Synthesis and In-Vivo Evaluation of Benzoxazole Derivatives as Promising Anti-Psoriatic Drugs for Clinical Use

Rami Ayoub, Jamal Jilani, Qais Jarrar, Raad Alani, Chrismawan Ardianto, Khang Wen Goh, Dalia Ali, Said Moshawih

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

2-(4-Chlorophenyl)-5-benzoxazoleacetic acid (CBA) and its ester, methyl-2-(4-chloro-phenyl)-5-benzoxazoleacetate (MCBA), were synthesized, and their structures were confirmed by 1 HNMR, IR, and mass spectrophotometry. The anti-psoriatic activities of CBA and MCBA were tested using an imiquimod (IMQ)-induced psoriatic mouse model, in which mice were treated both topically (1% w/w) and orally (125 mg/kg) for 14 days. The erythema intensity, thickness, and desquamation of psoriasis were scored by calculating the psoriasis area severity index (PASI). The study also included the determination of histopathological alterations in the skin tissues of treated mice. Topical and oral administration of CBA and MCBA led to a reduction in erythema intensity, thickness, and desquamation, which was demonstrated by a significant decrease in the PASI val-ue. In addition, skin tissues of mice treated with CBA and MCBA showed less evidence of psoriat-ic alterations, such as hyperkeratosis, parakeratosis, scale crust, edema, psoriasiform, and hyper-plasia. After administration of either topical or oral dosing, the anti-psoriatic effects were found to be stronger in MCBA-treated than in CBA-treated mice. These effects were comparable to those produced by Clobetasol propionate, the reference drug. This drug discovery could be translated into a potential new drug for future clinical use in psoriasis treatment.

Original languageEnglish
Article number3023
JournalMolecules
Volume27
Issue number9
DOIs
Publication statusPublished - 1 May 2022

Keywords

  • arylbenzoxazole
  • imiquimod
  • in vivo
  • prodrug
  • psoriasis
  • synthesis

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