Literature DB >> 12639566

A structure-permeability study of small drug-like molecules.

Thomas Fichert1, Mehran Yazdanian, John R Proudfoot.   

Abstract

A systematic structure-permeability relationship study on a set of small drug-like molecules with log D values in the range -2.5 to 3 and carrying a diverse array of functionality reveals that the compounds with log D>0 and <3 are highly permeable. Surprisingly, several tetrazole derivatives were found to be substrates for efflux pump(s).

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Year:  2003        PMID: 12639566     DOI: 10.1016/s0960-894x(02)01035-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  15 in total

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3.  Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections.

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4.  Photocaged permeability: a new strategy for controlled drug release.

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5.  Synthesis and in vitro pharmacological evaluation of indolyl carboxylic amide analogues as D3 dopamine receptor selective ligands.

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Journal:  Medchemcomm       Date:  2013-09       Impact factor: 3.597

6.  Evaluation of physicochemical properties and intestinal permeability of six dietary polyphenols in human intestinal colon adenocarcinoma Caco-2 cells.

Authors:  Himanshu Rastogi; Snehasis Jana
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7.  Peptide library approach to uncover phosphomimetic inhibitors of the BRCA1 C-terminal domain.

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Review 8.  Medicinal chemical properties of successful central nervous system drugs.

Authors:  Hassan Pajouhesh; George R Lenz
Journal:  NeuroRx       Date:  2005-10

9.  Synthesis, antibiotic modifying activity, ADMET study and molecular docking of chalcone (E)-3-(2,4-dichlorophenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one in strains of Staphylococcus aureus carrying MepA efflux pumps.

Authors:  Janaína Esmeraldo Rocha; Thiago Sampaio de Freitas; Jayze da Cunha Xavier; Raimundo Luiz Silva Pereira; Francisco Nascimento Pereira; Carlos Emídio Sampaio Nogueira; Márcia Machado Marinho; Paulo Nogueira Bandeira; Maria Alyce Albuquerque Fernandes; Emmanuel Silva Marinho; Alexandre Magno Rodrigues Teixeira; Hélcio Silva Dos Santos; Henrique Douglas Melo Coutinho
Journal:  Arch Microbiol       Date:  2021-12-23       Impact factor: 2.552

10.  Synthesis and Structure-Activity Relationships of 5'-Aryl-14-alkoxypyridomorphinans: Identification of a μ Opioid Receptor Agonist/δ Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects.

Authors:  Rakesh H Vekariya; Wei Lei; Abhisek Ray; Surendra K Saini; Sixue Zhang; Gabriella Molnar; Deborah Barlow; Kelly L Karlage; Edward J Bilsky; Karen L Houseknecht; Tally M Largent-Milnes; John M Streicher; Subramaniam Ananthan
Journal:  J Med Chem       Date:  2020-06-30       Impact factor: 8.039

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