Natural products are a constant source of potentially active compounds for the treatment of various disorders. The Middle East and tropical regions are believed to have the richest supplies of natural products in the world. Plant derived secondary metabolites have been used by humans to treat acute infections, health disorders and chronic illness for tens of thousands of years. Only during the last 100 years have natural products been largely replaced by synthetic drugs.
The discovery of efficacious new human therapeutic agents is one of humanity’s most vital
tasks. It is an enormously demanding activity that requires creativity, a vast range of scientific
knowledge, and great persistence. It is also an exceedingly expensive activity. In an
ideal world, no education would be complete without some exposure to the ways in which
new medicines are discovered and developed. For those young people interested in science
or medicine, such knowledge is arguably mandatory....
Great efﬁciencies have been achieved in the drug discovery process as a result of technological advances in target identiﬁcation, high-throughput screening, high-throughput organic synthesis, just-in-time in vitro ADME (absorption, distribution, metabolism, and excretion), and early pharmacokinetic screening of drug leads. These advances, spanning target selection all the way through to clinical candidate selection, have placed greater and greater demands on the analytical community to develop robust high-throughput methods.
The modern drug discovery process, in general, involves the identiﬁcation of a biochemical target (usually protein target), screening of synthetic compounds or compound libraries from combinatorial chemistry/natural sources for a lead compound, and optimization of the lead compound (activity, selectivity, pharmacokinetics, etc.) for recommending a potential clinical candidate.
Despite massive efforts in drug discovery fueled by combinatory
chemistry, recombinant DNA technology, and highthroughput
screening, surprisingly few molecules make it
through the drug development process. While the reasons
are debated, it is certain that many new chemical entities
(NCEs) suffer from recurring problems that hinder development—
low water solubility, instability, or inadequate
pharmacokinetics. An estimated 43% of NCEs are poorly
In a certain sense, the field of drug metabolism (DM) is standing still. More
specifically, the basic experiment of drug metabolism (i.e., administering a new
drug to an animal or human and determining the structures, amounts, and
disposition of the metabolites) has changed very little over a period of decades.
Remarkably, the experimental design and resulting data set from a typical
absorption, distribution, metabolism, and excretion (ADME) study conducted
today would be instantly recognized and understood by DM scientists from 50
Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Distribution patterns of small-molecule ligands in the protein universe and implications for origin of life and drug discovery...
The workshop summarized in this volume was the third international meeting in a series
sponsored by the Forum on Drug Discovery, Development, and Translation of the Institute of
Medicine (IOM) to gather information from experts around the world on the threat of drugresistant
tuberculosis (TB) and how it can be addressed. The workshop was held April 18-19 and
21, 2011, in New Delhi, India, in collaboration with the Indian National Science Academy
(INSA) and the Indian Council of Medical Research (ICMR)....
Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Wertheim cung cấp cho các bạn kiến thức về ngành y đề tài: Meeting the challenges of drug discovery: a multidisciplinary re-evaluation of current practices...
Advanced Computer-Assisted Techniques in Drug Discovery
edited by Han van de Waterbeemd
.Methods and Principles in Medicinal Chemistry
Edited by R. Mannhold P. Krogsgaard-Larsen H. Timmerman
Volume 1 Hugo Kubinyi, QSAR: Hansch Analysis and Related Approaches Volume 2 Han van de Waterbeemd (ed.), Chemometric Methods in Molecular Design Volume 3
Han van de Waterbeemd (ed.), Advanced Computer- Assisted Techniques in Drug Discovery
.Methods and Principles in Medicinal Chemistry
edited by R. Mannhold, P. Krogsgaard-Larsen, H.
It has been a privilege to watch the growth of RNA interference technology over
the last ten years. Starting with a mixture of curiosity and chagrin, the field has
grown into a substantial enterprise which impacts (and utilizes resources from)
virtually every field of biomedical research. Research in RNAi derives from a set of
apparently unconnected observations: strange pigment patterns in plants, unexpected
failures and successes in antisense and overexpression studies, small regulatory
RNAs in bacteria.
It has been nearly 20 years since the last Humana Press book devoted to
serotonin (5-hydroxytryptamine; 5-HT) receptors has appeared. Since then, the
field of 5-HT receptors has undergone a revolution due to the discovery of many
additional 5-HT receptors. Although 5-HT was chemically elucidated in 1948 by
Page and colleagues (Rapport et al.
Several years ago we noted a paucity of textbooks
that dealt with the principles of pharmacology as a science
rather than pharmacology as a therapeutic entity.
In an attempt to remedy this we organized a textbook
designed to meet the needs of students interested in
pharmacology at the advanced undergraduate and
early graduate level. This text addresses the many
facets that form the foundation of pharmacology.
Students will find extensive discussions by leaders in
the field are written in clear and straightforward manner.
For the last 60 or so years the chemotherapy of bacterial infections has been dominated
by natural products and their semi-synthetic variants. Although the term antibiotic
was initially used exclusively to describe those anti-bacterials of natural or
semi-synthetic origin, it has become broadened in common usage to include antibacterial
agents of purely synthetic origin as well. The emphasis of this chapter will be
on the discovery of novel prototype structures that represent the different classes of
Discovery of a new chemical entity that exerts pharmacological effects for
curing or treating diseases or relieving symptoms is only the first step in
the drug developmental process. In the developmental cycle of a new
drug, the delivery of a desired amount of a therapeutic agent to the target
at a specific time or duration is as important as its discovery. In order
to realize the optimal therapeutic outcomes, a delivery system should
be designed to achieve the optimal drug concentration at a predetermined
rate and at the desired location....
With publication of the human genome has come an
experiment in reductionism for drug discovery. With the
evaluation of the number and quality of new drug
treatments from this approach has come a reevaluation
of target-based versus systems-based strategies. Pharmacology,
historically rooted in systems-based approaches
and designed to give systems-independent measures
of drug activity, is suitably poised to be a major (if
not the major) tool in this new environment of drug
(BQ) Part 1 book "Textbook of organic medicinal and pharmaceutical chemistry" presents the following contents: Drug design strategies, metabolic changes of drugs and related organic compounds, biotechnology and drug discovery, immunobiologicals, anti infective agents, antibacterial antibiotics, antiviral agents,...
Medicinal chemistry is a discipline at the intersection of chemistry, especially synthetic
organic chemistry, and pharmacology and various other biological specialties, where
they are involved with design, chemical synthesis and development for market of
pharmaceutical agents (drugs). Compounds used in medical applications are most
often organic compounds, which are often divided into the broad classes of small
organic molecules and biologics, the latter of which are most often medicinal
preparations of proteins. Inorganic and organometallic compounds are also useful as
In the modern pharmaceutical industry, high-performance liquid chromatography (HPLC) is the major and integral analytical tool applied in all stages of drug discovery, development, and production. The development of new chemical entities (NCEs) is comprised of two major activities: drug discovery and drug development. The goal of the drug discovery program is to investigate a plethora of compounds employing fast screening approaches, leading to generation of lead compounds and then narrowing the selection through targeted synthesis and selective screening (lead optimization).