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Journals / Journal of Ongoing Chemical Research / 2017 / Cilt: 3 - Sayı: 1

SYNTHESIS, CHARACTERIZATION, UREASE INHIBITORY AND TYROSINASE INHIBITORY ACTIVITIES OF SOME CHIRAL PYRAZOLO DERIVATIVES

Yusuf SICAK
Said NADEEM
Bedriye Seda Kurşun AKTAR
Emine Elçin ORUÇ EMRE
Mehmet ÖZTÜRK
Ayşegül Karaküçük İYİDOĞAN
Mehmet Ali ÖZLER
İbrahim DEMİRTAŞ
Pages
32–49
Publication Date
2017-06-01
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

According to tyrosinase assay results, compound 2f showed the good tyrosinase inhibitory activity i.e. 6.12±0.40 mM of IC50

📌 3 Key Takeaways

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Objective & Hypothesis:A series of some pyrazolo derivatives a-f were synthesized and their urease inhibitory and tyrosinase inhibitory activities were evaluated.
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Key Findings & Data:Among synthesized compounds, 2f, 2e, 1f, 2d, 1e, 2b, and 1d showed excellent activities IC50 i.e. 11.73±0.28, 14.21±0.56, 15.37±0.89, 17.66±0.82, 18.64±0.19, 19.55±0.39, and 22.08±0.96 µM, respectively.
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Conclusion & Impact:According to tyrosinase assay results, compound 2f showed the good tyrosinase inhibitory activity i.e. 6.12±0.40 mM of IC50
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Pyrrolidine · chiral · thiazolidine-2

Abstract

A series of some pyrazolo derivatives a-f were synthesized and their urease inhibitory and tyrosinase inhibitory activities were evaluated. Among synthesized compounds, 2f, 2e, 1f, 2d, 1e, 2b, and 1d showed excellent activities IC50 i.e. 11.73±0.28, 14.21±0.56, 15.37±0.89, 17.66±0.82, 18.64±0.19, 19.55±0.39, and 22.08±0.96 µM, respectively. According to tyrosinase assay results, compound 2f showed the good tyrosinase inhibitory activity i.e. 6.12±0.40 mM of IC50

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Cite This Article

SICAK, Y., NADEEM, S., AKTAR, B. S. K., EMRE, E. E. O., ÖZTÜRK, M., İYİDOĞAN, A. K., ÖZLER, M. A., DEMİRTAŞ, İ. (2017). SYNTHESIS, CHARACTERIZATION, UREASE INHIBITORY AND TYROSINASE INHIBITORY ACTIVITIES OF SOME CHIRAL PYRAZOLO DERIVATIVES. Journal of Ongoing Chemical Research, Cilt: 3 - Sayı: 1, 32–49. https://ajindex.com/articles/778198

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References (1)

  1. F. Bellina, R. Rossi, Synthesis and biological activity of pyrrole, pyrroline and pyrrolidine derivatives with two aryl groups on adjacent positions, Tetrahedron, 62 (2006) 7213 [2] E. Hensler Mary, G. Bernstein, V. Nizet, A. Nefzi, Pyrrolidine bis-cyclic guanidines with antimicrobial activity against drug-resistant Gram-positive pathogens identified from a mixture-based combinatorial library, Bioorg Med Chem Lett, 16 (2006) 5073-5079 [3] X. Li, Y. Li, W. Xu, Design, synthesis, and evaluation of novel galloyl pyrrolidine derivatives as potential anti-tumor agents, Bioorg Med Chem, 14 (2006) 1287-1293 [4] J. Obniska, A. Zagorska, Synthesis and anticonvulsant properties of new N-[(4- arylpiperazin-1-yl)-methyl] derivatives of 3-aryl pyrrolidine-2,5-dione and 2- azaspiro[4.4]nonane-1,3-dione, Il Farmaco, 58 (2003) 1227-1234 [5] S. Imamura, Y. Ishihara, T. Hattori, O. Kurasawa, Y. Matsushita, Y. Sugihara, N. Kanzaki, Y. Lizawa, M. Baba, S. Hashiquchi, CCR5 antagonists as anti-HIV-1 agents. 1. Synthesis and biological evaluation of 5-oxopyrrolidine-3-carboxamide derivatives, Chem Pharm Bull, 52 (2004) 63-73 [6] F.E. Onen-Bayram, I. Durmaz, D. Scherman, J. Herscovici, R. Cetin- Atalay, A novel thiazolidine compound induces caspase-9 dependent apoptosis in cancer cells, Bioorg Med Chem, 20 (2012) 5094-5102 [7] F.E. Onen-Bayram, K. Buran, I. Durmaz, B. Berk, R. Çetin-Atalay, 3-Propionylthiazolidine-4-carboxylic acid ethyl esters: a family of antiproliferative thiazolidines, Med Chem Commun, 6 (2015) 90-93 [8] P. Prabhakar, H.S. Thatte, R.M. Goetz, M.R. Cho, D.E. Golan, T. Michel, Receptorregulated translocation of endothelial nitric-oxide synthase, J Biol Chem 273 (1998) 27383-27388 [9] N.F. Pavin, F. Donato, F.W. Cibin, C.R. Jesse, P.H. Schneider, H.D. De Salles, L.D.A. Soares, D. Alves, L. Savegnago, Antinociceptive and anti-hypernociceptive effects of Sephenyl thiazolidine-4-carboselenoate in mice, Eur J Pharmacol, 668 (2011) 169-176 [10] L. Del Fabbro, C. Borges Filho, L. Cattelan Souza, L. Savegnago, D. Alves, P. Henrique Schneider, H.D. de Salles, C.R. Jesse, Effects of Se-phenyl thiazolidine-4-carboselenoate on mechanical and thermal hyperalgesia in brachial plexus avulsion in mice: mediation by cannabinoid CB1 and CB2 receptors, Brain Res 1475 (2012) 31-6 [11] N.V. Francine, M.M. Débora, C. Micheli, M.C. Angela, A. Diego, JL. Eder, D.S. Salles, H.S. Paulo, S. Lucielli, Antioxidant properties of (R)-Se-aryl thiazolidine-4- carboselenoate, Chem Biol Inte