Current topics in medicinal chemistry

Publisher: Bentham Science Publishers

Current impact factor: 3.40

Impact Factor Rankings

2016 Impact Factor Available summer 2017
2014 / 2015 Impact Factor 3.402
2013 Impact Factor 3.453
2012 Impact Factor 3.702
2011 Impact Factor 4.174
2010 Impact Factor 4.112
2009 Impact Factor 4.473
2008 Impact Factor 4.268
2007 Impact Factor 4.325
2006 Impact Factor 4.167
2005 Impact Factor 4.4

Impact factor over time

Impact factor
Year

Additional details

5-year impact 3.63
Cited half-life 4.90
Immediacy index 0.62
Eigenfactor 0.01
Article influence 0.91
ISSN 1873-4294

Publisher details

Bentham Science Publishers

  • Pre-print
    • Author can archive a pre-print version
  • Post-print
    • Author cannot archive a post-print version
  • Restrictions
    • 12 months embargo
  • Conditions
    • Author's pre-print on author's personal website, institutional repository and open access repository
    • Author's post-print on author's personal website, institutional repository, open access repository, PubMed Central and arXiv
    • Non-Commercial
    • Published source must be acknowledged
    • Must link to journal homepage with DOI
    • Publisher's version/PDF cannot be used
  • Classification
    yellow

