Compound 2-(5-(3-bromophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenyl thiazole (5a) exhibited the most potent antiurease activity with IC50 of 2,28±0,02, which was comparable to the positive control.
📌 3 Key Takeaways
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Objective & Hypothesis:Six thiazolyl-pyrazoline derivatives were synthesized starting from corresponding chalcone compounds for their antioxidant capacity and antiurease inhibitory activities.
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Key Findings & Data:In addition to the conventional method, ultrasonic sonication and microwave irradiation methods which are environmental methods were used in the synthesis stage.
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Conclusion & Impact:Compound 2-(5-(3-bromophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenyl thiazole (5a) exhibited the most potent antiurease activity with IC50 of 2,28±0,02, which was comparable to the positive control.
Six thiazolyl-pyrazoline derivatives were synthesized starting from corresponding chalcone compounds for their antioxidant capacity and antiurease inhibitory activities. In addition to the conventional method, ultrasonic sonication and microwave irradiation methods which are environmental methods were used in the synthesis stage. Compound 2-(5-(3-bromophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenyl thiazole (5a) exhibited the most potent antiurease activity with IC50 of 2,28±0,02, which was comparable to the positive control.
MERMER, A. (2020). Microwave and ultrasound promoted greener synthesis of thiazolyl-pyrazoline derivatives and investigation of their biological activities. Journal of the Turkish Chemical Society Section A: Chemistry, Cilt: 7 - Sayı: 1, 25–36. https://ajindex.com/articles/781235
Rostom SAF, El-Ashmawy IM, El Razik H.A.A, Badr MH, Ashour HMA. Design and synthesis of some thiazolyl and thiadiazolyl derivatives of antipyrine as potential non-acidic anti-inflammatory, analgesic and antimicrobial agents. Bioorg Med Chem. 2009; 17: 882-895
Al-Saadi MS, Faidallah HM, Rostom SAF. Synthesis and biological evaluation of some 2,4,5‐trisubstituted thiazole derivatives as potential antimicrobial and anticancer agents. Arch Pharm Chem Life Sci. 2008; 341: 424-434
Li Z, Yang Q, Qian X. Novel thiazonaphthalimides as efficient antitumor and DNA photocleaving agents: Effects of intercalation, side chains, and substituent groups. Bioorg Med Chem. 2005; 13: 4864-4870
Li FY, Guo XF, Fan ZJ, Zhang YQ, Zong GN, Qian XL, Ma LY, Chen L, Zhu YJ, Tatiana K, Morzherin YY, Belskaya NP. Synthesis and biological activities of novel 2-amino-1,3-thiazole-4-carboxylic acid derivatives. Chinese Chem Lett. 2015; 26: 1315-1318
Tenórioa RP, Carvalho CS, Pessanha CS, de Lima JG, de Faria AR, Alves AJ, de Melo EJT, Góes AJS. Synthesis of thiosemicarbazone and 4-thiazolidinone derivatives and their in vitro anti-Toxoplasma gondii activity. Bioorg Med Chem. Lett. 2005; 15: 2575-2578
Karthikeyan, MS. Synthesis, analgesic, anti-inflammatory and antimicrobial studies of 2,4- 8. Scherman WR, Dickson DE. 4-(5-Nitro-2-furyl)thiazoles1a. J Org Chem. 1952; 27: 1351-1355. 9. de Aquino TM, Liesen AP, da Silva REA, Lima VT, Carvalho CS, de Faria AR, de Araújo JM, de Lima JG, Alves AJ, de Melo EJT, Góes AJS. Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids. Bioorg Med Chem. 2008; 16: 446-456
Taha M, Ismail NH, Imran S, Wadood A, Rahim F, Khan KM, Riaz M. Hybrid benzothiazole analogs as antiurease agent: Synthesis and molecular docking studies. Bioorg Chem. 2016; 66: 80-87
Tuncbilek M, Altanlar N. Synthesis of New 3‐(substituted phenacyl)‐5‐[3′‐(4h‐4‐oxo‐1‐benzopyran ‐2‐yl)‐benzylidene]‐2,4‐thiazolidinediones and their antimicrobial activity. Arch Pharm Chem Life Sci. 2006; 339: 213-216