5809-15-4Relevant academic research and scientific papers
Synthesis, spectral characterization and biological evaluation of a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl)propan-2-yl]-7H-[1,2,4] triazolo[3,4-b][1,3,4]thiadiazines
Puthiyapurayil, Pushpan,Poojary, Boja,Chikkanna, Chandrashekhar,Buridipad, Sunil Kumar
, p. 407 - 416 (2013/01/15)
On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl) propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These compounds were also evaluated for their in-vivo anthelmintic activity, as well as in-vitro antimicrobial studies. Amongst the tested compounds, the compound 7j was the most promising cytotoxic agent with IC50 value of 10.54 μM in MCF-7 cells. The compounds 7l and 7q exhibited excellent anthelmintic activity. The compounds 7d, 7f, 7j, 7l, 7o, 7p and 7r showed good antibacterial activity, whereas compounds 7e and 7k exhibited excellent antifungal activity. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and LCMS analysis.
Synthesis and biological activities of a novel series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles containing gem-dimethylbenzyl moiety
Puthiyapurayil, Pushpan,Poojary, Boja,Kumar, Sunil,Hunnur, Raveendra
experimental part, p. 998 - 1005 (2011/11/06)
A novel series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4- thiadiazoles (6a-r) containing gem-dimethyl benzyl moiety were prepared by the condensation of 4-amino-3-aryl/aralkyl substituted-5-mercapto-1,2,4-triazoles (5a-c) with various fluoro substituted aromatic acids in the presence of POCl3. IR, 1H NMR, 13C NMR, 2D NMR (COSY), and mass spectral data confirmed the structures of all the synthesized compounds. All the compounds were also screened for their antibacterial, antifungal and analgesic activities. Compounds 6b, 6d, 6f, 6g, 6h, 6i, 6m, 6n, 6o, 6p, and 6r exhibited promising antibacterial and compounds 6a, 6d, 6f, 6g, 6h, 6k, 6m, 6o, 6p, and 6q showed significant analgesic activities.
Microwave assisted synthesis of novel pyrazoles
Kidwai,Aryal,Misra
, p. 717 - 718 (2007/10/03)
1,3,4-Trisubstituted pyrazoles synthesized by the reaction of 2-methyl-2-phenylpropanoyl hydrazide with substituted acetophenone followed by Vilsmeier Haack reagent (POCl3/DMF) under microwave irradiation (MWI) and by conventional methods are described. The reaction rate is enhanced tremendously under microwave irradiation as compared to conventional method with improved yields.
Development of orally active nonpeptidic inhibitors of human neutrophil elastase
Ohmoto,Yamamoto,Okuma,Horiuchi,Imanishi,Odagaki,Kawabata,Sekioka,Hirota,Matsuoka,Nakai,Toda,Cheronis,Spruce,Gyorkos,Wieczorek
, p. 1268 - 1285 (2007/10/03)
5-Amino-2-phenylpyrimidin-6-ones, some of their desamino derivatives, and miscellaneous derivatives were synthesized and biologically evaluated on both in vitro activity and oral activity in an acute hemorrhagic assay. These compounds contained an α-keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydroxy group of human neutrophil elastase (HNE). Among those tested, compounds 11a-c,e,i-l(F), 11d,e,k(H), 21d,e,k(F), and 21d,e(H) showed a good oral profile. RS-Mixture 3(H) was selected for clinical evaluation based on its oral potency, duration of action, enzyme selectivity, safety profile, and ease of synthesis. Structure -activity relationships (SARs) are discussed.