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: Anxiety disorders are the most common mental illnesses affecting human beings. They range from panic to generalized anxiety disorders upsetting the well-being and psychosocial performance of patients. Several conventional anxiolytic drugs are being used which in turn result in several adverse effects. Therefore, studies to find suitable safe medicines from natural sources are being conducted by researchers. The aim of the present study is to comprehensively review phytochemical compounds with well-established anxiolytic activities and their structure-activity relationships as well as neuropsychopharmacological aspects. Results showed that phytochemicals like; alkaloids, flavonoids, phenolic acids, lignans, cinnamates, terpenes and saponins possess anxiolytic effects in a wide range of animal models of anxiety. The involved mechanisms include interaction with γ-aminobutyric acid (GABA)A receptors at benzodiazepine (BZD) and non-BZD sites with various affinity to different subunits, serotonergic 5-hydrodytryptamine (5-HT)1A and 5-HT2A/C receptors, noradrenergic and dopaminergic systems, glycine and glutamate receptors, and κ-opioid receptor as well as cannabinoid (CB)1 and CB2 receptors. Phytochemicals also modulate the hypothalamo-pituitary-adrenal (HPA) axis, the levels of pro-inflammatory cytokines like interleukin (IL)-2, IL-6, IL-1β and tumor necrosis factor (TNF)-α, and improve brain derived neurotrophic factor (BDNF) levels. Transient receptor potential cation channel subfamily V (TRPV)3, nitric oxide cyclic guanosine monophosphate (NO-cGMP) pathway and monoamine oxidase enzymes are other targets of phytochemicals with anxiolytic activity. Taking together, these phytochemicals may be considered as supplements to conventional anxiolytic therapies in order to improve efficacy and reduce adverse effects. Further preclinical and clinical studies are still needed in order to recognize the structure-activity relationships, metabolism, absorption, and neuropsychopharmacological mechanisms of plant-derived natural agents.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Resveratrol (3,4',5-trihydroxystilbene) is a naturally occurring polyphenolic compound present in over 70 different plant-derived products, including red wine, grapes, berries, chocolate and peanuts. Clinically, resveratrol demonstrates strong antioxidant, anti-inflammatory, anti-viral, and anti-cancer properties. Although resveratrol was first isolated in 1940, it was not until the last decade that it was recognised for its potential therapeutic role in reducing the risk of neurodegenerative disorders, and Alzheimer's disease (AD) in particular. AD is the leading cause of progressive dementia, in the elderly. Resveratrol has been shown to exhibit neuroprotective effects in a variety of in vitro and in vivo models of AD. Apart from its potent antioxidant and anti-inflammatory roles, evidence suggests that resveratrol also facilitates non-amyloidogenic cleavage of the amyloid precursor protein (APP), and promotes clearance of neurotoxic amyloid beta (Aβ) peptides, a critical step in preventing and slowing down AD pathology. Resveratrol also reduces damage to neuronal cells via a variety of additional mechanisms, most notably is the activation of a new class of NAD+-dependent histone deacetylases enzymes known as sirtuins. However in spite of the considerable advances in defining the mechanism of action of resveratrol, it is unlikely to be effective as monotherapy in AD due to its poor bioavailability, biotransformation, and requisite synergism with other dietary factors. This review summarizes the relevance of resveratrol in the pathophysiology of AD. It also highlights why resveratrol alone may not be an effective single therapy, and how resveratrol coupled to other compounds might yet prove an effective therapy with multiple targets.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: According to the epidemiological reports published by the World Health Organization, the proportion of elderly people (over 60 years) will increase from 11% to 22% by 2050 worldwide. This increase will be associated with a growing rate of morbidity and mortality of age-related diseases. Mental and neurodegenerative diseases are important health problems in elderly people. Therefore, recent research has been focused on finding effective neuroprotective agents with low adverse effects. Over the last two decades, much attention has been drawn to plant-derived bioactive compounds as novel therapeutic agents for treatment of neurodegenerative diseases such as Alzheimer's disease (AD) and Parkinson's disease (PD). Among them, flavonoid chemical class is known as one of the most bioactive and non-toxic phytochemicals, which are widely found in different herbal medicines and edible plants. Fisetin is one of the most common and bioactive flavonoids which possesses potential neuroprotective effects. Fisetin also enhances learning and memory, decreases neuronal cell death, and suppresses oxidative stress. The present paper aims to critically evaluate the available literature regarding the beneficial effects of fisetin on neurodegenerative diseases, especially AD and PD.. In addition, we provide information regarding the chemistry, sources, bioavailability and clinical impacts of fisetin to provide a broad spectrum for the use of this compound as a new approach to the treatment of AD and PD.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Parkinson's disease is a motor dysfunction that have been widely studied but many of the reports on commercial drugs for the treatment of this disease have afforded some undesirable side effects that generate an extensive and unviable treatment by economic costs and due to the bioavailability of the assayed compounds. At present, some molecules are used as L-DOPA agonists or can change the dopamine concentrations in the CNS. Thus, the use of aporphine-type alkaloids has given a real alternative due to the diverse natural sources where can be isolated or to obtain them by means of conventional syntheses. Isoquinoline alkaloids as Liriodenine, phenanthrene-type alkaloids, alkoxy-hydroxyaporphine, aminothiazole-aporphine or Lipoic ester aporphine derivatives are some of the examples to be considered in this mini-review, wherein the applied pharmacological effects to reduce the motor disorders and the possible medical properties of these alkaloids on the dopaminergic receptors are analyzed.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Due to multi-faceted pathology of AD, no drug can seize the progress of the disease, whereas only the symptomatic treatment is available at the moment. Several drug classes to treat AD are available in clinical use, AChEIs being the most prescribed. In addition to AChEIs, secretase enzymes and iron chelators have turned out to be the focus of research and the popular targets in drug discovery against AD. The latest approaches such as immunotherapy, multi-targeted drug ligand design, AChE inhibitors, antioxidants, metal chelators, monoamine oxidase (MAO) inhibitors, anti-inflammatory drugs, and N-methyl-D-aspartate (NMDA) inhibitors are currently in use to cure this disease to some extent. But, there is a certain need to develop new drugs to fight with AD, particularly acting on multi-targets or with dual mechanisms of action. In this review, a particular emphasis will be focused on multi-targets aiming at AD to design new drug molecules with respect to treatment strategies and preventive measures. Since the underlying pathogenesis of AD is complicated and still under investigation, the attempts to design highly selective and potent agents to treat AD are quite intensively continuing. In this respect, designing novel drugs with dual/multi-acting mechanisms seems to be more rational.