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Molecules 2016, 21(3), 266; doi:10.3390/molecules21030266

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

1
Department of Chemistry, Faculty of Science and Technology, Government College University Faisalabad, Faisalabad 38000, Pakistan
2
Department of Chemistry, Faculty of Science, University of Sargodhah, Bhakkar Campus, Bhakkar 30000, Pakistan
3
Department of Chemistry, Faculty of Science, University of Gujrat, Hafiz Hayat Campus, Gujrat 50700, Pakistan
4
International Center for Chemical and Biological Sciences, Hussain Ebrahim Jamal Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan
5
Department of Chemistry, Faculty of Science, Islamia University of Bahawalpur, Bahawalpur 63000, Pakistan
6
Department of Pharmaceutical and Biomedical Sciences, University of Salerno, Via Ponte don Melillo, Fisciano (Salerno) I-84084, Italy
7
Offices of Research, Innovation and Commercialization, Lahore College for Women University, Lahore 54600, Pakistan
*
Authors to whom correspondence should be addressed.
Academic Editor: Maxim L. Kuznetsov
Received: 31 December 2015 / Revised: 29 January 2016 / Accepted: 1 February 2016 / Published: 25 February 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [6380 KB, uploaded 25 February 2016]   |  

Abstract

A new series of N-(6-arylbenzo[d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition. View Full-Text
Keywords: Suzuki cross coupling; Pd(0) catalyst; benzothiazole; nitric oxide scavenging activity; antiurease activity; haemolytic activity Suzuki cross coupling; Pd(0) catalyst; benzothiazole; nitric oxide scavenging activity; antiurease activity; haemolytic activity
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Gull, Y.; Rasool, N.; Noreen, M.; Altaf, A.A.; Musharraf, S.G.; Zubair, M.; Nasim, F.-U.-H.; Yaqoob, A.; DeFeo, V.; Zia-Ul-Haq, M. Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach. Molecules 2016, 21, 266.

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