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Volumn 8, Issue 19, 1998, Pages 2737-2742

2-substituted-4-methoxybenzimidazole-based PDE4 inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; PHOSPHODIESTERASE IV INHIBITOR; PICLAMILAST; ROLIPRAM;

EID: 0032491238     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00497-1     Document Type: Article
Times cited : (15)

References (26)
  • 13
    • 0010364856 scopus 로고    scopus 로고
    • Byk Gulden Lomberg: WO 96/03399, 1996 and Chiroscience: WO 97/44337, 1997
    • (b) For recent patent activity on the replacement of the 3,4-dialkoxyphenyl ring with benzofurans see: Byk Gulden Lomberg: WO 96/03399, 1996 and Chiroscience: WO 97/44337, 1997.
  • 15
    • 0010404915 scopus 로고    scopus 로고
    • Chiroscience: WO 97/44036, 1997
    • (c) For recent reports of other heterocycles as surrogates for the 3,4-dialkoxyphenyl ring see: Hulme, C.; Moriarity, K.; Miller, B.; Mathew, R.; Ramanjulu, M.; Cox, P.; Souness, J.; Page, K. M.; Uhl, J.; Travis, J.; Huang, F-C.; Labaudinere, R.; Djuric, S. W. Bioorg. Med. Chem. Lett. 1998, 8, 1867; Chiroscience: WO 97/44036, 1997; Pfizer: WO 97/42174-Al, 1997 and Rhône-Poulenc Rorer: WO 97/48697, 1997.
  • 16
    • 0010359160 scopus 로고    scopus 로고
    • Pfizer: WO 97/42174-Al, 1997 and Rhône-Poulenc Rorer: WO 97/48697, 1997
    • (c) For recent reports of other heterocycles as surrogates for the 3,4-dialkoxyphenyl ring see: Hulme, C.; Moriarity, K.; Miller, B.; Mathew, R.; Ramanjulu, M.; Cox, P.; Souness, J.; Page, K. M.; Uhl, J.; Travis, J.; Huang, F-C.; Labaudinere, R.; Djuric, S. W. Bioorg. Med. Chem. Lett. 1998, 8, 1867; Chiroscience: WO 97/44036, 1997; Pfizer: WO 97/42174-Al, 1997 and Rhône-Poulenc Rorer: WO 97/48697, 1997.
  • 17
    • 0010362295 scopus 로고    scopus 로고
    • unpublished results
    • 11. Pharmacokinetic studies on 2 have shown that this compound undergoes extensive first pass metabolism in mice resulting in <5% bioavailability. Page, K. M. unpublished results.
    • Page, K.M.1
  • 25
    • 0010316928 scopus 로고    scopus 로고
    • note
    • 18. Murine endotoxemia model. Compounds were administered orally in a vehicle of 0.24% methylcellulose/0.2% Tween-20 in water to male, Balb/c mice (20-25 g, Harlan-Sprague Dawley, Inc., Indianapolis, IN) 4 h prior to challenge with LPS (E. coli 055:B5, Sigma Chemical Co., St. Louis, MO, 30 μg/mouse by intraperitoneal injection). Ninety minutes following LPS challenge, mice were anesthetized with Isoflurane and blood was collected by cardiac puncture. The whole blood was allowed to clot on ice and serum was prepared by centrifugation at 500 x g for 10 min. Serum was assayed for TNF-α by ELISA (Genzyme Corp., Cambridge, MA). Dose response curves were generated in duplicate from n = 4-6 mice per dose.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.