Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives.
A group of 3,5-diaryl-2-pyrazoline derivatives were prepared via the reaction of various chalcones with hydrazine hydrate in ethanol. A group of NO-donating-2-pyrazoline derivatives were synthesized by carrying a nitrate ester group or an oxime group onto the prepared pyrazoline derivatives through different spacers. The prepared compounds were evaluated for their anti-inflammatory activity using carrageenan-induced rat paw edema and compared to a well-known NSAID, indomethacin as a reference drug. The ability of the prepared compounds to induce gastric toxicity was also evaluated. Most of the prepared compounds showed significant anti-inflammatory activity at the injected dose (100mg/kg) but they were safer than indomethacin in regard to gastric toxicity. The incorporation of the NO-donating group into the parent pyrazoline derivatives caused a non-significant reduction in the anti-inflammatory activity while a marked decrease in gastric ulcerations induced by their parent pyrazolines was observed.
Shoman
Mai E
ME
Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.
Abdel-Aziz
Mohamed
M
Aly
Omar M
OM
Farag
Hassan H
HH
Morsy
Mohamed A
MA
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000009:adverse effects* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004487:Edema / Q000188:drug therapy; D007213:Indomethacin / Q000009:adverse effects / Q000494:pharmacology; D008297:Male; D009569:Nitric Oxide / Q000737:chemistry*; D011720:Pyrazoles / Q000009:adverse effects* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D012015:Reference Standards; D013276:Stomach Ulcer / Q000139:chemically induced*
D000893:Anti-Inflammatory Agents; D011720:Pyrazoles; D009569:Nitric Oxide; C031280:pyrazole; D007213:Indomethacin