Synthesis, Anti-inflammatory, and Neuroprotective Activity of N-Substituted Phthalimide Derivatives

Bhat, M. A.King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia. (författare)

A new series of N-substituted phthalimide compounds was synthesized in good yield. All the compounds were characterized by spectroscopic data and were evaluated for their inhibitory activity against the expression of cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) and pro-inflammatory proteins in the bacterial lipopolysaccharide (LPS)-induced murine macrophage (RAW 264.7) cells. All the compounds significantly (p <0.05) downregulated the LPS-stimulated COX-2 and iNOS expression from 100% to the ranges of 61.9±5.1–84.5±4.1% and 41.1±5.4–85.3±1.9%) at 10 µM, respectively. Among others, 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(3,4-dichlorophenyl)methylidene]benzohydrazide displayed the most potent inhibition to the level of (41.1±5.4%) iNOS expression, about half of the potency of dexamethasone (23.0±3.3%). Moreover, the neuroprotective activity of the compounds was assessed against the 6-hydroxydopamine (6-OHDA)-challenged neuroblastoma SH-ST5Y cells, and all compounds exhibited significant (p <0.05) protection with variable potencies. 4-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(3,4-dihydroxyphenyl)methylidene]benzohydrazide was found to display more than 70% relative neuroprotection against 6-OHDA-induced cell death with the additional advantage of keeping the highest cell viability index (83.3±4.5%) to the cells.

Ahmed, A. F.King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia. (författare)
Wen, Z.-H.Natl Sun Yat Sen Univ, Dept Marine Biotechnol & Resources, Kaohsiung 80424, Taiwan. (författare)
El-Seedi, Hesham R.Uppsala universitet,Farmakognosi(Swepub:uu)heels173 (författare)
Naglah, A. M.King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia. (författare)
Al-Omar, M. A.King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia. (författare)
King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia.King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia. (creator_code:org_t)

Ingår i:Russian journal of general chemistry: Pleiades Publishing Ltd93:11, s. 2935-29401070-36321608-3350

Av författaren/redakt...: Bhat, M. A.; Ahmed, A. F.; Wen, Z.-H.; El-Seedi, Hesham ...; Naglah, A. M.; Al-Omar, M. A.

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