ABSTRACT
We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate.
Subject(s)
Artemisinins , Cycloaddition Reaction , ParasitesABSTRACT
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disorder that causes progressive muscular weakness, severe weight loss, and ultimately death. Gastrostomy or nasogastric tube is beneficial for ALS patients with severe weight loss and dysphagia. However, the development of superior mesenteric artery (SMA) syndrome in ALS patients when the enteral feeding time is delayed is rarely reported. We report herein the first case of SMA syndrome in a Korean ALS patient who showed improvement after percutaneous endoscopic gastrojejunostomy(PEGJ).