Anti-inflammatory and analgesic activities of newly synthesized chiral peptide derivatives using (3-benzoyl- 4,5-dioxo-2-phenyl-pyrrolidin-1-yl)acetic acid ethyl ester as starting material.
A series of heterocyclic derivatives was synthesized using (3-benzoyl-4,5-dioxo-2-phenyl-pyrrolidin-1-yl)acetic acid ethyl ester 1 as starting material. Treatment of 1 with 1 N NaOH or hydrazine hydrate afford the corresponding acid 2 and acid hydrazides 4 and 5, which were reacted with several reagents to produce some new peptido hetero-organic derivatives 6-12. The pharmacological screening showed that many of these newly synthesized compounds have good anti-inflammatory and analgesic activities comparable to diclofenac potassium and valdecoxib as reference drugs.
Fakhr
Issa M
IM
Applied Organic Chemistry Department, National Research Center, Dokki, Cairo, Egypt.
Amr
Abdel-Galil E
AG
Sabry
Nermien M
NM
Abdalah
Mohamed M
MM
D000700:Analgesics / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D004008:Diclofenac / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D007555:Isoxazoles / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D011759:Pyrrolidines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology; D023382:Toxicity Tests, Acute; D000096926:Benzenesulfonamides
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D004008:Diclofenac; D007555:Isoxazoles; D011759:Pyrrolidines; D013449:Sulfonamides; C529261:(3-benzoyl-4,5-dioxo-2-phenyl-pyrrolidin-1-yl)acetic acid ethyl ester; C406224:valdecoxib; D000096926:Benzenesulfonamides