55737-29-6Relevant academic research and scientific papers
Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives
Bhavsar, Zeel A.,Acharya, Prachi T.,Jethava, Divya J.,Patel, Dhaval B.,Vasava, Mahesh S.,Rajani, Dhanji P.,Pithawala, Edwin,Patel, Hitesh D.
, p. 4215 - 4238 (2020)
Some derivatives of 2-substituted benzimidazole were prepared via coupling of N-methyl-o-phenylenediamine or o-phenylenediamine with different aromatic aldehydes catalyzed by Ni(OAc)2 in the presence of chloroform under microwave-assisted condi
A fluorobenzene imidazole impurity E preparation method
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Paragraph 0060; 0065; 0066, (2019/04/10)
The invention discloses a fluorobenzene imidazole impurity E preparation method. Characterized in that in order to para-benzoic acid as the starting material, after chlorination reaction, esterification reaction, a Friedel-crafts acylation reaction, hydro
Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro
Ríos Martínez, Carlos H.,Nué Martínez, J. Jonathan,Ebiloma, Godwin U.,De Koning, Harry P.,Alkorta, Ibon,Dardonville, Christophe
, p. 806 - 817 (2015/08/06)
Diphenyl-based bis(2-iminoimidazolidines) are promising antiprotozoal agents that are curative in mouse models of stage 1 trypanosomiasis but devoid of activity in the late-stage disease, possibly due to poor brain penetration caused by their dicationic nature. We present here a strategy consisting in reducing the pKa of the basic 2-iminoimidazolidine groups though the introduction of chlorophenyl, fluorophenyl and pyridyl ring in the structure of the trypanocidal lead 4-(imidazolidin-2-ylideneamino)-N-(4-(imidazolidin-2-ylideneamino)phenyl)benzamide (1). The new compounds showed reduced pKa values (in the range 1-3 pKa units) for the imidazolidine group linked to the substituted phenyl ring. In vitro activities (EC50) against wild type and resistant strains of T. b. brucei (s427 and B48, respectively) were in the submicromolar range with four compounds being more active and selective than 1 (SI > 340). In particular, the two most potent compounds (3b and 5a) acted approximately 6-times faster than 1 to kill trypanosomes in vitro. No cross-resistance with the diamidine and melaminophenyl class of trypanocides was observed indicating that these compounds represent interesting leads for further in vivo studies.
PYRAZOLE COMPOUNDS AND THIAZOLE COMPOUNDS AS PROTEIN KINASES INHIBITORS
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Paragraph 0046; 0047, (2013/03/26)
A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.
Novel approach to synthesis of substituted 3-aminoquinolines from nitroarenes and protected ethyl aminocrotonate
Bujok, Robert,Kwast, Andrzej,Cmoch, Piotr,Wróbel, Zbigniew
experimental part, p. 698 - 708 (2010/09/05)
The addition of mono- and dianions of ethyl N-pivaloyl-3-aminocrotonate to substituted nitroarenes, followed by action of silylating or acylating agent, leads to 3-aminoquinoline carboxylic acid derivatives. Hydrolysis and decarboxylation of the latter, carried out efficiently under relatively mild conditions, afford 3-aminoquinolines diversely substituted in the benzo-fused ring.
NOVEL COMPOUNDS
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Page/Page column 112, (2008/06/13)
There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
Optimization of novel combi-molecules: Identification of balanced and mixed bcr-abl/DNA targeting properties
Rachid, Zakaria,Katsoulas, Athanasia,Williams, Christopher,Larroque, Anne-Laure,McNamee, James,Jean-Claude, Bertrand J.
, p. 4248 - 4253 (2008/02/09)
Steps toward the identification of combi-molecules with strong abl tyrosine kinase (TK) inhibitory property and significant DNA damaging potential are described. The optimized combi-molecule 13a was shown to induce approximately twofold stronger abl TK in
Synthesis and antiparasitic activity of Albendazole and Mebendazole analogues
Navarrete-Vazquez, Gabriel,Yepez, Lilian,Hernandez-Campos, Alicia,Tapia, Amparo,Hernandez-Luis, Francisco,Cedillo, Roberto,Gonzalez, Jose,Martinez-Fernandez, Antonio,Martinez-Grueiro, Mercedes,Castillo, Rafael
, p. 4615 - 4622 (2007/10/03)
Albendazole (Abz) and Mebendazole (Mbz) analogues have been synthesized and in vitro tested against the protozoa Giardia lamblia, Trichomonas vaginalis and the helminths Trichinella spiralis and Caenorhabditis elegans. Results indicate that compounds 4a, 4b (Abz analogues), 12b and 20 (Mbz analogues) are as active as antiprotozoal agents as Metronidazole against G. lamblia. Compound 9 was 58 times more active than Abz against T. vaginalis. Compounds 8 and 4a also shown high activity against this protozoan. Compounds 4b and 5a were as active as Abz. None of the Mbz analogues showed activity against T. vaginalis. The anthelmintic activity presented by these compounds was poor.
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5- tetrahydro-1H-1-benzazepine (OPC-41061): A potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist
Kondo, Kazumi,Ogawa, Hidenori,Yamashita, Hiroshi,Miyamoto, Hisashi,Tanaka, Michinori,Nakaya, Kenji,Kitano, Kazuyoshi,Yamamura, Yoshitaka,Nakamura, Shigeki,Onogawa, Toshiyuki,Mori, Toyoki,Tominaga, Michiaki
, p. 1743 - 1754 (2007/10/03)
We previously reported a series of benzazepine derivatives as orally active nonpeptide arginine vasopressin (AVP) V2 receptor antagonists. After the lead structure OPC-31260 was structurally evaluated and optimized, the introduction of the 7-Cl moiety on the benzazepine and 2-CH3 on the aminobenzoyl moiety enhanced its oral activity. The new AVP-V2 selective antagonist OPC-41061 was determined to be a potent and orally active agent. Copyright (C) 1999 Elsevier Science Ltd.
