S 98 Synthesis of new 1,3,4-thiadiazines capable of inhibiting nonenzymatic glycosylation of proteins / L. P. Sidorova, T. A. Tseitler, N. M. Perova [et al.] // Pharmaceutical Chemistry Journal. - 2015. - Vol. 49, № 8. - P501-505. - Bibliogr. : p. 505 (12 ref.) Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): 1,3,4-THIADIAZINE -- CYCLOCONDENSATION -- NONENZYMATIC GLYCOSYLATION OF PROTEINS -- THIOSEMICARBAZIDES Аннотация: A series of new 1,3,4-thiadiazines with cycloalkylamino (cyclopropylamino, cyclobutylamino, cyclopentylamino, cyclohexylamino) groups were synthesized via cyclocondensation of α-haloacetophenones with thiosemicarbazides containing 4-cycloalkyl groups. Five of the synthesized compounds showed the capability to inhibit nonenzymatic glycosylation of proteins in vitro in a model system. The obtained test results allowed compounds containing cyclopropylamino residues (LT-1a and LT-1d) to be recommended for further in vivo testing \\\\expert2\\nbo\\Pharmaceutical Chemistry Journal\\2015, 49 (8), 501-505.pdf |
2-Thiomorpholino-5-aryl-6 H-1,3,4-thiadiazine hydrobromides and their ability to inhibit nonenzymatic protein glycosylation / L. P. Sidorova, T. A. Tseitler, V. V. Emel’yanov [et al.] // Pharmaceutical Chemistry Journal. - 2017. - Vol. 51, № 1. - P9-12 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): GLYCOSYLATION -- ESTERIFICATION -- GLYCOSYL COMPOUNDS -- DEGLYCOSYLATION -- ?-HALOGENACETOPHENONES -- 1,3,4-THIADIAZINE -- 4-MORPHOLINE THIOSEMICARBAZIDES -- CYCLOCONDENSATION -- NONENZYMATIC PROTEIN GLYCOSYLATION Аннотация: Cyclocondensation of α-halogenacetophenones with an original 4-morpholine thiosemicarbazide was used to synthesize a group of new Captions: of the 1,3,4-thiadiazine group, containing a thiomorpholine fragment at position 2 of the thiadiazine ring. Two members of this group of compounds were found to produce effective inhibition of nonenzymatic protein glycosylation in an in vitro model system. These test results allow compounds containing phenyl and fluorophenyl fragments IIIa and IIIb to be recommended for further study in in vivo experiments. \\\\Expert2\\NBO\\Pharmaceutical Chemistry Journal\\2017 v.51 p.9-12.pdf |