Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Abstract

Synthesis and bioactivity of novel dual acting nitric oxide releasing and reactive oxygen scavenging hybrid compound SA-2 is described. The hybrid molecule SA-2 significantly increased the superoxide dismutase enzyme level and protected the photoreceptor cells from H2O2 induced oxidative stress. Synthesis of ocular esterase sensitive aceloxy alkyl carbamate prodrug SA-4 with improved aqueous half-life is achieved to aid topical ocular formulation. This class of hybrid molecule and prodrug may have dual potential of improved IOP lowering and neuroprotection in glaucomatous optic neuropathy.

Original languageEnglish
Pages (from-to)1490-1494
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number5
DOIs
StatePublished - 1 Mar 2016

Fingerprint

Optic Nerve Diseases
Prodrugs
Optics
Photoreceptor Cells
Molecules
Oxidative stress
Carbamates
Scavenging
Esterases
Bioactivity
Superoxide Dismutase
Half-Life
Nitric Oxide
Oxidative Stress
Oxygen
Enzymes
Neuroprotection

Keywords

  • Aceloxy acyl carbamate prodrug
  • Catalytic anti-oxidant
  • Glaucoma
  • Nitric oxide
  • Optic neuropathy
  • SOD mimetic
  • Sydnonimine
  • TEMPOL

Cite this

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title = "Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy",
abstract = "Synthesis and bioactivity of novel dual acting nitric oxide releasing and reactive oxygen scavenging hybrid compound SA-2 is described. The hybrid molecule SA-2 significantly increased the superoxide dismutase enzyme level and protected the photoreceptor cells from H2O2 induced oxidative stress. Synthesis of ocular esterase sensitive aceloxy alkyl carbamate prodrug SA-4 with improved aqueous half-life is achieved to aid topical ocular formulation. This class of hybrid molecule and prodrug may have dual potential of improved IOP lowering and neuroprotection in glaucomatous optic neuropathy.",
keywords = "Aceloxy acyl carbamate prodrug, Catalytic anti-oxidant, Glaucoma, Nitric oxide, Optic neuropathy, SOD mimetic, Sydnonimine, TEMPOL",
author = "Suchismita Acharya and Preston Rogers and Raghu Krishnamoorthy and Stankowska, {Dorota Luiza} and Dias, {H. V.Rasika} and Thomas Yorio",
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Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy. / Acharya, Suchismita; Rogers, Preston; Krishnamoorthy, Raghu; Stankowska, Dorota Luiza; Dias, H. V.Rasika; Yorio, Thomas.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 26, No. 5, 01.03.2016, p. 1490-1494.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy

AU - Acharya, Suchismita

AU - Rogers, Preston

AU - Krishnamoorthy, Raghu

AU - Stankowska, Dorota Luiza

AU - Dias, H. V.Rasika

AU - Yorio, Thomas

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AB - Synthesis and bioactivity of novel dual acting nitric oxide releasing and reactive oxygen scavenging hybrid compound SA-2 is described. The hybrid molecule SA-2 significantly increased the superoxide dismutase enzyme level and protected the photoreceptor cells from H2O2 induced oxidative stress. Synthesis of ocular esterase sensitive aceloxy alkyl carbamate prodrug SA-4 with improved aqueous half-life is achieved to aid topical ocular formulation. This class of hybrid molecule and prodrug may have dual potential of improved IOP lowering and neuroprotection in glaucomatous optic neuropathy.

KW - Aceloxy acyl carbamate prodrug

KW - Catalytic anti-oxidant

KW - Glaucoma

KW - Nitric oxide

KW - Optic neuropathy

KW - SOD mimetic

KW - Sydnonimine

KW - TEMPOL

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