Chelini G, Galleni M, Docquier JD, Hernandez JF.Bioorg Chem. 2021 Aug;113:105024.
