699-83-2Relevant articles and documents
Synthesis and evaluation of trypanocidal activity of chromane-type compounds and acetophenones
Escobar, Gustavo,González, Luis A.,Qui?ones, Wiston,Robledo, Sara,Upegui, Yulieth
, (2021/12/02)
American trypanosomiasis (Chagas disease) caused by the Trypanosoma cruzi parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process. Some acetophenones and chalcones, as well as chromane-type substances, such as chromones and flavones, are natural products that have been studied as trypanocides, but the relationships between structure and activity are not yet fully understood. In this work, 26 compounds were synthesized to determine the effect of hydroxyl and isoprenyl substituents on trypanocide activity. One of the compounds showed interesting activity against a resistant strain of T. cruzi, with a half effective concentration of 18.3 μM ± 1.1 and an index of selectivity > 10.9.
Rapid synthesis of polyprenylated acylphloroglucinol analogs via dearomative conjunctive allylic annulation
Grenning, Alexander J.,Boyce, Jonathan H.,Porco, John A.
supporting information, p. 11799 - 11804 (2014/10/16)
Polyprenylated acylphloroglucinols (PPAPs) are structurally complex natural products with promising biological activities. Herein, we present a biosynthesis-inspired, diversity-oriented synthesis approach for rapid construction of PPAP analogs via double decarboxylative allylation (DcA) of acylphloroglucinol scaffolds to access allyl-desoxyhumulones followed by dearomative conjunctive allylic alkylation (DCAA).
NaOAc-mediated selective deprotection of aromatic acetates and Its application in the synthesis of natural products
Narender,Reddy, K. Papi,Madhur
experimental part, p. 1949 - 1956 (2009/10/17)
We have developed an efficient method to deacetylate the aromatic acetates using NaOAc in excellent yields and demonstrated the application of the procedure in the synthesis of natural products.