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The spectacular advances of medicinal chemistry in the last few
decades have been triggered by a greater understanding of cellular
processes at the molecular level. The understanding of biochemical
processes and diseases at molecular level has revolutionized the
field. This volume summarizes recent developments in the area of
biological inhibitors such as squalene epoxidase inhibitors, dual
inhibitors of 5-lipoxygenase and cycloxgenase, inhibition of
cholestrol biosynthesis, HIV proteinase inhibitors, nonpeptide
antagonists at peptide receptors, and binding interaction of
thyroid hormones.
The goal of an activity-directed isolation process is to isolate
bioactive compounds which may provide structural leads of
therapeutic importance. Whereas the traditional process of drug
development is long and expensive, simple and rapid bioassays can
serve as the starting point for drug discovery. This book presents
a range of "bench top" bioassay techniques useful for natural
product and pharmaceutical chemists involved in drug discovery and
pharmacognosy. The contents detail a number of enzyme-based assays,
cell-based functional bioassays and receptor radioligand binding
assays along with detailed descriptions of each type. The majority
of these bioassays are presented in a step-by-step format, so they
could even be implemented by technical personnel with little
background in microbiology, biochemistry or pharmacology.
Originally published by Bentham and now distributed by Elsevier,
Recent Advances in Medicinal Chemistry, Volume 1 covers
leading-edge research and recent developments in rational drug
design, synthetic chemistry, bioorganic chemistry, high-throughput
screening, combinatorial chemistry, drug targets, and natural
product research and structure-activity relationship studies. The
fourteen updated reviews include unique experimental data and
references, and each article highlights an important topic in
current medicinal chemistry research. Topics covered include:
aureolic acid group of anti-cancer antibiotics and non-steroidal
anti-inflammatory drugs; aromatase inhibitors in adjuvant endocrine
treatment of early-stage breast cancer in postmenopausal women; Rho
GTPases and statins in targeting and developing therapies for
tumors; and more.
The inhibition of angiogenesis is an effective mechanism of slowing
down tumor growth and malignancies. The process of induction or
pro-angiogenesis is highly desirable for the treatment of
cardiovascular diseases, wound healing disorders, and more. Efforts
to understand the molecular basis, both for inhibition and
induction, have yielded fascinating results. Originally published
by Bentham and now distributed by Elsevier, Anti-Angiogenesis Drug
Discovery and Development, Volume 2 is an compilation of
well-written reviews on various aspects of the anti-angiogenesis
process. These reviews have been contributed by leading
practitioners in drug discovery science and highlight the major
developments in this exciting field in the last two decades. These
reader-friendly chapters cover topics of great scientific
importance, many of which are considered significant medical
breakthroughs, making this book excellent reading both for the
novice as well as for expert medicinal chemists and clinicians.
Solving Problems with NMR Spectroscopy, Second Edition, is a fully
updated and revised version of the best-selling book. This new
edition still clearly presents the basic principles and
applications of NMR spectroscopy with only as much math as is
necessary. It shows how to solve chemical structures with NMR by
giving many new, clear examples for readers to understand and try,
with new solutions provided in the text. It also explains new
developments and concepts in NMR spectroscopy, including
sensitivity problems (hardware and software solutions) and an
extension of the multidimensional coverage to 3D NMR. The book also
includes a series of applications showing how NMR is used in real
life to solve advanced problems beyond simple small-molecule
chemical analysis. This new text enables organic chemistry students
to choose the most appropriate NMR techniques to solve specific
structures. The problems provided by the authors help readers
understand the discussion more clearly and the solution and
interpretation of spectra help readers become proficient in the
application of important, modern 1D, 2D, and 3D NMR techniques to
structural studies.
Drug Design and Discovery in Alzheimer's Disease includes expert
reviews of recent developments in Alzheimer's disease (AD) and
neurodegenerative disease research. Originally published by Bentham
as Frontiers in Drug Design and Discovery, Volume 6and now
distributed by Elsevier, this compilation of the sixteen articles,
written by leading global researchers, focuses on key developments
in the understanding of the disease at molecular levels,
identification and validation of molecular targets, as well as
innovative approaches towards drug discovery, development, and
delivery. Beginning with an overview of AD pharmacotherapy and
existing blockbuster drugs, the reviews cover the potential of both
natural and synthetic small molecules; the role of cholinesterases
in the on-set and progression of AD and their inhibition; the role
of beta-site APP clearing enzyme-1 (BACE-1) in the production of
ss-amyloid proteins, one of the key reasons of the progression of
AD; and other targets identified for AD drug discovery.
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