- Method for synthesizing mebendazole by means of methyl cyanocarbamate
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The invention discloses a method for synthesizing mebendazole by means of methyl cyanocarbamate. The method comprises the steps that 3,4-diaminobenzophenone and methyl cyanocarbamate react in acetone and hydrochloric acid to prepare a crude mebendazole, the crude mebendazole forms salt in methyl alcohol-nitric acid to obtain mebendazole nitrate, and finally the mebendazole nitrate is subjected to crystal transformation in methyl alcohol-nitric acid to obtain C crystal type mebendazole. The cheap and easily-obtained 3,4-diaminobenzophenone and methyl cyanocarbamate are adopted as raw materials, a large quantity of waste salts generated in the O-methyl isourea methyl formate synthesis process are avoided, the cyclization time is short and only needs 4-6 h, the production period is remarkably shortened, high-salt wastewater by-products can be treated through simple distillation, and the good industrial prospect is achieved.
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Paragraph 0025-0042; 0051-0056
(2019/10/10)
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- Synthesis of benzimidazoles by Cul-catalyzed three-component reaction of 2-haloaniline, ammonia and aldehyde in water
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An efficient copper-catalyzed three-component reaction of 2-haloaniline, ammonia and aldehyde for the synthesis of benzimidazoles with 1,10-phenanthroline as the ligand has been developed. A variety of substituted benzimidazole derivatives can be obtained in yields up to 95%.
- Ke, Fang,Zhang, Peng,Lin, Chen,Lin, Xiaoyan,Xu, Jianhua,Zhou, Xiangge
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supporting information
p. 8090 - 8094
(2018/11/23)
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- MEBENDAZOLE POLYMORPH FOR TREATMENT AND PREVENTION OF TUMORS
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Mebendazole is an antiparasitic drug with over 40 years of safe use. Recently mebendazole was repurposed for glioblastoma therapy. Three polymorphs of mebendazole exist, but the relative polymorph content for existing drugs varies, and the therapeutic anti-cancer relevance of the different polymorphs was unknown. As an oral drug mebendazole polymorph C is a superior form, and it reaches the brain and brain tumors in effective concentrations. Efficacy is further improved by combining mebendazole with a P-glycoprotein inhibitor. Mebendazole may also be used for therapy of other cancers, as well as a chemo-preventative agent.
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- Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy
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Sodium taurocholate cotransporting polypeptide (NTCP) is a multiple transmembrane transporter predominantly expressed in the liver, functioning as a functional receptor for HBV. Through our continuous efforts to identify NTCP as a novel HBV target, we designed and synthesized a series of new compounds based on the structure of our previous compound NT-5. Molecular docking and MD simulation validated that a new compound named NTI-007 can tightly bind to NTCP, whose efficacy was also measured in vitro virological examination and cytotoxicity studies. Furthermore, autophagy was observed in NTI-007 incubated HepG2.2.15 cells, and results of q-PCR and Western blotting revealed that NTI-007 induced autophagy through NTCP-APOA1-HBx-Beclin1-mediated pathway. Taken together, considering crucial role of NTCP in HBV infection, NTCP-mediated autophagic pathway may provide a promising strategy of HBV therapy and given efficacy of NTI-007 triggering autophagy. Our study suggests pre-clinical potential of this compound as a novel anti-HBV drug candidate.
- Zhang, Jin,Fu, Lei-Lei,Tian, Mao,Liu, Hao-Qiu,Li, Jing-Jing,Li, Yan,He, Jun,Huang, Jian,Ouyang, Liang,Gao, Hui-Yuan,Wang, Jin-Hui
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p. 976 - 984
(2015/03/04)
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- DMSO-mediated ligand dissociation: Renaissance for biological activity of N-heterocyclic-[Ru(η6-arene)Cl2] drug candidates
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Slipped under the radar? 1HNMR spectroscopic examination revealed that [Ru(η6-arene)Cl2(L)] (L=N-heterocyclic ligands) complexes readily undergo a ligand exchange reaction in DMSO (see scheme), a popular medium for preparing stock solutions for biological screening. It is therefore highly important for researchers to study the stability in DMSO before reporting on the biological activity of such complexes. Copyright
- Patra, Malay,Joshi, Tanmaya,Pierroz, Vanessa,Ingram, Katrin,Kaiser, Marcel,Ferrari, Stefano,Spingler, Bernhard,Keiser, Jennifer,Gasser, Gilles
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p. 14768 - 14772
(2013/11/06)
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- 1,5-diphenyl-3-formazancarbonitril parasiticides
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The present invention is directed to the use of 1,5-diaryl-3 -formazancarbonitrile compounds for the control of parasites in vertebrate animals.
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- 1-Alkoxycarbonylbenzimidazole-2-carbamates
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Several benzimidazole-2-carbamates with a substituent at position-5 have been reacted with alkyl chloroformates.The isomers (1) and (2) thus obtained have been separated and their structures established by PMR spectra.In some cases the 1,3-dialkoxycarbonyl-2-benzimidazolones (3) are also obtained.The compounds show high anthelmintic activity.
- Viswanathan, N.,Sidhaye, A. R.
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p. 948 - 951
(2007/10/02)
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- Synthesis and anthelminthic acitivity of alkyl-(5-acyl-1-benzimidazol-2-yl) carbamates
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A series of alkyl-(5-acyl-l-H-benzimidazol-2-yl)-carbamates were prepared and screened for anthelminthic activity. Some of them were found to be fully active at low, atoxic oral dose levels against gastro-intestinal nematodes. The activity against Syphacia muris and Strongyloides ratta is indicated. From these studies methyl (5-benzoyl-1-H-benzimidazol-2-yl) carbamate (mebendazole) and methyl [5-(4-fluorobenzoyl)-1-H-benzimidazol-2-yl]carbamate (flubendazole) were selected for detailed investigation.
- Raeymackers,Van Gelder,Roevens,Janssen
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p. 586 - 594
(2007/10/05)
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