753026-06-1Relevant academic research and scientific papers
Microwave-Assisted synthesis of novel 1,2,3-triazole derivatives and their antimicrobial activity
Ashok,Mohan Gandhi,Srinivas,Vikas Kumar
, p. 3005 - 3018 (2014/05/06)
An environmentally benign and economic synthesis of 1-[7-(1-benzyl-1H-[1,2, 3]triazol-4-ylmethoxy)-2,2-dimethyl-chroman-6-yl]-3-Aryl-2-propen-1-ones and 1-[5-(1-benzyl-1H-[1,2,3]triazol-4-ylmethoxy)-2,2-dimethyl-chroman-6-yl] -3-Aryl-propen-1-ones is desc
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.
Synthesis, characterisation of new chromanoisoxazoles and investigation of optical power limiting properties
Murthy,Surya Prabha,Shettigar, Seetharam
, p. 361 - 366 (2007/10/03)
Five new chromanoisoxazoles are prepared by the common (3+2) route. Chalcones on condensation with hydroxylamine hydrochloride furnish 3-substituted phenyl-5-(2″,2″-dimethyl-7″ -hydroxychroman)isoxazoles. Chalcones, have been prepared from resorcinol by acetylation. Resacetophenone thus formed on nuclear prenylation with isoprene/PPA affords 7-hydroxy-6-acetyl-2′,2′-dimethylchroman. This on treatment with substituted benzaldehydes forms chalcones 1-5. Compounds 1-5 react with hydroxylamine hydrochloride in the presence of KOH/EtOH resulting in the formation of chromano isoxazoles 6-10, which are identified and characterized by IR, 1H NMR, 13C NMR and mass spectral data. The physico-chemical parameters (absorbance and fluorescence) have been studied for two newly synthesized isoxazoles. Besides the above studies, the optical power limiting performances have also been measured at 532 nm with nano second pulses for the above isoxazoles. The variation of the transmitted power corresponding to the incident power showed a decrease in the transmitted power to a greater extent. The curve corresponding to 7 mm solution path shows that the transmitted power gets saturated with the input intensity which shows the optical limiting behaviour.
