Optimizing The Drug Like Properties Of Leads In Drug Discovery
DOWNLOAD
Download Optimizing The Drug Like Properties Of Leads In Drug Discovery PDF/ePub or read online books in Mobi eBooks. Click Download or Read Online button to get Optimizing The Drug Like Properties Of Leads In Drug Discovery book now. This website allows unlimited access to, at the time of writing, more than 1.5 million titles, including hundreds of thousands of titles in various foreign languages. If the content not found or just blank you must refresh this page
Optimizing The Drug Like Properties Of Leads In Drug Discovery
DOWNLOAD
Author : Ronald Borchardt
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-12-31
Optimizing The Drug Like Properties Of Leads In Drug Discovery written by Ronald Borchardt and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-12-31 with Medical categories.
This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.
Drug Like Properties Concepts Structure Design And Methods
DOWNLOAD
Author : Li Di
language : en
Publisher: Elsevier
Release Date : 2010-07-26
Drug Like Properties Concepts Structure Design And Methods written by Li Di and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-07-26 with Science categories.
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint
Towards Drugs Of The Future
DOWNLOAD
Author : Chris G. Kruse
language : en
Publisher: IOS Press
Release Date : 2008
Towards Drugs Of The Future written by Chris G. Kruse and has been published by IOS Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008 with Business & Economics categories.
"The ninth Solvay Pharmaceutical Conference on Medicinal Chemistry held in Garmisch-Partenkirchen (Germany) September 26-28, 2007"--P. vi.
Drug Like Properties
DOWNLOAD
Author : Li Di
language : en
Publisher: Academic Press
Release Date : 2015-12-17
Drug Like Properties written by Li Di and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-12-17 with Medical categories.
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property. Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization. - Provides a comprehensive and valuable working handbook for scientists and students in medicinal chemistry - Includes expanded coverage of pharmacokinetics fundamentals and effects - Contains updates throughout, including the authors' recent work in the importance of solubility in drug development; new and currently used property methods, with a reduction of seldom-used methods; and exploration of computational modeling methods
Optimization In Drug Discovery
DOWNLOAD
Author : Zhengyin Yan
language : en
Publisher: Springer Science & Business Media
Release Date : 2008-02-06
Optimization In Drug Discovery written by Zhengyin Yan and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-02-06 with Medical categories.
Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addition to potency, which include optimal physicochemical properties, reasonable ph- macokinetic parameters, and good safety profiles. Therefore, research tools must be available in drug discovery to rapidly screen for compounds with favorable drug-like properties, and thus adequate resources can be directed to projects with high potential. Optimization in Drug Discovery: In Vitro Methods is a compilation of detailed experimental protocols necessary for setting up a variety of assays important in compound evaluation. A total of 25 chapters, contributed by many experts in their research areas, cover a wide spectrum of subjects including physicochemical properties, abso- tion, plasma binding, metabolism, drug interactions, and toxicity. A good pharmacokinetic profile has long been recognized as an imp- tant drug-like characteristic. Pharmacokinetic parameters are affected by many properties of drug molecules such as physicochemical nature, abso- tion, metabolic stability, and so on.
Pharmaceutical Profiling In Drug Discovery For Lead Selection
DOWNLOAD
Author : Ronald Borchardt
language : en
Publisher: Springer Science & Business Media
Release Date : 2005-12-05
Pharmaceutical Profiling In Drug Discovery For Lead Selection written by Ronald Borchardt and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2005-12-05 with Medical categories.
At a time when pharmaceutical companies have limited resources to develop newer and better drugs, they must continually evaluate the effectiveness and efficiency of their research and development process. This volume focuses on how to increase the efficiency of drug discovery and development. Written by experienced discovery scientists from diverse disciplines, including chemistry, drug metabolism, and development sciences, it details in silico, in vitro, and in vivo tools for prediction, measurement, and application of compound properties to select and improve potential drug candidates.
