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11(R),12(S),15(S)-trihydroxyeicosa-5(Z),8(Z),13(E)-trienoic acid: an endothelium-derived 15-lipoxygenase metabolite that relaxes rabbit aorta.
It is suggested that 11(R),12(S),15(S)-trihydroxyeicosa-5(Z),8-Z),13(E)-trienoic acid is the active stereoisomer produced by the rabbit aorta that relaxes smooth muscle by activating K+ channels. Expand
3-Oxa-15-cyclohexyl prostaglandin DP receptor agonists as topical antiglaucoma agents.
A series of prostaglandin DP agonists containing a 3-oxa-15-cyclohexyl motif was synthesized and evaluated in several in vitro and in vivo biological assays, finding that selected amide prodrugs of the carboxylic acid enhance in vivo potency, presumably by increasing bioavailability. Expand
Identification of PDE6D as a molecular target of anecortave acetate via a methotrexate-anchored yeast three-hybrid screen.
The identification of PDE6D as the molecular binding partner of AA provides insight into the role of this drug candidate in treating glaucoma. Expand
Enantioselective Synthesis of Brinzolamide (AL-4862), a New Topical Carbonic Anhydrase Inhibitor. The “DCAT Route” to Thiophenesulfonamides
A large scale synthesis of the topical carbonic anhydrase inhibitors AL-4623A (13a·HCl) and AL-4862 (13b) from 3-acetyl-2,5-dichlorothiophene (“DCAT”, 1) is described. Reaction of 1 with NaSBn gaveExpand
AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey.
Topical ocular dosing of AL-12182, the isopropyl ester prodrug of the potent agonist 13, lowered intraocular pressure in the monkey by 40% accompanied by minimal conjunctival hyperemia in the rabbit. Expand
Synthesis of the 16alpha,17alpha,21-Trimethyl Corticosteroid Rimexolone from Prednisolone.
  • R. Conrow
  • Chemistry, Medicine
  • The Journal of organic chemistry
  • 6 January 1999
Efficient Preparation of Polyfunctional a-Diketones from Carboxylic Acids
Synthese en particulier de l'acide benzyl-3 dioxo-4,5 caproique et de la phenyl-5 pentanedione-2,3
Corticosteroid decomposition via a mixed anhydride.
Oxidation of dexamethasone in an aqueous suspension by air during prolonged storage produces the 17alpha-formyloxy-17beta-carboxylic acid 4. A pathway to 4 is proposed that involvesExpand
Allylic alcohol transposition by ortho ester-initiated carbonate extension. synthesis of the vasodilator 11(R),12(S),15(S)-trihydroxyeicosa- 5(Z),8(Z),13(E)-trienoic acid.
  • R. Conrow
  • Chemistry, Medicine
  • Organic letters
  • 5 May 2006
The title compound 1 was obtained via methyl ester 2, which was synthesized in four steps from an isomeric 11,14,15-triol ester 5 using TMS triflate to initiate intramolecular nucleophilic substitution with allylic transposition. Expand
Manufacture of (5Z,8Z,11Z,13E)(15S)-15-Hydroxyeicosa-5,8,11,13-tetraenoic Acid Sodium Salt for Clinical Trials
A robust synthesis of (5Z,8Z,11Z,13E)(15S)-15-hydroxyeicosa-5,8,11,13-tetraenoic acid (15(S)-HETE) sodium salt was established, utilising a biooxidation process. Treatment of arachidonic acid withExpand