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Mini-Reviews
in Medicinal Chemistry
ISSN: 1389-5575
Mini-Reviews in Medicinal
Chemistry
Volume 8, Number 8, July 2008
Contents
Natural Marine Anti-inflammatory Products
Pp. 740-754
María José Abad, Luis Miguel
Bedoya and Paulina Bermejo
[Abstract]
Inhibitors of c-jun-N-Terminal Kinase (JNK)
Pp. 755-766
Philip LoGrasso and Theodore Kamenecka
[Abstract]
Which Treatment for Nonalcoholic Fatty Liver Disease?
Pp. 767-775
S. Moscatiello, R. Marzocchi, N. Villanova,
E. Bugianesi and G. Marchesini
[Abstract]
Antipsychotic Drugs and Cerebrovascular Events
in Elderly Patients with Dementia: A Systematic Review
Pp. 776-783
Sara Mazzucco, Andrea Cipriani, Corrado
Barbui and Salvatore Monaco
[Abstract]
Conformational Changes of Prion Protein and Nucleic
Acid Arising from their Interaction and Relation of the Altered
Structures in Causing Prion Disease Pp.
784-789
P.K. Nandi
[Abstract]
Current Anti-Infective Treatment of Bacterial
Urinary Tract Infections Pp. 790-795
Florian M.E. Wagenlehner, Christine Wagenlehner,
Kurt G. Naber and W. Weidner
[Abstract]
Nociceptin/Orphanin FQ Peptide Receptor as a Therapeutic
Target for Obesity Pp. 796-811
Magdalena J. Przydzial and Lora
K. Heisler
[Abstract]
Non-Selective Cation Channel Blockers: Potential
Use in Nervous System Basic Research and Therapeutics
Pp. 812-819
Fernando Peña and Benito
Ordaz
[Abstract]
Endothelins Role in the Control of the Acute Phase
of Trypanosoma cruzi Infection Pp. 820-827
Conceição R.S. Machado and
Elizabeth R.S. Camargos
[Abstract]
Hypotensive Natural Products: Current Status
Pp. 828-855
Monica Rosa Loizzo, Rosa Tundis, Federica Menichini,
Giancarlo Antonio Statti and Francesco Menichini
[Abstract]
Abstracts
[Back to top]
Natural Marine Anti-inflammatory Products
María José Abad, Luis Miguel
Bedoya and Paulina Bermejo
The marine environment has been shown to be the source
of a great diversity of chemical structures with promising
biological activities. The isolation, biological evaluation,
chemical properties and synthetic elaborations of the products
of marine organisms and microorganisms have attracted the
attention of organic chemists, medicinal chemists, biologists
and pharmacists. Marine organisms and microorganisms have
provided a large proportion of the natural anti-inflammatory
products over the last years. Marine organisms include green
algae, brown algae, red algae, sponges, coelenterates, bryozoans,
molluscs, tunicates, echinoderms, miscellaneous marine organisms
and marine microorganisms and phytoplankton. This review describes
current progress in the development of a selection of new
anti-inflammatory agents from marine sources. The chemistry
and biological evaluation are discussed.
[Back to top]
Inhibitors of c-jun-N-Terminal Kinase (JNK)
Philip LoGrasso and Theodore Kamenecka
Inhibitors of c-jun-N-Terminal Kinase (JNK) have many
potential therapeutic indications ranging from neurodegenerative
disease, to metabolic disorders, inflammation, cardiovascular
disease, and cancer. This overview will highlight biological
inhibitors such as JNK-interacting protein (JIP) as well as
small molecule inhibitors from various structural classes
including, aminopyrimidines and indazoles.
[Back to top]
Which Treatment for Nonalcoholic Fatty Liver Disease?
S. Moscatiello, R. Marzocchi, N. Villanova,
E. Bugianesi and G. Marchesini
Subjects with nonalcoholic fatty liver disease are at
risk of progressive liver failure. Lifestyle changes including
weight-loss strategies and increased physical activity remain
the first-line approach, but a few pharmacological treatments
have also been successfully tested. Several drugs improve
biochemistry, only a few improve histology; in all cases,
the results were not sustained after treatment stop. Pharmacological
treatment is not so far indicated outside controlled clinical
trials with histological outcomes.
[Back to top]
Antipsychotic Drugs and Cerebrovascular Events in
Elderly Patients with Dementia: A Systematic Review
Sara Mazzucco, Andrea Cipriani, Corrado
Barbui and Salvatore Monaco
Recently, Canadian, US and European health regulatory
agencies issued warnings about an increased risk of stroke
and death in elderly patients with dementia receiving atypical
antipsychotics. Assessing both randomised and non-randomised
evidence, this systematic review found conflicting findings,
particularly for risperidone. More research is needed to better
inform clinical practice.
