78650-01-8Relevant academic research and scientific papers
Synthesis of novel fused pyrimidines and imidazoles as potential analgesics from 2-amino-4-substituted-striazino[1,2-a]-benzimidazoles
El-Feky, Said A.,Thabet, Hamdy Kh.,Mudawi, Mahmoud M. E.
, p. 709 - 718 (2015/10/28)
The synthesis of novel fused pyrimidines and imidazole derivatives from 2-amino-s-triazino[1,2-a]benzimidazoles 2a-e and 3a-c was successfully carried out by a ring annelation reaction in a very good yield. Compound 3c was screened for analgesic activity against acetic acid irritation and has shown protection equal to the reference drug (diclofenac sodium). The acute toxicity study revealed that compound 3c is safe up to 300 mg/kg and there is no sign and symptoms of toxicity and mortality for 72 hours.
Synthesis of 2-amino-s-triazino[1,2-a]benzimidazoles as potential antifolates from 2-guanidino- and 2-guanidino-5-methylbenzimidazoles
Dolzhenko, Anton V.,Chui, Wai-Keung
, p. 95 - 100 (2007/10/03)
The syntheses of 2-amino-s-triazino[1,2-a]benzimidazoles from 2-guanidinobenzimidazoles were successfully carried out by a ring annelation reaction. The regiochemistry of the ring closure of 5-methyl-2- guanidinobenzimidazole with diethyl azodicarboxylate, aldehydes, acetone, diethyl ethoxymethylene-malonate and orthoesters, leading to the formation of s-triazine ring was studied. High regioselectivity was not observed in any of these reactions. However, the synthesis of s-triazino[1,2-a]benzimidazole system was found to be more regioselective than its 3,4-dihydro analogue. NOESY experiment indicated that the compound, 2-amino-4,4-dimethyl-3,4-dihydro-s- triazino[1,2-a]benzimidazole existed predominantly as the 3,4-dihydro tautomer in dimethyl sulfoxide. It was found to inhibit bovine dihydrofolate reductase with IC50 10.9 μM.
