ChemInform Abstract: Substituted cis‐3,3,5‐Trimethylcyclohexyl Thienylglycolates.

Unterhalt, B.; Gores, Peter

doi:10.1002/chin.199016130

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“…3-Substituted [1,2,4]Triazino[4,3-a]benzimidazol-4(10H)ones 1d,k,l and 2d,k (Procedure 2). A solution of 3 or 4 (4 mmol) and the appropriate glyoxylic acid ethyl ester 39,41,42 (4.4 mmol) in 10 mL of absolute ethanol was refluxed for 2-11 h (TLC analysis). After cooling, the precipitate which formed was collected and purified by recrystallization from the appropriate solvent (Table 2, Supporting Information).…”

Section: -Substituted [124]triazino[43-a]benzimidazol-4(10h)ones 1amentioning

confidence: 99%

3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: Tricyclic Heteroaromatic Derivatives as a New Class of Benzodiazepine Receptor Ligands

et al. 1999

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A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the central benzodiazepine receptor (BzR). These compounds were designed as rigid analogues of the previously described N-benzylindolylglyoxylylamide derivatives IV. The title compounds V showed an affinity which depended directly on the presence of the N(10)-H group and an aromatic ring at position 3. Some of them elicited a 2- or 3-fold higher affinity with respect to that of the indolylglyoxylylamide derivatives IV (R = H). The GABA ratio and [(35)S]-tert-butylcyclophosphorothionate binding data revealed an efficacy profile of partial inverse agonists/antagonists for compounds 1c,e,f,j,k, and of a partial agonist for 2c. This last compound proved to be effective in antagonizing pentylenetetrazole-induced seizures in mice. Attempts were made to interpret the structure-affinity relationships of compounds V in the light of possible tautomeric equilibria involving the ligands.

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Section: -Substituted [124]triazino[43-a]benzimidazol-4(10h)ones 1amentioning

confidence: 99%

3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: Tricyclic Heteroaromatic Derivatives as a New Class of Benzodiazepine Receptor Ligands

et al. 1999

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ChemInform Abstract: Substituted cis‐3,3,5‐Trimethylcyclohexyl Thienylglycolates.

Cited by 1 publication

References 1 publication

3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: Tricyclic Heteroaromatic Derivatives as a New Class of Benzodiazepine Receptor Ligands

3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: Tricyclic Heteroaromatic Derivatives as a New Class of Benzodiazepine Receptor Ligands

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