Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents.
With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound6bshowed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt. emy28_s@hotmail.com.
Eman S
ES
Nossier
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza 12622, Egypt. hh_fahmy@yahoo.com.
Hoda H
HH
Fahmy
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza 12622, Egypt. nagykhalifa@hotmail.com.|Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. nagykhalifa@hotmail.com.
Nagy M
NM
Khalifa
Pharmacology Department, National Research Centre, Dokki, Cairo 12622, Egypt. wafaa_nrc@yahoo.com.
Wafaa I
WI
El-Eraky
Pharmacology Department, National Research Centre, Dokki, Cairo 12622, Egypt. dr.marawan@gmail.com.
Marawan A
MA
Baset
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002351:Carrageenan; D000068579:Celecoxib / Q000737:chemistry / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D007267:Injections; D008297:Male; D062105:Molecular Docking Simulation; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D000077285:Rimonabant
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D006571:Heterocyclic Compounds; D010880:Piperidines; D011720:Pyrazoles; C031280:pyrazole; D002351:Carrageenan; D000068579:Celecoxib; D000077285:Rimonabant
1,3-diaryl pyrazole derivatives; anti-inflammatory activity; synthesis