Tags

Type your tag names separated by a space and hit enter

Orally active PDE4 inhibitors with therapeutic potential.
Bioorg Med Chem Lett 2004; 14(5):1323-7BM

Abstract

Based on the successful results in the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid moiety, nitrile moiety and 3-cyclopentyl-4-methoxyphenyl moiety) in the structure of Ariflo 1 was attempted using a bicyclo[3.3.0]octane template instead of a cyclohexane template. As a result, 2a, 7a and 7b were found to be orally active and were predicted to have an improved therapeutic potential based on evaluation by cross-species and same-species comparisons. Structure-activity relationships (SARs) of these compounds are also discussed.

Authors+Show Affiliations

Minase Research Institute, Ono Pharmaceutical Co. Ltd., 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

14980691

Citation

Ochiai, Hiroshi, et al. "Orally Active PDE4 Inhibitors With Therapeutic Potential." Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 5, 2004, pp. 1323-7.
Ochiai H, Ohtani T, Ishida A, et al. Orally active PDE4 inhibitors with therapeutic potential. Bioorg Med Chem Lett. 2004;14(5):1323-7.
Ochiai, H., Ohtani, T., Ishida, A., Kishikawa, K., Obata, T., Nakai, H., & Toda, M. (2004). Orally active PDE4 inhibitors with therapeutic potential. Bioorganic & Medicinal Chemistry Letters, 14(5), pp. 1323-7.
Ochiai H, et al. Orally Active PDE4 Inhibitors With Therapeutic Potential. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1323-7. PubMed PMID: 14980691.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Orally active PDE4 inhibitors with therapeutic potential. AU - Ochiai,Hiroshi, AU - Ohtani,Tazumi, AU - Ishida,Akiharu, AU - Kishikawa,Katuya, AU - Obata,Takaaki, AU - Nakai,Hisao, AU - Toda,Masaaki, PY - 2003/11/14/received PY - 2003/12/01/revised PY - 2003/12/03/accepted PY - 2004/2/26/pubmed PY - 2004/10/13/medline PY - 2004/2/26/entrez SP - 1323 EP - 7 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 14 IS - 5 N2 - Based on the successful results in the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid moiety, nitrile moiety and 3-cyclopentyl-4-methoxyphenyl moiety) in the structure of Ariflo 1 was attempted using a bicyclo[3.3.0]octane template instead of a cyclohexane template. As a result, 2a, 7a and 7b were found to be orally active and were predicted to have an improved therapeutic potential based on evaluation by cross-species and same-species comparisons. Structure-activity relationships (SARs) of these compounds are also discussed. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/14980691/Orally_active_PDE4_inhibitors_with_therapeutic_potential_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960894X03013027 DB - PRIME DP - Unbound Medicine ER -