Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives.
A series of diazipine, pyrimidine, fused triazolopyrimidine and imide derivatives were newly synthesized using 4-phenyl-but-3-en-2-one 1 as a starting material and compounds 2 and 9 are intermediates. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds were interestingly less toxic than the reference drug. The pharmacological screening showed that many of these obtained compounds have good analgesic, anticonvulsant and anti-inflammatory activities comparable to Valdecoxib, Carbamazepine and Predensilone as reference drugs. Regarding the protection against Carrageenan induced edema, five compounds were found more potent than Prednisolone. On the other hand, in searching for COX-2 inhibitor, the inhibition of plasma PGE2 for the compounds were determined and four compounds were found more potent than Prednisolone. The detailed synthesis, spectroscopic data, pharmacological screening and acute toxicity LD(50) for the synthesized compounds were reported.
Said
Said A
SA
Department of Chemistry, Faculty of Science, Zagazige University, Zagazige, Egypt.
Amr
Abd el-Galil E
Ael-G
Sabry
Nermien M
NM
Abdalla
Mohamed M
MM
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001391:Azo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D015195:Drug Design; D005260:Female; D007094:Imides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D007555:Isoxazoles / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D011241:Prednisone / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013449:Sulfonamides / Q000494:pharmacology; D000096926:Benzenesulfonamides
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000927:Anticonvulsants; D001391:Azo Compounds; D007094:Imides; D007555:Isoxazoles; D011241:Prednisone; D011743:Pyrimidines; D013449:Sulfonamides; C406224:valdecoxib; D000096926:Benzenesulfonamides