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Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors.
J Fluoresc. 2018 Nov; 28(6):1295-1304.JF

Abstract

A quinoline functionalized two novel fluorescent Schiff bases, N-(quinolin-2-ylmethylene) anthracen-1-amine (SB1) and 2-(quinolin-2-ylmethyleneamino) benzene thiol (SB2) were synthesized and confirmed by using 1H NMR, IR and GC-MS techniques. The spectroscopic properties were examined by absorption spectroscopy and fluorescence spectroscopy. The absorption and fluorescence spectra of the probes (SB1 and SB2) were measured in a variety of solvents. Both the compounds were tested for urease inhibitory activity. The synthesized compound SB2 proved to be the most effective screening for enzyme inhibitory activity with IC50 = 0.111 μM than SB1 (IC50 = 0.287 μM). Molecular docking studies were performed to delineate the binding affinity and conformational positions of chemical compounds within the active region of the target protein. In-vitro analysis depicts the potency of SB1 in free radical scavenging as compared to the reference drug vitamin C.

Authors+Show Affiliations

Department of Chemistry, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Chemistry, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biological Sciences, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea.Department of Biomedical Engineering, Mokwon University, Seo-gu, Daejeon, 35349, Republic of Korea.Department of Chemistry, College of Natural Sciences, Kongju National University, Gongju, Chungnam, 32588, Republic of Korea. khlee@kongju.ac.kr.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30215145

Citation

Vanjare, Balasaheb D., et al. "Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors." Journal of Fluorescence, vol. 28, no. 6, 2018, pp. 1295-1304.
Vanjare BD, Mahajan PG, Hassan M, et al. Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors. J Fluoresc. 2018;28(6):1295-1304.
Vanjare, B. D., Mahajan, P. G., Hassan, M., Raza, H., Seo, S. Y., Hong, S. K., & Lee, K. H. (2018). Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors. Journal of Fluorescence, 28(6), 1295-1304. https://doi.org/10.1007/s10895-018-2289-1
Vanjare BD, et al. Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors. J Fluoresc. 2018;28(6):1295-1304. PubMed PMID: 30215145.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors. AU - Vanjare,Balasaheb D, AU - Mahajan,Prasad G, AU - Hassan,Mubashir, AU - Raza,Hussain, AU - Seo,Sung-Yum, AU - Hong,Seong-Karp, AU - Lee,Ki Hwan, Y1 - 2018/09/13/ PY - 2018/06/06/received PY - 2018/08/20/accepted PY - 2018/9/15/pubmed PY - 2018/12/26/medline PY - 2018/9/15/entrez KW - Molecular docking KW - Photophysical properties KW - Schiff base KW - Urease inhibition SP - 1295 EP - 1304 JF - Journal of fluorescence JO - J Fluoresc VL - 28 IS - 6 N2 - A quinoline functionalized two novel fluorescent Schiff bases, N-(quinolin-2-ylmethylene) anthracen-1-amine (SB1) and 2-(quinolin-2-ylmethyleneamino) benzene thiol (SB2) were synthesized and confirmed by using 1H NMR, IR and GC-MS techniques. The spectroscopic properties were examined by absorption spectroscopy and fluorescence spectroscopy. The absorption and fluorescence spectra of the probes (SB1 and SB2) were measured in a variety of solvents. Both the compounds were tested for urease inhibitory activity. The synthesized compound SB2 proved to be the most effective screening for enzyme inhibitory activity with IC50 = 0.111 μM than SB1 (IC50 = 0.287 μM). Molecular docking studies were performed to delineate the binding affinity and conformational positions of chemical compounds within the active region of the target protein. In-vitro analysis depicts the potency of SB1 in free radical scavenging as compared to the reference drug vitamin C. SN - 1573-4994 UR - https://www.unboundmedicine.com/medline/citation/30215145/Design_Synthesis_Photophysical_Properties_Biological_Estimation_and_Molecular_Docking_Studies_of_Novel_Schiff_Base_Derivatives_as_Potential_Urease_Inhibitors_ L2 - https://doi.org/10.1007/s10895-018-2289-1 DB - PRIME DP - Unbound Medicine ER -