2. Academic Validation
  3. Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist

Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist

  • Bioorg Med Chem Lett. 2005 Jan 3;15(1):41-5. doi: 10.1016/j.bmcl.2004.10.041.
Jun Chiba 1,  Nobuo Machinaga,  Tohru Takashi,  Akio Ejima,  Gensuke Takayama,  Mika Yokoyama,  Atsushi Nakayama,  John J Baldwin,  Edward McDonald,  Kevin J Moriarty,  Christopher R Sarko,  Kurt W Saionz,  Robert Swanson,  Zahid Hussain,  Angela Wong
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd, 16-13 Kitakasai 1-chome, Edogawa-ku, Tokyo 134-8630, Japan. chiba2mk@daiichipharm.co.jp
PMID: 15582407 DOI: 10.1016/j.bmcl.2004.10.041
Abstract

An investigation into the structure-activity relationship of a lead compound, prolyl-5-aminopentanoic acid 4, led to the identification of a novel series of 4-piperidinylacetic acid, 1-piperazinylacetic acid, and 4-aminobenzoic acid derivatives as potent VLA-4 antagonists with low nanomolar IC(50) values. A representative compound morpholinyl-4-piperidinylacetic acid derivative (13d: IC(50)=4.4 nM) showed efficacy in the Ascaris-antigen sensitized murine airway inflammation model by oral administration.

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