89193-76-0Relevant academic research and scientific papers
Microwave-mediated synthesis of some novel heterocycles containing thiazole, oxazole, thiazine, oxazine, thiadiazine and triazolo-thiadiazine moiety
Dabholkar, Vijay V.,Mishra, Sushil Kumar J.
, p. 2112 - 2117 (2007/10/03)
5,5-Dimethyl cyclohexane-1,3-dione 1 has been brominated to yield 2-bromo-5,5-dimethyl cyclohexane-1,3-dione 2 which on further reaction with substituted thiocarbamides, carbamides, 2-aminothiophenols, 2-aminophenol, thiocarbohydrazones, thiosemicarbazones and triazoles has furnished 2-substituted imino-5,5-dimethyl-2,3,5,6 -tetrahydro-4H-benzothiazol-7-one 3, 2-substituted imino-5,5-dimethyl-2,3,5,6,-tetrahydro-4H-benzoxazol-7-one 4, 7-substituted-2,2-dimethyl-2,3-dihydro-1H,10H -phenothiazin-4-one 5, 2,2-dimethyl-2,3-dihydro-1H,10H-phenoxazin-4-one 6, Schiff base of 2-hydrazino-6,6-dimethyl-6,7-dihydro-4H,5H-benzo[1,3,4]thiadiazin-8-one 7, Schiff base of 2-amino-6,6-dimethyl-6,7-dihydro-4H,5H-benzo[1,3,4] thiadiazin-8-one 8 and 3-substituted alkyl-7,7-dimethyl-7,8-dihydro-5H,6H-1,2,4- triazolo[3,4-b][1,3,4]benzothiadiazin-9-one 9 respectively. All the final compounds have been synthesized by microwave irradiation as well as by conventional method.
Synthesis and antimalarial effects of phenothiazine inhibitors of a plasmodium falciparum cysteine protease
Domínguez, José N.,López, Simón,Charris, Jaime,Iarruso, Lúcido,Lobo, Gricela,Semenov, Andrey,Olson, Jed E.,Rosenthal, Philip J.
, p. 2726 - 2732 (2007/10/03)
Acridinediones have previously been shown to have potent antimalarial activity. A series of sulfur isosteres of acridinediones have been synthesized and evaluated for their inhibition of the Plasmodium falciparum cysteine protease falcipain and for their antimalarial activity. A number of these phenothiazines inhibited falcipain and demonstrated activity against cultured P. falciparum parasites at low micromolar concentrations. We propose that the compounds exerted their antimalarial effects by two mechanisms, one of which involves the inhibition of falcipain and a consequent block in parasite degradation of hemoglobin. Those compounds and related phenothiazines are worthy of further study as potential antimalarial agents.
