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

Yasmeen Gull²  Nasir Rasool²  Mnaza Noreen²  Faiz-ul-Hassan Nasim³  Asma Yaqoob³  Shazia Kousar²  Umer Rashid¹  Iftikhar Hussain Bukhari²  Muhammad Zubair² 

[1] Institute of Advanced Technology, Universiti Putra Malaysia, UPM Serdang 43400, Selangor, Malaysia;Department of Chemistry, Governament College University, Faisalabad 38000, Pakistan; E-Mails:;Department of Chemistry, the Islamia University of Bahawalpur, Bahawalpur 63000, Pakistan; E-Mail:

关键词: Suzuki cross coupling;    benzothiazoles;    urease activity;    nitric oxide scavenging activity;   

DOI  :  10.3390/molecules18088845

来源: mdpi

【 摘 要 】

In general, benzothiazole derivatives have attracted great interest due to their 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 100 µg/mL.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.