[Back to top]
Conformational Changes of Prion Protein and Nucleic
Acid Arising from their Interaction and Relation of the Altered
Structures in Causing Prion Disease
P.K. Nandi
Nucleic acids catalyse the conversion of α-helical
prion protein to the β-structured
protein oligomers and amyloids structurally similar to the
infectious isoform of protein. Simultaneously, the prion protein,
similar to gene regulating proteins, bends, unwinds and condenses
nucleic acid. These properties might be related to the biological
function and prion infection.
[Back to top]
Current Anti-Infective Treatment of Bacterial Urinary
Tract Infections
Florian M.E. Wagenlehner, Christine Wagenlehner,
Kurt G. Naber and W. Weidner
Antibiotic resistance nowadays plays an important role
in the treatment of uncomplicated and complicated urinary
tract infections (UTIs). In uncomplicated UTI efforts are
made to use antibiotic substances exclusively for this indication.
In complicated UTI substances with activity against bacteria
harbouring common resistance mechanisms are investigated.
Additionally pharmacokinetic/ pharmacodynamic parameters are
used to improve dosing strategies.
[Back to top]
Nociceptin/Orphanin FQ Peptide Receptor as a Therapeutic
Target for Obesity
Magdalena J. Przydzial and Lora
K. Heisler
Nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor
is a candidate target for novel therapeutics for a range of
conditions, including obesity. This article reviews recent
advances in understanding of N/OFQ’s involvement in
the regulation of food intake and appraises current developments
in the rational design of antagonists aimed at the NOP receptor.
[Back to top]
Non-Selective Cation Channel Blockers: Potential Use
in Nervous System Basic Research and Therapeutics
Fernando Peña and Benito
Ordaz
Non-selective cationic channels (NSCC) are a heterogeneous
family of channels, widely expressed in non-excitable and
excitable cells, that share several functional characteristics
but have diverse molecular origin. NSCC can be formed by transient
receptor potential (TRP) channels, calcium activated non-selective
channels, hyperpolarization activated cation currents, acid-sensitive
cationic channels (ASIC), etc. As a result of its wide expression,
as well as to the fact that the activation of such currents
produce a persistent membrane depolarization, NSCC have been
involved in a variety of neuronal processes such as signal
transduction, firing pattern (including plateau potentials
and bursting mechanisms) as well as synaptic transmission.
Due to the relevance of such channels, alterations in their
normal function have been associated with the pathophysiology
of several nervous system diseases. Over the last years several
blockers of such channels have been discovered. Here we review
the pharmacology of NSCC blockers including trivalent cations,
verapamil derivates, flufenamic acid, the “typical”
TRP blockers 2-APB, ACA and SKF 96365 as well as ASIC blockers.
This review focuses on the pharmacological properties of such
drugs and their potential use for the understanding of the
nervous system as well as for the treatment of neurological
diseases.
[Back to top]
Endothelins Role in the Control of the Acute Phase
of Trypanosoma cruzi Infection
Conceição R.S. Machado and
Elizabeth R.S. Camargos
Disturbances of endothelin production or clearance contribute
to the pathophysiology of several cardiovascular diseases
including Chagas disease cardiomyopath y caused by the protozoan
Trypanosoma cruzi. In rats, endothelins contribute
to control the acute phase, probably by stimulating nitric
oxide production. We point out the necessity for new studies
to better evaluate high levels of endothelin in the course
of other infectious diseases, for which only its detrimental
effects have been emphasized.
[Back to top]
Hypotensive Natural Products: Current Status
Monica Rosa Loizzo, Rosa Tundis, Federica Menichini,
Giancarlo Antonio Statti and Francesco Menichini
Hypertension is a common and progressive disorder that
possesses a major risk for cardiovascular and renal disease.
Recent data have revealed that the global burden of hypertension
is an important and increasing public health problem worldwide
and that the level of awareness, treatment and control of
hypertension varies considerably among countries. Hypertension
is often called a ‘silent killer’ because persons
with this pathological condition can be asymptomatic for years
and then have a fatal heart attack or stroke. The field of
naturally occurring antihypertensive agent is a research area
rapidly expanding due to the high potential of such molecules
as new antihypertensive drugs. Recently, a great number of
plant-derived substances have been evaluated as possible antihypertensive
agents through different mechanisms of action such as alkaloids,
flavonoids and terpenoids. In this mini-review we will discuss
the medicinal chemistry of these compounds.
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