100634-10-4Relevant academic research and scientific papers
Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents
Tadigoppula, Narender,Korthikunta, Venkateswarlu,Gupta, Shweta,Kancharla, Papireddy,Khaliq, Tanvir,Soni, Awakash,Srivastava, Rajeev Kumar,Srivastava, Kumkum,Puri, Sunil Kumar,Raju, Kanumuri Siva Rama,Wahajuddin,Sijwali, Puran Singh,Kumar, Vikash,Mohammad, Imran Siddiqi
, p. 31 - 45 (2013/02/25)
Licochalcone A (I), isolated from the roots of Chinese licorice, is the most promising antimalarial compound reported so far. In continuation of our drug discovery program, we isolated two similar chalcones, medicagenin (II) and munchiwarin (III), from Crotalaria medicagenia, which exhibited antimalarial activity against Plasmodium falciparum. A library of 88 chalcones were synthesized and evaluated for their in vitro antimalarial activity. Among these, 67, 68, 74, 77, and 78 exhibited good in vitro antimalarial activity against P. falciparum strains 3D7 and K1 with low cytotoxicity. These chalcones also showed reduction in parasitemia and increased survival time of Swiss mice infected with Plasmodium yoelii (strain N-67). Pharmacokinetic studies indicated that low oral bioavailability due to poor ADME properties. Molecular docking studies revealed the binding orientation of these inhibitors in active sites of falcipain-2 (FP-2) enzyme. Compounds 67, 68, and 78 showed modest inhibitory activity against the major hemoglobin degrading cysteine protease FP-2.
A concise synthesis of polyhydroxydihydrochalcones and homoisoflavonoids
Siddaiah, Vidavalur,Rao, Chunduri Venkata,Venkateswarlu, Somepalli,Subbaraju, Gottumukkala V.
, p. 841 - 846 (2007/10/03)
A general and single step synthesis of polyhydroxydihydrochalcones from the readily available phenols and dihydrocinnamic acids using BF 3·Et2O is described. The method allows the synthesis of a wide range of compounds with multiple phenolic hydroxyls and other substituents. These dihydrochalcones are converted into homoisoflavonoids by DMF/PCl5 and the methodology has been applied to the synthesis of naturally occurring phloretin and 5,7-dihydroxy-3-[(4-hydroxyphenyl)methyl]-4H- chromen-4-one. The antioxidant activity of dihydrochalcones and homoisoflavonoids was determined by superoxide free radical (NBT) and DPPH free radical scavenging methods. Polyhydroxydihydrochalcones 3c, 3f, 3g and homoisoflavonoids 4c, 4f, 4g displayed excellent antioxidant activity.
Anti-ulcer agent comprising chalcone derivative as effective ingredient and novel chalcone derivative
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, (2008/06/13)
The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: STR1 wherein X and Y independently stand for a hydrogen atom or together form a single bond, R1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R3 stands for hydroxyl group or a methoxy group, R4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R7 stands for a hydrogen atom or a methoxy group.
