Search results for "benzimidazole"
showing 10 items of 161 documents
CCDC 191616: Experimental Crystal Structure Determination
2003
Related Article: J.R.Galan-Mascaros, K.R.Dunbar|2003|Angew.Chem.,Int.Ed.|42|2289|doi:10.1002/anie.200250152
Hydrogels for potential colon drug release by thiol-ene conjugate addition of a new inulin derivative.
2008
Inulin was chosen as a starting polymer for biocompatible, pH-sensitive and biodegradable hydrogels. Three INUDVSA-TT hydrogels were obtained by crosslinking inulin derivatives with trimethylolpropane tris(3-mercaptopropionate) under varying conditions. The resulting hydrogels were cell compatible, as demonstrated by MTS and trypan blue exclusion assays acting on Caco-2 cells, and were biodegraded by inulinase and esterase, thus suggesting their use as colonic drug delivery systems. 2-Methoxyestradiol, an anti-cancer drug, was soaked in INUDVSA-TT hydrogels and its in vitro release and apoptotic effect on Caco-2 cells were evaluated.
Randomized trial of a single, double and triple dose of 10 mg/kg of a human formulation of triclabendazole in patients with fascioliasis.
2004
1. A study performed > 10 years ago and case reports published recently suggest that triclabendazole is effective for the treatment of patients with fascioliasis. 2. To confirm the efficacy of a human formulation of triclabendazole, we enrolled 165 patients into the present study and divided the subjects into two groups: (i) those who had fascioliasis, as evidenced by the presence of ova in their stools; and (ii) patients with clinical and laboratory data suggesting fascioliasis. 3. Patients were randomly allocated to receive 10 mg/kg, p.o., triclabendazole for 1, 2 or 3 days (single-, double- and triple-dose groups, respectively). Medical history and physical and laboratory examinations we…
CCDC 2095301: Experimental Crystal Structure Determination
2022
Related Article: Javier López-Cabrelles, Eugenia Miguel-Casañ, María Esteve-Rochina, Eduardo Andres-Garcia, Iñigo J. Vitórica-Yrezábal, Joaquín Calbo, Guillermo Mínguez Espallargas|2022|Chemical Science|13|842|doi:10.1039/D1SC04779E
Benzimidazoles as NMDA Glycine-Site Antagonists: Study on the Structural Requirements in 2-Position of the Ligand
2000
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 microM (9 b) and 38.0 microM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazole-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen …
ChemInform Abstract: Benzimidazoles as NMDA Glycine-Site Antagonists: Study on the Structural Requirements in 2-Position of the Ligand.
2010
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 microM (9 b) and 38.0 microM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazole-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen …
Struktur-Wirkungsbeziehungen bei Histaminanaloga, 14. Mitt. 4-Aminomethyl-benzimidazole und 9-Amino-naphth[1,2-d]imidazole
1977
Es wird die Darstellung der bicyclischen Histaminanaloga 4-Aminomethyl-benzimidazol (3a) und 4-Aminomethyl-4,5,6,7-tetrahydro-benzimidazol (3b) sowie der tricyclischen Analoga 9-Amino-6,7,8,9-tetrahydro-naphth[1,2-d]imidazol (6b) und 9-Amino-4,5,5a,6,7,8,9,9a-octahydro-naphth[1,2-d]imidazol (6c) beschrieben. 4-(Aminomethyl)benzimidazoles and 9-Aminonaphth[1,2-d]imidazoles Syntheses of the bicyclic histamine analogues 4-(aminomethyl)benzimidazole (3a) and 4-aminomethyl-4,5,6,7-tetrahydrobenzimidazole (3b) and of the tricyclic analogues 9-amino-6,7,8,9-tetrahydronaphth[1,2-d]imidazole (6b) and 9-amino-4,5,5a,6,7,8,9,9a-octahydronaphth[1,2-d]-imidazole (6c) are described.
The triplet excited state of the biocative compound thiabendazole. Characterization and suitability as reporter for cyclodextrin complexation
2012
Fluorescence spectroscopy, laser flash photolysis (LPF), and density functional theory calculations have been performed to characterize the photobehavior of thiabendazole (1). Direct LFP of 1 results in the generation of a transient absorbing at λmax = 570 nm identified as the triplet excited state (31∗). The intersystem crossing quantum yield is 0.91, and the triplet energy is 288 kJ mol−1. The singlet–triplet energy gap is 84 kJ mol−1. The behavior of thiabendazole within CDs results in a marked enhancement of the triplet lifetime, this change is attributed to the mobility restrictions of included 1 imposed by the cyclodextrin cavities.
Synthesis of polycyclic fused benzimidazole derivatives
1977
Am easy method for the synthesis of tetraeyclie systems containing an imidazole and an iso-thiazole or an imidazole and a thiazine ring, by reacting 2H-1,3-benzothiazine-2-thion-4(3H)one with aromatic primary diarnines is reported. The structures were assigned based upon mass spectra and modes of cleavage of the compounds. The most important fragments are described.
Herbizide, 2. Mitt. 2-Trifluormethylpyrimido[1,2-a]benzimidazole
1982
Aus der Kondensation von 2-Aminobenzimidazol (1) mit den Trifluormethyl-β-Diketonen 2a-f gehen die 2-Trifluormethylpyrimido[1,2-a]benzimidazole 3a-f hervor. Auffallende herbizide Wirksamkeit vermag 3a zu entfalten. Herbicides, II: 2-(Trifluoromethyl)pyrimido[1,2-a]benzimidazoles The condensation of 2-aminobenzimidazole (1) with the trifluoromethyl-β-diketones 2a-f furnishes the 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazoles 3a-f. Marked herbicidal activity is exhibited by 3a.