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Synthesis and Studies of Fluorescein Based Derivatives for their Optical Properties, Urease Inhibition and Molecular Docking.
J Fluoresc. 2018 Nov; 28(6):1305-1315.JF

Abstract

Herein, we design and synthesized new fluorescein based derivatives by insitu formation of fluorescein ester and further treated with corresponding hydrazide and amine to yield respective compounds i.e. FB1, FB2, FB3 and FB4. The spectral purity and characterization was done by using IR, NMR and Mass spectroscopies. The synthesized derivatives were examined for their photophysical properties by using variety of organic solvents and results were discussed in details. The structural diversity of synthesized compounds motivate us to evaluate these compounds for urease inhibition. The compound FB3 (IC50 = 0.0456 μM) shows 100 fold more active against Jack bean urease than standard drug thiourea (IC50 = 4.7455 μM). Other synthesized compounds showed potent activity. Free radical percentage scavenging assay further supported the capacity of compounds to urease inhibition. While, molecular docking simulations helps to examine the molecular interactions of active compounds FB1, FB2, FB3 and FB4 within the binding site of urease enzyme.

Authors+Show Affiliations

Department of Chemistry, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Chemistry, Shivaji University, Kolhapur, Maharashtra, 416004, India.Department of Chemistry, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Division of Bio and Health Sciences, Mokwon University, Seo-gu, Daejeon, 35349, Republic of Korea.Department of Chemistry, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea. khlee@kongju.ac.kr.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30220013

Citation

Mahajan, Prasad G., et al. "Synthesis and Studies of Fluorescein Based Derivatives for Their Optical Properties, Urease Inhibition and Molecular Docking." Journal of Fluorescence, vol. 28, no. 6, 2018, pp. 1305-1315.
Mahajan PG, Dige NC, Vanjare BD, et al. Synthesis and Studies of Fluorescein Based Derivatives for their Optical Properties, Urease Inhibition and Molecular Docking. J Fluoresc. 2018;28(6):1305-1315.
Mahajan, P. G., Dige, N. C., Vanjare, B. D., Raza, H., Hassan, M., Seo, S. Y., Hong, S. K., & Lee, K. H. (2018). Synthesis and Studies of Fluorescein Based Derivatives for their Optical Properties, Urease Inhibition and Molecular Docking. Journal of Fluorescence, 28(6), 1305-1315. https://doi.org/10.1007/s10895-018-2291-7
Mahajan PG, et al. Synthesis and Studies of Fluorescein Based Derivatives for Their Optical Properties, Urease Inhibition and Molecular Docking. J Fluoresc. 2018;28(6):1305-1315. PubMed PMID: 30220013.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and Studies of Fluorescein Based Derivatives for their Optical Properties, Urease Inhibition and Molecular Docking. AU - Mahajan,Prasad G, AU - Dige,Nilam C, AU - Vanjare,Balasaheb D, AU - Raza,Hussain, AU - Hassan,Mubashir, AU - Seo,Sung-Yum, AU - Hong,Seong-Karp, AU - Lee,Ki Hwan, Y1 - 2018/09/15/ PY - 2018/07/13/received PY - 2018/08/28/accepted PY - 2018/9/17/pubmed PY - 2018/12/26/medline PY - 2018/9/17/entrez KW - Fluorescein derivatives KW - Molecular docking KW - Optical properties KW - Synthesis KW - Urease inhibitors SP - 1305 EP - 1315 JF - Journal of fluorescence JO - J Fluoresc VL - 28 IS - 6 N2 - Herein, we design and synthesized new fluorescein based derivatives by insitu formation of fluorescein ester and further treated with corresponding hydrazide and amine to yield respective compounds i.e. FB1, FB2, FB3 and FB4. The spectral purity and characterization was done by using IR, NMR and Mass spectroscopies. The synthesized derivatives were examined for their photophysical properties by using variety of organic solvents and results were discussed in details. The structural diversity of synthesized compounds motivate us to evaluate these compounds for urease inhibition. The compound FB3 (IC50 = 0.0456 μM) shows 100 fold more active against Jack bean urease than standard drug thiourea (IC50 = 4.7455 μM). Other synthesized compounds showed potent activity. Free radical percentage scavenging assay further supported the capacity of compounds to urease inhibition. While, molecular docking simulations helps to examine the molecular interactions of active compounds FB1, FB2, FB3 and FB4 within the binding site of urease enzyme. SN - 1573-4994 UR - https://www.unboundmedicine.com/medline/citation/30220013/Synthesis_and_Studies_of_Fluorescein_Based_Derivatives_for_their_Optical_Properties_Urease_Inhibition_and_Molecular_Docking_ L2 - https://doi.org/10.1007/s10895-018-2291-7 DB - PRIME DP - Unbound Medicine ER -