Insilico Identification And Optimization Of Natural Inhibitors For Drug Target Sites In Cryptosporidium Parvum
DOWNLOAD
Author : Dr. Pratibha Teotia
language : en
Publisher: Manojvm Publishing House
Release Date :
Insilico Identification And Optimization Of Natural Inhibitors For Drug Target Sites In Cryptosporidium Parvum written by Dr. Pratibha Teotia and has been published by Manojvm Publishing House this book supported file pdf, txt, epub, kindle and other format this book has been release on with Fiction categories.
Now day’s computer-aided drug design considered as a powerful method to design very specific lead compounds that can be developed as drug molecules. Using different in-silico tools, a target is selected and then its structure is defined and determined. After that new chemical/ synthetic compounds can be designed in-silico on the basis of combinatorial chemistry or chosen from an already available chemical library of molecules or library of molecules is generated from a subset of small molecules on the basis of docking and scoring against the particular target. In this study, I attempt to generate 2D QSAR model using small pIC50 values for thirty-eight benzoxazole derivatives binding with C. parvum IMPDH protein resulting correlation coefficient value R2/r2 is 0.7948. Docking results show that out of 38 benzoxazole derivatives, four compounds are most active. The present examination may give the data about potential derivatives of Benzoxazole as chemotherapeutic operators to battle against the expanding weight of Cryptosporidiosis infections.
Computational Drug Discovery
DOWNLOAD
Author : Pooja A. Chawla
language : en
Publisher: Walter de Gruyter GmbH & Co KG
Release Date : 2024-10-07
Computational Drug Discovery written by Pooja A. Chawla and has been published by Walter de Gruyter GmbH & Co KG this book supported file pdf, txt, epub, kindle and other format this book has been release on 2024-10-07 with Science categories.
Computational methods and understanding computational models are important in modern drug discovery. The book focuses on computational approaches that can improve the development of in silico methodologies. It includes lead hit methods, docking algorithms, computational chiral compounds, structure-based drug design, GROMACS and NAMD, structural genomics, toxicity prediction, enzyme inhibitors and peptidomimetic therapeutics
Physicochemical And Biomimetic Properties In Drug Discovery
DOWNLOAD
Author : Klara Valko
language : en
Publisher: John Wiley & Sons
Release Date : 2013-11-25
Physicochemical And Biomimetic Properties In Drug Discovery written by Klara Valko and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-11-25 with Medical categories.
Demonstrating how and why to measure physicochemical and biomimetic properties in early stages of drug discovery for lead optimization, Physicochemical and Biomimetic Properties in Drug Discovery encourages readers to discover relationships between various measurements and develop a sense of interdisciplinary thinking that will add to new research in drug discovery. This practical guide includes detailed descriptions of state-of-the-art chromatographic techniques and uses real-life examples and models to help medicinal chemists and scientists and advanced graduate students apply measurement data for optimal drug discovery.
Prodrug Design
DOWNLOAD
Author : Vivekkumar K Redasani
language : en
Publisher: Academic Press
Release Date : 2015-07-07
Prodrug Design written by Vivekkumar K Redasani and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-07-07 with Science categories.
Prodrug Design: Perspectives, Approaches and Applications in Medicinal Chemistry provides a focused overview of this critical area of drug discovery, as that continuous process strives not only to discover new drug compounds but also to modify the existing ones. This valuable primer supports this mission of drug development and its goal of reducing undesired effects and improving therapeutic effectiveness of drug compounds. Providing a unique compilation of data, insightful case studies, and review of existing literature in the area, the book will promote innovation in medicinal and pharmaceutical chemistry research, exploring the limitations of existing drugs and their improvement. Prodrug Design reviews marketed compounds, the safety of promoieties, and a detailed classification of prodrugs organized by therapeutic area for easy reference. - Offers unique, detailed overview of Prodrug research and literature - Provides detailed chemical structures - Includes Prodrug listing by therapeutic area