Literature DB >> 11745742

High throughput physicochemical profiling for drug discovery.

E H Kerns1.   

Abstract

The drug development bottlenecks of attrition and development time are being addressed by acquiring a profile of the candidate's physicochemical and physiological properties during early discovery phases. This information assists selection and optimization of pharmaceutical properties in parallel with activity. High throughput methods to measure the properties: solubility, permeability, lipophilicity, pKa, stability and integrity are described and compared in this article. The underlying discovery requirements, needs and application strategies are discussed. Copyright 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association

Mesh：

Year:  2001        PMID： 11745742     DOI： 10.1002/jps.1134

Source DB:  PubMed          Journal:  J Pharm Sci        ISSN： 0022-3549            Impact factor:   3.534


  28 in total

1.  Impact of the amount of excess solids on apparent solubility.

Authors:  Kohsaku Kawakami; Kyoko Miyoshi; Yasuo Ida
Journal:  Pharm Res       Date:  2005-08-24       Impact factor: 4.200

2.  Discovery pharmaceutics--challenges and opportunities.

Authors:  Xue-Qing Chen; Melissa D Antman; Christoph Gesenberg; Olafur S Gudmundsson
Journal:  AAPS J       Date:  2006-06-02       Impact factor: 4.009

Review 3.  Current industrial practices of assessing permeability and P-glycoprotein interaction.

Authors:  Praveen V Balimane; Yong-Hae Han; Saeho Chong
Journal:  AAPS J       Date:  2006-01-13       Impact factor: 4.009

4.  Comparative QSAR studies on PAMPA/modified PAMPA for high throughput profiling of drug absorption potential with respect to Caco-2 cells and human intestinal absorption.

Authors:  Rajeshwar P Verma; Corwin Hansch; Cynthia D Selassie
Journal:  J Comput Aided Mol Des       Date:  2007-01-26       Impact factor: 3.686

5.  Screening candidate anticancer drugs for brain tumor chemotherapy: pharmacokinetic-driven approach for a series of (E)-N-(substituted aryl)-3-(substituted phenyl)propenamide analogues.

Authors:  Hua Lv; Fan Wang; M V Ramana Reddy; Qingyu Zhou; Xiaoping Zhang; E Premkumar Reddy; James M Gallo
Journal:  Invest New Drugs       Date:  2012-03-01       Impact factor: 3.850

6.  Rapid experimental measurements of physicochemical properties to inform models and testing.

Authors:  Chantel I Nicolas; Kamel Mansouri; Katherine A Phillips; Christopher M Grulke; Ann M Richard; Antony J Williams; James Rabinowitz; Kristin K Isaacs; Alice Yau; John F Wambaugh
Journal:  Sci Total Environ       Date:  2018-05-02       Impact factor: 7.963

7.  Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies.

Authors:  Eric M Guantai; Kanyile Ncokazi; Timothy J Egan; Jiri Gut; Philip J Rosenthal; Ravi Bhampidipati; Anitha Kopinathan; Peter J Smith; Kelly Chibale
Journal:  J Med Chem       Date:  2011-05-05       Impact factor: 7.446

8.  Determination of drug-like properties of a novel antileishmanial compound: In vitro absorption, distribution, metabolism, and excretion studies.

Authors:  Susanta Kumar Mondal; Nirup B Mondal; Sukdeb Banerjee; Upal Kanti Mazumder
Journal:  Indian J Pharmacol       Date:  2009-08       Impact factor: 1.200

Review 9.  Applications of hot-melt extrusion for drug delivery.

Authors:  Michael A Repka; Soumyajit Majumdar; Sunil Kumar Battu; Ramesh Srirangam; Sampada B Upadhye
Journal:  Expert Opin Drug Deliv       Date:  2008-12       Impact factor: 6.648

10.  2-Aminooxazole as a Novel Privileged Scaffold in Antitubercular Medicinal Chemistry.

Authors:  Elisa Azzali; Miriam Girardini; Giannamaria Annunziato; Marialaura Pavone; Federica Vacondio; Giorgia Mori; Maria Rosalia Pasca; Gabriele Costantino; Marco Pieroni
Journal:  ACS Med Chem Lett       Date:  2020-06-08       Impact factor: 4.345
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