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Molecules 2013, 18(8), 8845-8857; doi:10.3390/molecules18088845
Article

Efficient Synthesis of 2-Amino-6-Arylbenzothiazoles via Pd(0) Suzuki Cross Coupling Reactions: Potent Urease Enzyme Inhibition and Nitric Oxide Scavenging Activities of the Products

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1 Department of Chemistry, Governament College University, Faisalabad 38000, Pakistan 2 Department of Chemistry, the Islamia University of Bahawalpur, Bahawalpur 63000, Pakistan 3 Institute of Advanced Technology, Universiti Putra Malaysia, UPM Serdang 43400, Selangor, Malaysia 4 Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, UPM Serdang 43400, Selangor, Malaysia
* Authors to whom correspondence should be addressed.
Received: 21 May 2013 / Revised: 24 June 2013 / Accepted: 9 July 2013 / Published: 25 July 2013
(This article belongs to the Section Medicinal Chemistry)
Download PDF [248 KB, 18 June 2014; original version 18 June 2014]

Abstract

In general, benzothiazole derivatives have attracted great interest due to thier pharmaceutical and biological importance. New 2-amino-6-arylbenzothiazoles were synthesized in moderate to excellent yields via Suzuki cross coupling reactions using various aryl boronic acids and aryl boronic acid pinacol esters and the antiurease and nitric oxide (NO) scavenging activity of the products were also examined. The most active compound concerning urease enzyme inhibition was 6-phenylbenzo[d]thiazole-2-amine 3e, with an IC50 value of 26.35 µg/mL. Compound 3c, 6-(4-methoxyphenyl) benzo[d]thiazole-2-amine, exhibited the highest nitric oxide percentage scavenging at 100µg/mL.
Keywords: Suzuki cross coupling; benzothiazoles; urease activity; nitric oxide scavenging activity Suzuki cross coupling; benzothiazoles; urease activity; nitric oxide scavenging activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Gull, Y.; Rasool, N.; Noreen, M.; Nasim, F.-U.-H.; Yaqoob, A.; Kousar, S.; Rashid, U.; Bukhari, I.H.; Zubair, M.; Islam, M.S. Efficient Synthesis of 2-Amino-6-Arylbenzothiazoles via Pd(0) Suzuki Cross Coupling Reactions: Potent Urease Enzyme Inhibition and Nitric Oxide Scavenging Activities of the Products. Molecules 2013, 18, 8845-8857.

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