Thiazolo[3,2-a]benzimidazoles Synthetic Strategies, Chemical Transformations and Biological Activities 英文参考文献.docVIP

Molecules 2010, 15, 3775-3815; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Thiazolo[3,2-a]benzimidazoles: Synthetic Strategies, Chemical Transformations and Biological Activities Khalid A. Al-Rashood and Hatem A. Abdel-Aziz * Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia * Author to whom correspondence should be addressed; E-Mail: hatem_741@; Tel.: +966-1-467-7338; Fax: +966-1-467-6220. Received: 8 April 2010; in revised form: 11 May 2010 / Accepted: 14 May 2010 / Published: 26 May 2010 Abstract: The present review covers the recent synthetic strategies and chemical transformations of thiazolo[3,2-a]benzimidazoles and it also presents the highlights of the biological activities of these compounds. Keywords: thiazolo[3,2-a]benzimidazole; thiazolo[3,2-a]bezimidazol-3(2H)one; YM- 298198; tilomisole; anticancer activities; MGlu1 antagonists 1. Introduction Thiazolo[3,2- a]benzimidazole systems have been known for more than seven decades [1]. Thiazolo[3,2-a]bezimidazol-3(2H)one (1, Figure 1)) was synthesized in 1926, while thiazolo[3,2- a]-benzimidazole (2, Figure 1) was reported in 1966 [2,3]. Nevertheless, various substituted thiazolo[3,2- a]-benzimidazoles were reported before compound 2 [4–8]. Figure 1. Structure of compounds 1 and 2. O N N S S N 2 N 1  Molecules 2010, 15 3776 In 1988, a review on fused thiazolobenzimidazoles was published by Chimirri et al. [9]. In recent years, there has been considerable interest of researchers in thiazolo[3,2- a]benzimidazoles, stimulated by their biological activities. Additionally an enormous variety of thiazolo[3,2- a]- benzimidazoles with unique pharmaceutical and medicinal applications have been reported in the patent literature. These considerable biologic