102632-04-2Relevant academic research and scientific papers
Topical Nonsteroidal Antipsoriatic Agents. 1. 1,2,3,4-Tetraoxygenated Naphthalene Derivatives
Jones, Gordon H.,Venuti, Michael C.,Young, John M.,Murthy, D.V. Krishna,Loe, Brad E.,et al.
, p. 1504 - 1511 (1986)
On the basis of previous observations that both 2,3-dihydro-2,2,3,3-tetrahydroxy-1,4-naphthoquinone (oxoline, 1) and 6-chloroisonaphthazarin (2) had demonstrated antipsoriatic activity in vivo, a series of structural derivatives of 2 were prepared and examined in the Scholtz-Dumas topical psoriasis bioassay.Of these six (5, 6, 9a, 10, 11a, 11b), the most effective compound was found to be 6-chloro-1,4-diacetoxy-2,3-dimethoxynaphthalene (RS-43179,lonapalene, 11a).An extensive series of 1,2,3,4-tetraoxygenated naphthalenes (16-74) incorporating variations of the ester, eth er and aryl substituents were prepared as analogues of 11a to examine the structural requirements for activity and were screened in vivo as inhibitors of arachidonic acid induced mouse ear edema, a topical bioassay capable of detecting 5-lipoxygenase inhibitors.Net lipophilicity, hydrolytic stability, and ring substitution play significant roles in determining the observed in vivo activity.Lonapalene (11a) is currently in clinical development as a topical applied nonsteroidal antipsoriatic agent.
Naphthalene anti-psoriatic agents
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, (2008/06/13)
Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: STR1 wherein: R1 and R2 are the same and are lower alkoxy or optionally substituted phenoxy, R3 is lower alkyl, lower alkoxy, or halo
Naphthalene anti-psoriatic agents
-
, (2008/06/13)
Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: STR1 wherein: R1 and R2 are the same and are lower alkoxy, lower alkylthio, optionally substituted phenoxy or optionally substituted phenylthio,
Naphthoquinone anti-psoriatic agents
-
, (2008/06/13)
Psoriasis in mammals is relieved by topically administering naphthoquinones of the formula: STR1 wherein: R1 and R2 are lower alkoxy; and R3 is halo or cyano.
Naphthalene anti-psoriatic agents
-
, (2008/06/13)
Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: STR1 wherein: R1 and R2 are lower alkoxy or lower alkylthio; R3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl
