Search results for "Oxazole"
showing 10 items of 227 documents
Thiazole–amino acids: influence of thiazole ring on conformational properties of amino acid residues
2021
Abstract Post-translational modified thiazole–amino acid (Xaa–Tzl) residues have been found in macrocyclic peptides (e.g., thiopeptides and cyanobactins), which mostly inhibit protein synthesis in Gram + bacteria. Conformational study of the series of model compounds containing this structural motif with alanine, dehydroalanine, dehydrobutyrine and dehydrophenylalanine were performed using DFT method in various environments. The solid-state crystal structure conformations of thiazole–amino acid residues retrieved from the Cambridge Structural Database were also analysed. The studied structural units tend to adopt the unique semi-extended β2 conformation; which is stabilised mainly by N–H⋯N…
Synthesis of Isoxazole and 1,2,3-Triazole Isoindole Derivatives via Silver- and Copper-Catalyzed 1,3-Dipolar Cycloaddition Reaction.
2016
International audience; The CuI-or Ag 2 CO 3-catalyzed [3+2] cycloaddition of propargyl-substituted dihydroisoindolin-1-one (3) with arylnitrile oxides 1a-d (Ar = Ph, p-MeC 6 H 4 , p-MeOC 6 H 4 , p-ClC 6 H 4) produces in good yields novel 3,5-disubstituted isoxazoles 4 of the ethyl-2-benzyl-3-oxo-1-((3-arylisoxazol-5yl)methyl)-2,3-dihydro-1H-isoindole-1-carboxylate type. With aryl azides 2a-d (Ar = Ph, p-MeC 6 H 4 , p-OMeC 6 H 4 , p-ClC 6 H 4), a series of 1,4-disubstituted 1,2,3-triazoles 6 (ethyl-2-benzyl-3-oxo-1-((1-aryl-1H-1,2,3-triazol-4-yl)methyl)-2,3-dihydro-1H-isoindole-1-carboxylates) was obtained. The reactions proceed in a regioselective manner affording exclusively racemic adduc…
SYNTHESIS AND ANTITUMOR ACTIVITY OF 2,5-BIS(3'-INDOLYL)-FURANS AND 3,5-BIS(3'-INDOLIY)-ISOXAZOLES, NORTOPSENTIN ANALOGUES
2010
Abstract A series of novel 2,5-bis(3′-indolyl)furans and 3,5-bis(3′-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC50 values of 17.4 μg/mL (3a) and 20.5 μg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.
CCDC 160805: Experimental Crystal Structure Determination
2001
Related Article: E.Aiello, S.Aiello, F.Mingoia, A.Bacchi, G.Pelizzi, C.Musiu, M.G.Setzu, A.Pani, P.La Colla, M.E.Marongiu|2000|Bioorg.Med.Chem.|8|2719|doi:10.1016/S0968-0896(00)00211-X
CCDC 2051973: Experimental Crystal Structure Determination
2021
Related Article: Jan Sietmann, Mike Ong, Christian Mück-Lichtenfeld, Constantin G. Daniliuc, Johannes M. Wiest|2021|Angew.Chem.,Int.Ed.|60|9719|doi:10.1002/anie.202100642
CCDC 906031: Experimental Crystal Structure Determination
2013
Related Article: Pekka K.Poutiainen ,Jorma J.Palvimo,Ari E.Hinkkanen,Arto Valkonen,Topi K.Vaisanen,Reino Laatikainen,Juha T.Pulkkinen|2013|J.Med.Chem.|56|1064|doi:10.1021/jm301516q
CCDC 906030: Experimental Crystal Structure Determination
2013
Related Article: Pekka K.Poutiainen ,Jorma J.Palvimo,Ari E.Hinkkanen,Arto Valkonen,Topi K.Vaisanen,Reino Laatikainen,Juha T.Pulkkinen|2013|J.Med.Chem.|56|1064|doi:10.1021/jm301516q
Mossbauer spectroscopic study of the thermal spin crossover in [Fe(II)(isoxazole)(6)](ClO(4))(2)
2008
The (57)Fe Mossbauer spectroscopy of mononuclear [Fe(II)(isoxazole)(6)](ClO(4))(2) has been studied to reveal the thermal spin crossover of Fe(II) between low-spin (S = 0) and high-spin (S = 2) states.Temperature-dependent spin transition curves have been constructed with the least-square fitted data obtained from the Mossbauer spectra measured at various temperatures between 84 and 270 K during a cooling and heating cycle. This compound exhibits an unusual temperature-dependent spin transition behaviour with T(C)(down arrow) = 223 and T(C)(up arrow) = 213 K occurring in the reverse order in comparison to those observed in SQUID observation and many other spin transition compounds. The comp…
CCDC 1561793: Experimental Crystal Structure Determination
2017
Related Article: Tile Gieshoff, Anton Kehl, Dieter Schollmeyer, Kevin D. Moeller, Siegfried R. Waldvogel|2017|J.Am.Chem.Soc.|139|12317|doi:10.1021/jacs.7b07488
Perspectives for the Treatment of Brucellosis in the 21st Century: The Ioannina Recommendations
2007
Policy Forum. Competing interests: ER has received research grants from Daiichi, Bayer, and Theravance and has served as a consultant to Pfizer, Theravance, Bayer, Wyeth, Rosetta, and BiondVax. Summary Points Brucellosis remains the commonest anthropozoonosis worldwide, and its treatment remains complex, requiring protracted administration of more than one antibiotic. In November 2006, a consensus meeting aimed at reaching a common specialist statement on the treatment of brucellosis was held in Ioannina, Greece under the auspices of the International Society of Chemotherapy and the Institute of Continuing Medical Education of Ioannina. The author panel suggests that the optimal treatment o…