TY - JOUR
T1 - 2,4,5-trisubstituted thiazole
T2 - A privileged scaffold in drug design and activity improvement
AU - Zhang, Zhen
AU - Shu, Bing
AU - Zhang, Yaodong
AU - Deora, Girdhar Singh
AU - Li, Qing Shan
PY - 2020
Y1 - 2020
N2 - Thiazole is an important 5-membered heterocyclic compound containing nitrogen and sulfur atoms with various pharmaceutical applications including anti-inflammatory, anti-cancer, anti-viral, hy-poglycemic, anti-bacterial and anti-fungal activities. Until now, the FDA-approved drugs containing thi-azole moiety have achieved great success such as dasatinib and dabrafenib. In recent years, considerable research has been focused on thiazole derivatives, especially 2,4,5-trisubstituted thiazole derivatives, due to their multiple medicinal applications. This review covers related literature in the past 20 years, which reported the 2,4,5-trisubstituted thiazole as a privileged scaffold in drug design and activity im-provement. Moreover, this review aimed to provide greater insights into the rational design of more potent pharmaceutical molecules based on 2,4,5-trisubstituted thiazole in the future.
AB - Thiazole is an important 5-membered heterocyclic compound containing nitrogen and sulfur atoms with various pharmaceutical applications including anti-inflammatory, anti-cancer, anti-viral, hy-poglycemic, anti-bacterial and anti-fungal activities. Until now, the FDA-approved drugs containing thi-azole moiety have achieved great success such as dasatinib and dabrafenib. In recent years, considerable research has been focused on thiazole derivatives, especially 2,4,5-trisubstituted thiazole derivatives, due to their multiple medicinal applications. This review covers related literature in the past 20 years, which reported the 2,4,5-trisubstituted thiazole as a privileged scaffold in drug design and activity im-provement. Moreover, this review aimed to provide greater insights into the rational design of more potent pharmaceutical molecules based on 2,4,5-trisubstituted thiazole in the future.
KW - 2,4,5-trisubstituted thiazole
KW - Anti-cancer
KW - Anti-inflammatory
KW - Biological activity
KW - Structure activity relationships
KW - Supplementary drug design
UR - http://www.scopus.com/inward/record.url?scp=85093951768&partnerID=8YFLogxK
U2 - 10.2174/1568026620999200917153856
DO - 10.2174/1568026620999200917153856
M3 - Review Article
C2 - 32942975
AN - SCOPUS:85093951768
SN - 1568-0266
VL - 20
SP - 2535
EP - 2577
JO - Current Topics in Medicinal Chemistry
JF - Current Topics in Medicinal Chemistry
IS - 28
ER -