- Synthesis and in vitro cysticidal activity of new benzimidazole derivatives
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Despite albendazole being the drug of choice in neurocysticercosis treatment, its low solubility limits its bioavailability; therefore, more research is required in order to find new molecules with cestocidal activity and adequate aqueous solubility. A set of 13 benzimidazole derivatives were synthesized and their in vitro activities were evaluated against Taenia crassiceps cysts, using albendazole sulfoxide as reference molecule, showing that two of them exhibited good activity. Molecular modelling revealed that the cysticidal efficacy depends on the presence on the molecule of an H in the 1-position, a planar carbamate group at 2-position, and if the substituent in 5-position is voluminous, it should be orthogonal to the benzimidazole ring.
- Palomares-Alonso, Francisca,Jung-Cook, Helgi,Perez-Villanueva, Jaime,Piliado, Juan Carlos,Rodriguez-Morales, Sergio,Palencia-Hernandez, Guadalupe,Lopez-Balbiaux, Nayeli,Hernandez-Campos, Alicia,Castillo, Rafael,Hernandez-Luis, Francisco
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p. 1794 - 1800
(2009/07/18)
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- Synthesis and biological activity of certain alkyl 5(alkoxycarbonyl)-1H- benzimidazole-2-carbamates and related derivatives: A new class of potential antineoplastic and antifilarial agents
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A series of methyl and ethyl 5-(alkoxycarbonyl)-1H-benzimidazole-2- carbamates (7-19) and methyl 5-carbamoyl-1H-benzimidazole-2-carbamates (24- 34) have been synthesized via the reaction of an appropriate alcohol or amine with the acid chloride derivative
- Ram,Wise,Wotring,McCall,Townsend
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p. 539 - 547
(2007/10/02)
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- Studies in Antiparasitic Agents: Part 9 - Synthesis of 5(6)-Alkoxycarbonyl-2-substituted-benzimidazoles as Potential Anthelmintics
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Methyl 5(6)-alkoxycarbonylbenzimidazole-2-carbamates (5a-5f) and 5(6)-carboxyl analogue (5g) and its salts (6a-6b) have been synthesized starting from 4-amino-3-nitrobenzoic acid (2), and their structures established by elemental analysis and spectral data.The drugs 5a-5g and 6a-6b have been tested for their anthelmintic activity in rodents infested by Ancylostoma ceylanicum, Syphacia obvelata, Nippostrongylus brasiliensis, Hymenolepis nana, Cysticercus fasciolaris, Litomosoides carinii and Dipetalonema viteae and found to cause 100percent elimination of A. ceylanicum hookworms at an oral dose of 25-250 mg/kg but not so effective against other helminths.
- Naim, S. Shawkat,Singh, Sudhir K.,Sharma, Satyavan,Gupta, Suman,Fatma, N.,et al.
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p. 1106 - 1109
(2007/10/02)
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