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

@article{Chiba2005IdentifiedAM,
  title={Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.},
  author={Jun Chiba and Nobuo Machinaga and Tohru Takashi and Akio Ejima and Gensuke Takayama and Mika Yokoyama and Atsushi Nakayama and John J. Baldwin and Edward McDonald and Kevin Joseph Moriarty and Christopher Sarko and Kurt W. Saionz and Robert Swanson and Zahid Hussain and Angela S. Wong},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2005},
  volume={15 1},
  pages={
          41-5
        }
}
4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.
TLDR
A novel series of benzoic acid derivatives as VLA-4 antagonists with good activity and moderate lipophilicity demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.
Synthesis and antibacterial activity of (1-aryl-1, 2, 3-triazol-4-yl) methyl esters of morpholine-3-carboxylic acid
A series of new 1,2,3-triazolyl methyl ester of morpholine-3-carboxylic acid analogues were designed and synthesized employing click chemistry by using Huisgen 1,3 dipolar cyclo addition reaction
Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
We have focused on optimization of the inadequate pharmacokinetic profile of trans-4-substituted cyclohexanecarboxylic acid 5, which is commonly observed in many small molecule very late antigen-4
Evaluation of stereochemically dense morpholine-based scaffolds as proline surrogates in beta-turn peptides.
TLDR
This study suggests the possibility of functionalizing morpholine-containing beta-turn peptides with no significant loss of the secondary framework.
Synthesis of anti Tricyclic Morpholine Derivatives through Iodine(III)-Mediated Intramolecular Umpolung Cycloaddition of Olefins.
TLDR
A (diacetoxyiodo)benzene-mediated intramolecular cycloaddition of olefins to construct tricyclic morpholines is presented and shows that transformation of Z-alkene was inhibited, which is interpreted by DFT calculations on Z- and E-transition state models.
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