D 46 Design, synthesis, computational and biological evaluation of new anxiolytics [Text] / A. Geronikaki [и др.]> // Bioorganic and Medicinal Chemistry. - 2004. - Vol. 12, № 24. - P6559-6568 : ил. - Библиогр.: с. 6568 (53 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): 2-INDOLINONES -- ANXIOLYTICS -- FUSED IMIDAZOLES -- SYNTHESIS -- PYRAZOLES -- THIAZOLES Аннотация: New anxiolytics have been discovered by prediction of biological activity with computer programs pass and derek for a heterogeneous set of 5494 highly chemically diverse heterocyclic compounds (thiazoles, pyrazoles, isatins, a-fused imidazoles and others). The majority of tested compounds exhibit the predicted anxiolytic effect. The most potent activity was found in 2-(4-nitrophenyl)-3-(4-phenylpiperazinomethyl)imidazo[1,2-a]pyridine 8, 1-[(4-bromophenyl)-2-oxoethyl]-3-(1,3-dioxolano)-2-indolinone 3, 5-hydroxy-3-methoxycarbonyl-1-phenylpyrazole 5 and 2-(4-fluorophenyl)-3-(4- methylpiperazinomethyl)imidazo[1,2-a]pyridine 7. The application of the computer-assisted approach significantly reduced the number of synthesized and tested compounds and increased the chance of finding new chemical entities (NCEs). |
F 70 Fluoro-containing Heterocycles. IV. Synthesis of Benzimidazole Derivatives [Electronic resource] / S. K. Kotovskaya, N. M. Perova, Z. M. Baskakova, S. A. Romanova, V. N. Charushin, O. N. Chupakhin> // Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii). - 2001. - Vol. 37, № 4. - P564-569 Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: 2-Mercapto-5,6-difluorobenzimidazole reacts with aliphatic and alicyclic ketones in acetic acid in the presence of catalytic amount of sulfuric acid to afford fluorinated derivatives of 2,3-disubstituted benz[4,5]imidazo[2,1-b][1,3]thiazoles. Reaction with aromatic -haloketones occurs in another way: to furnish 2-phenylacylthio-5,6-difluorobenzimidazoles that in the system acetic anhydride-pyridine undergo cyclization into the corresponding fluorinated derivatives of benz[4,5]imidazo[2,1-b][1,3]thiazoles \\\\Expert2\\nbo\\Russian Journal of Organic Chemistry\\2001, 37 (4), 564.pdf |
A 19 Acylation and Carbamoylation of 2-Hydrazinothiazole Derivatives. Identification of Isomeric Structures [Electronic resource] / A. V. Denisova, V. A. Bakulev, W. Dehaen, S. Toppet, L. Van Meerlent, M. I. Kodess> // Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii). - 2005. - Vol. 41, № 4. - P584-590 Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Acylation and carbamoylation of 2-(arylmethylidenehydrazino)- and 2-(aroylhydrazino)thiazoles was performed, and structure of the products was established \\\\Expert2\\nbo\\Russian Journal of Organic Chemistry\\2005, 41 (4), 584.pdf |
S 98 Synthesis of dihydrothiazoles and thiazoles based on monothiooxamides [Text] / V. N. Yarovenko, A. V. Polushina, I. V. Zavarzin, M. M. Krayushkin, S. K. Kotovskaya, V. N. Charushin> // Journal of Sulfur Chemistry. - 2009. - Vol. 30, № 3-4. - P327-337 Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Dihydrothiazoles and thiazoles were synthesized by the reaction of monothiooxamides containing allylamine and propargylamine fragments with halogens in ionic liquids |
F 70 Fluorinated derivatives of benz[4,5]imidazo[2,1-b][1,3]thiazoles are inhibitors of measles viruses [Электронный ресурс] / A. G. Pokrovskii, E. A. Il"ichyova, S. K. Kotovskaya, S. A. Romanova, V. N. Charushin, O. N. Chupakhin> // Doklady Akademii Nauk . - 2004. - Vol.398, №3. - P412-414 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANTIVIRAL ACTIVITY -- CYTOTOXICITY -- FLUORINATED BENZIMIDAZOLES Аннотация: The results of in vitro anti-virus activity investigation for the new benzimidazoles (their synthesis is reported previously) are presented. The activity of the most active compound was studied in dependence of its introduction to the culture (before virus adsorption, simultaneously with virus, directly after virus adsorption, after 6 hours and after 1 day). Preliminary treatment of cells didn't protect them from further infecting; therewith the compound introduction simultaneously with virus or after infection caused no considerable effect on its anti-virus activity. The latter is attributed to blocking of late stages of measles virus reproduction - synthesis or arrangement of virus proteins |
F 70 Fluorinated derivatives of Benz[4,5]imidazo[1,2-b][1,3] thiazole - Inhibitors of reproduction of measles virus [Электронный ресурс] / A. G. Pokrovskii, E. A. Il"ichyova, S. K. Kotovskaya, S. A. Romanova, V. N. Charushin, O. N. Chupakhin> // Doklady Biochemistry and Biophysics . - 2004. - Vol.398, №1-6. - P285-287 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): RIBAVIRIN -- ANTIVIRAL AGENTS -- THIAZOLES |
Bis(azolyl)sulfonamidoacetamides: Synthesis and bioassay / P. S. Sankar, K. N. Babu, V. N. Padmavathi [et al.]> // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020021 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANTIMICROBIALS -- BIOASSAYS -- ANTIFUNGAL Аннотация: Azole derivatives are valuable precursors in pharmacological arena. In fact, oxazole, thiazole and imidazole containing scaffolds display a variety of biological activities such as antitumor,1 antibacterial,2 antiviral,3 antioxidant,4,5 anti-inflammatory6 and antifungal7 activities. Azoles are also prominant molecules in various biochemical and synthetic transformations. Based on the importance of these heteroaromatics and also our interest to link the heterocycle molecules with a variety of functional groups we have synthesized a new class of bis(azolyl)sulfonamide acetamides from azolylsulfonylamines and azolylchloroacetamides in the presence of DMAP under ultrasonication and studied their antimicrobial activity. The compounds chloro substituted bis(thiazoles) (6c) and chloro substituted imidazolyl thiazoles (7c) displayed excellent antibacterial activity against B. subtilis greater than the standard drug, Chloramphenicol. Whereas 7c also showed excellent antifungal activity on A. niger higher than the standard drug, Ketoconazole. |