Literature DB >> 8273545

The design and synthesis of second generation leukotriene B4 (LTB4) receptor antagonists related to SC-41930.

T D Penning1, S W Djuric, S H Docter, S S Yu, D Spangler, C P Anglin, D J Fretland, J F Kachur, R H Keith, B S Tsai.   

Abstract

SC-41930, 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4- dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid, is a selective, orally active, LTB4 receptor antagonist currently in clinical trials for psoriasis and ulcerative colitis. Exhaustive SAR studies found a potential backup compound, SC-50605, which was 7-16 times more potent than SC-41930 in LTB4 receptor binding, chemotaxis and degranulation assays. SC-50605 also inhibited LTB4-induced intradermal chemotaxis in cavine skin at an oral dose of 0.10 mg/kg and displayed good activity in animal models of colitis and epidermal inflammation both orally and topically.

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Year:  1993        PMID： 8273545     DOI： 10.1007/bf01972705

Source DB:  PubMed          Journal:  Agents Actions        ISSN： 0065-4299


  8 in total

1.  7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist.

Authors:  S W Djuric; P W Collins; P H Jones; R L Shone; B S Tsai; D J Fretland; G M Butchko; D Villani-Price; R H Keith; J M Zemaitis
Journal:  J Med Chem       Date:  1989-06       Impact factor: 7.446

2.  Effect of the leukotriene B4 receptor antagonist SC-41930 on colonic inflammation in rat, guinea pig and rabbit.

Authors:  D J Fretland; D Widomski; B S Tsai; J M Zemaitis; S Levin; S W Djuric; R L Shone; T S Gaginella
Journal:  J Pharmacol Exp Ther       Date:  1990-11       Impact factor: 4.030

3.  Pharmacologic and clinical effects of lonapalene (RS 43179), a 5-lipoxygenase inhibitor, in psoriasis.

Authors:  A K Black; R D Camp; A I Mallet; F M Cunningham; M Hofbauer; M W Greaves
Journal:  J Invest Dermatol       Date:  1990-07       Impact factor: 8.551

4.  SC-41930: an inhibitor of leukotriene B4-stimulated human neutrophil functions.

Authors:  B S Tsai; D Villani-Price; R H Keith; J M Zemaitis; R F Bauer; R Leonard; S W Djuric; R L Shone
Journal:  Prostaglandins       Date:  1989-12

5.  Effect of a leukotriene B4 receptor antagonist on leukotriene B4-induced neutrophil chemotaxis in cavine dermis.

Authors:  D J Fretland; D L Widomski; J M Zemaitis; S W Djurić; R L Shone
Journal:  Inflammation       Date:  1989-10       Impact factor: 4.092

6.  The analysis of arachidonic acid metabolites in normal, uninvolved and lesional psoriatic skin.

Authors:  R M Barr; E Wong; A I Mallet; L A Olins; M W Greaves
Journal:  Prostaglandins       Date:  1984-07

7.  Enhanced synthesis of leukotriene B4 by colonic mucosa in inflammatory bowel disease.

Authors:  P Sharon; W F Stenson
Journal:  Gastroenterology       Date:  1984-03       Impact factor: 22.682

8.  Inflammation of guinea pig dermis. Effects of leukotriene B4 receptor antagonist, SC-41930.

Authors:  D J Fretland; D L Widomski; J M Zemaitis; R E Walsh; S Levin; S W Djuric; R L Shone; B S Tsai; T S Gaginella
Journal:  Inflammation       Date:  1990-12       Impact factor: 4.092
  8 in total
  2 in total

1.  Dermal inflammation in primates, mice, and guinea pigs: attenuation by second-generation leukotriene B4 receptor antagonist, SC-53228.

Authors:  D J Fretland; R Gokhale; L Mathur; D A Baron; S K Paulson; J Stolzenbach
Journal:  Inflammation       Date:  1995-06       Impact factor: 4.092

2.  Discovery of leukotriene A4 hydrolase inhibitors using metabolomics biased fragment crystallography.

Authors:  Douglas R Davies; Bjorn Mamat; Olafur T Magnusson; Jeff Christensen; Magnus H Haraldsson; Rama Mishra; Brian Pease; Erik Hansen; Jasbir Singh; David Zembower; Hidong Kim; Alex S Kiselyov; Alex B Burgin; Mark E Gurney; Lance J Stewart
Journal:  J Med Chem       Date:  2009-08-13       Impact factor: 7.446
  2 in total

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