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Molecular Modeling, Synthesis, and Antihyperglycemic Activity of the New Benzimidazole Derivatives - Imidazoline Receptor Agonists.
Martynov, Artur; Farber, Boris; Bomko, Tatyana; Beckles, Daniel L; Kleyn, Ilya.
Afiliación
  • Martynov A; Laboratory and Clinical department of Molecular Immunopharmacology, SI " I. Mechnikov Institute of Microbiology and Immunology of National Academy of Medical Sciences of Ukraine, Kharkiv, Ukraine.
  • Farber B; R&D Department, Noigel LLC, New York, NY, USA.
  • Bomko T; Laboratory and Clinical department of Molecular Immunopharmacology, SI " I. Mechnikov Institute of Microbiology and Immunology of National Academy of Medical Sciences of Ukraine, Kharkiv, Ukraine.
  • Beckles DL; Baylor Scott & White Health, Round Rock, TX, USA.
  • Kleyn I; SUNY Downstate Medical Center / University Hospital of Brooklyn, New York, NY, USA.
Drug Des Devel Ther ; 18: 1035-1052, 2024.
Article en En | MEDLINE | ID: mdl-38585255
ABSTRACT

Introduction:

The paper presents the results of a study on the first synthesized benzimidazole derivatives obtained from labile nature carboxylic acids. The synthesis conditions of these substances were studied, their structure was proved, and some components were found to have sugar-reducing activity on the model of alloxan diabetes in rats.

Methods:

The study used molecular modeling methods such as docking based on the evolutionary model (igemdock), RP_HPLC method to monitor the synthesis reaction, and 1H NMR and 13C NMR, and other methods of organic chemistry to confirm the structures of synthesized substances. Results &

Discussion:

The docking showed that the ursodeoxycholic acid benzimidazole derivatives have high tropics to all imidazoline receptor carriers (PDB ID 2XCG, 2bk3, 3p0c, 1QH4). The ursodeoxycholic acid benzimidazole derivative and arginine and histidine benzimidazole derivatives showed the highest sugar-lowering activity in the experiment on alloxan-diabetic rats. For these derivatives, the difference in glucose levels of treated rats was significant against untreated control. Therefore, the new derivatives of benzimidazole and labile natural organic acids can be used to create new classes of imidazoline receptor inhibitors for the treatment of diabetes mellitus and hypertension.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diabetes Mellitus Experimental / Hipoglucemiantes Límite: Animals Idioma: En Revista: Drug Des Devel Ther Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2024 Tipo del documento: Article País de afiliación: Ucrania Pais de publicación: Nueva Zelanda
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diabetes Mellitus Experimental / Hipoglucemiantes Límite: Animals Idioma: En Revista: Drug Des Devel Ther Asunto de la revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Año: 2024 Tipo del documento: Article País de afiliación: Ucrania Pais de publicación: Nueva Zelanda