16212-34-3Relevant academic research and scientific papers
Syntheses and in Vitro Antiplasmodial Activity of Aminoalkylated Chalcones and Analogues
Wilhelm, Anke,Kendrekar, Pravin,Noreljaleel, Anwar E. M.,Abay, Efrem T.,Bonnet, Susan L.,Wiesner, Lubbe,De Kock, Carmen,Swart, Kenneth J.,Van Der Westhuizen, Jan Hendrik
, p. 1848 - 1858 (2015)
(Chemical Equqation Presented). A series of readily synthesized and inexpensive aminoalkylated chalcones and diarylpropane analogues (1-55) were synthesized and tested against chloroquinone-sensitive (D10 and NF54) and -resistant (Dd2 and K1) strains of Plasmodium falciparum. Hydrogenation of the enone to a diarylpropane moiety increased antiplasmodial bioactivity significantly. The influence of the structure of the amine moiety, A-ring substituents, propyl vs ethyl linker, and chloride salt formation on further enhancing antiplasmodial activity was investigated. Several compounds have IC50 values similar to or better than chloroquine (CQ). The most active compound (26) had an IC50 value of 0.01 μM. No signs of resistance were detected, as can be expected from compounds with structures unrelated to CQ and other currently used antimalarial drugs. Toxicity tests (in vitro CHO cell assay) gave high SI indices.
Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics
Tran, Thanh-Dao,Nguyen, Thi-Thao-Nhu,Do, Tuong-Ha,Huynh, Thi-Ngoc-Phuong,Tran, Cat-Dong,Thai, Khac-Minh
experimental part, p. 6684 - 6696 (2012/08/28)
A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthe
ORGANIC COMPOUNDS
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Page/Page column 141, (2009/09/04)
Compounds of formula (I) in free or salt or solvate form, where T1, T2, X, Ra, Rb, R8 and R9 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
