39573-31-4Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF AMYLOID-RELATED DISEASES
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Paragraph 0192, (2020/08/28)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
CRBN LIGANDS AND USES THEREOF
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Paragraph 00412; 00414, (2019/08/20)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
Highly efficient tandem syntheses of unsymmetrically substituted isomeric S,N-disubstituted-2-mercaptobenzimidazoles
Rao, S. Srinivas,Reddy, Ch Venkata Ramana,Dubey
, p. 829 - 832 (2015/06/30)
Highly efficient tandem syntheses of unsymmetrically substituted isomeric S,N-disubstituted-2-mercaptobenzimidazoles have been developed. The structures of 6a-d and isomeric compounds 9a-d have been synthesized from 2-mercaptobenzimidazole using tandem synthesis. The structures of 6a-d and isomeric compounds 9a-d have been established by spectral and analytical data, and by unambiguous syntheses.
A green and simple synthesis of N-substituted-2-mercaptobenzimidazoles
Rao, S Srinivas,Dubey,Kumari, Y Bharathi
, p. 1210 - 1213 (2013/10/08)
A green and simple synthesis of N-alkyl-2-mercaptobenzimidazoles 5 (R= CH3, C2H5, CH2Ph) under, different conditions has been developed from N-alkyl-2-chlorobenzimidazole (i.e. CH 3, C2H5, CH2Ph) 4 by reaction with thiourea by physical grinding or by using green solvents like ethanol, PEG-600, etc. or by using micro-wave irradiation technique. Copyright
Design of benzimidazole- and benzoxazole-2-thione derivatives as inhibitors of bacterial hyaluronan lyase
Braun, Stephan,Botzki, Alexander,Salmen, Sunnhild,Textor, Christian,Bernhardt, Günther,Dove, Stefan,Buschauer, Armin
experimental part, p. 4419 - 4429 (2011/11/06)
Bacterial hyaluronan lyases (Hyal) degrade hyaluronan, an important component of the extracellular matrix, and are involved in microbial spread. Hyal inhibitors may serve as tools to study the role of the enzyme, its substrates and products in the course of bacterial infections. Moreover, such enzyme inhibitors are potential candidates for antibacterial combination therapy. Based on crystal structures of Streptococcus pneumoniae Hyal in complex with a hexasaccharide substrate and with different inhibitors, 1-acylated benzimidazole-2-thiones and benzoxazole-2-thiones were derived as new leads for the inhibition of Streptococcus agalactiae strain 4755 Hyal. Structure-based optimization led to N-(3-phenylpropionyl)benzoxazole-2-thione, one of the most potent compounds known to date (IC50 values: 24 μM at pH 7.4, 15 μM at pH 5). Among the 27 new derivatives, other N-acylated benzimidazoles and benzoxazoles are just as active at pH 7.4, but not at pH 5. The results support a binding mode characterized by interactions with residues in the catalytic site and with a hydrophobic patch.
Synthesis, antitrichinnellosis and antiprotozoal activity of some novel thieno[2,3-d]pyrimidin-4(3H)-ones containing benzimidazole ring
Mavrova, Anelia Ts.,Vuchev, Dimitar,Anichina, Kameliya,Vassilev, Nikolay
experimental part, p. 5856 - 5861 (2011/01/03)
Some novel thieno[2,3-d]pyrimidin-4(3H)-ones containing benzimidazol-2-yl-thioethyl- and benzimidazol-2-yl-methanethioethyl moiety in second position of the pyrimidine ring were synthesized in order to determine their antitrichinellosis and antiprotozoal effects. The structures of the compounds were confirmed by IR, 1H NMR and elemental analysis. The antiparasitic screening showed that the benzimidazole derivatives of thieno[2,3-d]pyrimidin-4(3H)-ones exhibited higher activity against Trichinella spiralis in vitro in comparison albendazole. The most active compound, 2-[2-(5-nitro-1H-benzimidazol-1-yl)ethyl]-5,6,7,8-tetrahydro[1]benzothieno[2, 3-d]pyrimidin-4(3H)-one 22 revealed 95% activity at a dosage of 5 mg/kg mw after 24 h, while compounds 8 and 10 applied at the same dose showed efficacy of 90% after 48 h. The compound 2-{2-[(5(6)-nitro-1H-benzimidazol-2-yl)thio]ethyl}-5,6, 7,8-tetrahydro[1]-benzothieno[2,3-d]pyrimidin-4(3H)-one 11 exhibited 90% efficacy after 24 h. The pharmaco-therapeutic study in vivo on invaded with Lamblia muris white mice showed 100% effectiveness of the compounds 8, 10, 11, 13-15 and 22, 23 after five-days-treatment course.
Synthesis and antitrichinellosis activity of some bis(benzimidazol-2-yl)amines
Mavrova, Anelia Ts.,Denkova, Pavletta,Tsenov, Yordan A.,Anichina, Kameliya K.,Vutchev, Dimitar I.
, p. 6291 - 6297 (2008/04/05)
Novel bis(benzimidazol-2-yl)amines were synthesized using two methods and studied for antitrichinellosis activity. DFT calculations were performed in order to determine the geometry of molecules. All derivatives of 2-aminobenzimidazole exhibited higher activity in vitro against Trichinella spiralis larvae in regard to the activity of albendazole, moreover compounds 4f-i manifested antitrichinellosis effect, which surpassed five times the activity of albendazole. The in vivo screening of intestinal phase of the T. spiralis revealed 100% effectiveness of compounds 4g-i at oral dosages of 50 and 100 mg/kg mw, while albendazole possesses 100% efficacy only at a dose of 100 mg/kg mw.
Synthesis of N-substituted benzimidazole-2-thiones
Doerge,Cooray
, p. 1789 - 1795 (2007/10/02)
General methods were developed for N-substitution of benzimidazoline-2-thione with alkyl, alkenyl, alkynyl and acyl groups using S-tritylation as a protecting reaction.
A Facile One Pot Synthesis of 1-Alkylbenzimidazoline-2-thiones
Lee, Tae Ryong,Kim, Kyongtae
, p. 747 - 751 (2007/10/02)
Reactions of benzimidazoline-2-thione with alkyl halides in the presence of sodium naphthalenide in tetrahydrofuran at room temperature under a nitrogen atmosphere afforded 1-alkyl-2-alkylthiobenzimidazoles in excellent yields, which underwent a bond cleavage between S and C of alkyl group to give excellent yields of 1-alkylbenzimidazoline-2-thiones by the treatment with an additional amount of sodium naphthalenide.
CONDENSED DERIVATIVES OF BENZAZOLES. 1. SYNTHESIS OF 6- AND 5-SUBSTITUTED BENZIMIDAZOQUINAZOLIN-12-ONES
Popov, I. I.,Boroshko, S. L.,Tertov, B. A.,Makarov, S. P.,Simonov, A. M.,Simkin, B. Ya.
, p. 1348 - 1352 (2007/10/02)
6(5)H-Benzimidazoquinazolin-12-one was obtained in high yield by condensation of benzimidazole-2-sulfonic acid with anthranilic acid.Methods for the introduction of substituents selectively into the 5 and 6 positions of this heterocycle were develo