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Omega-3 and omega-6 fatty acids are polyunsaturated fatty acids (PUFAs) with multiple double bonds. Linolenic and alpha-linolenic acids are omega-6 and omega-3 PUFAs, precursors for the synthesis of long-chain PUFAs (LC-PUFAs), such as arachidonic acid (omega-6 PUFA), and eicosapentaenoic and docosahexaenoic acids (omega-3 PUFAs). The three most important omega-3 fatty acids are alpha-linolenic, eicosapentaenoic and docosahexaenoic acids, which cannot be synthesized in enough amounts by the body, and therefore they must be supplied by the diet. Omega-3 fatty acids are essential for the correct functioning of the organism and participate in many physiological processes in the brain. Epilepsy is a common and heterogeneous chronic brain disorder characterized by recurrent epileptic seizures leading to neuropsychiatric disabilities. The prevalence of epilepsy is high achieving about 1% of the general population. There is evidence suggesting that omega-3 fatty acids may have neuroprotective and anticonvulsant effects and, accordingly, may have a potential use in the treatment of epilepsy. In the present review, the potential use of omega-3 fatty acids in the treatment of epilepsy, and the possible proposed mechanisms of action are discussed. The present article summarizes the recent knowledge of the potential protective role of dietary omega-3 fatty acids in epilepsy.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Δ9-tetrahydrocannabinol and its analogues are found to have particular application in psychiatry because of their antipsychotic properties suggesting a therapeutic use as neuroleptic agents in limiting psychotic diseases. These treatments should not only aim to alleviate specific symptoms but also attempt to delay/arrest disease progression. In the present review, we reported recent studies supporting the view that the cannabinoid signalling system is a key modulatory element in the activity of the striatum and temporal cortex that has been traditionally associated with psychosis and schizophrenia. This idea is supported by different anatomical, electrophysiological, pharmacological and biochemical data. Furthermore, these studies indicate that the cannabinoid system is impaired in different psychotic disorders, supporting the idea of developing novel pharmacotherapies with compounds that selectively target specific elements of the cannabinoid system.
    No preview · Article · Feb 2016 · Current topics in medicinal chemistry
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    ABSTRACT: Breathomics, the multidimensional molecular analysis of exhaled breath, includes analysis of exhaled breath with gas-chromatography/mass spectrometry (GC/MS) and electronic noses (e-noses), and metabolomics of exhaled breath condensate (EBC), a non-invasive technique which provides information on the composition of airway lining fluid, generally by high-resolution nuclear magnetic resonance (NMR) spectroscopy or MS methods. Metabolomics is the identification and quantification of small molecular weight metabolites in a biofluid. Specific profiles of volatile compounds in exhaled breath and metabolites in EBC (breathprints) are potentially useful surrogate markers of inflammatory respiratory diseases. Electronic noses (e-noses) are artificial sensor systems, usually consisting of chemical cross-reactive sensor arrays for characterization of patterns of breath volatile compounds, and algorithms for breathprints classification. E-noses are handheld, portable, and provide real-time data. E-nose breathprints can reflect respiratory inflammation. E-noses and NMR-based metabolomics of EBC can distinguish patients with respiratory diseases such as asthma, COPD, and lung cancer, or diseases with a clinically relevant respiratory component including cystic fibrosis and primary ciliary dyskinesia, and healthy individuals. Breathomics has also been reported to identify patients affected by different types of respiratory diseases. Patterns of breath volatile compounds detected by e-nose and EBC metabolic profiles have been associated with asthma phenotypes. In combination with other -omics platforms, breathomics might provide a molecular approach to respiratory disease phenotyping and a molecular basis to tailored pharmacotherapeutic strategies. Breathomics might also contribute to identify new surrogate markers of respiratory inflammation, thus, facilitating drug discovery. Validation in newly recruited, prospective independent cohorts is essential for development of e-nose and EBC NMRbased metabolomics techniques.
    No preview · Article · Dec 2015 · Current topics in medicinal chemistry
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    ABSTRACT: Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play important roles both in the control of heart rate and neuronal excitability. HCN channels open on hyperpolarization voltage, permeate to potassium and sodium, and generate an inward current, which is modulated by intracellular cAMP. HCN channels have been reported to involve in various human diseases, including heart failure, pain and epilepsy with datas from mutagenesis, transgenic mice and pharmacological studies. As a result, HCN channels may offer excellent drug development opportunities for novel analgestic, bradycardic and anticonvulsant drugs. Ivabradine is the first HCN channel inhibitor being clinically approved in 2005 for the treatment of chronic stable angina pectoris and heart failure. This review will summarize the structure and function of HCN channels. Further, we will discuss recent advances concerning the identification and action mechanism of reported HCN channel inhibitors.
    No preview · Article · Dec 2015 · Current topics in medicinal chemistry
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    ABSTRACT: The prime role of mutations in the genes encoding chloride ion channels in various human diseases of muscle, kidney, bone and brain have been well established. It includes diseases such as myotonia congenita, dystrophia myotonica, cystic fibrosis, osteopetrosis, epilepsy as well as glioma progression in brain and malaria parasite in red blood cells. In view of this the present article emphasises on the various diseases associated with chloride channel regulation and their modulators. Studies on various chloride channels and their modulators have been discussed in detail.
    No preview · Article · Dec 2015 · Current topics in medicinal chemistry
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    ABSTRACT: Hepatitis C virus (HCV) infection is a major worldwide epidemic disease. It is estimated that more than 170 million individuals are infected with HCV and with three to four million new cases each year. Many new direct-acting antiviral (DAA) agents that specifically target HCV NS3 protease or NS5B polymerase inhibitors are therefore in development, with a significant effect for the patient and for the market recently. The non-structural 4B (NS4B) protein, is among the least characterized of the HCV proteins. A variety of functions have been recognized for NS4B, such as the ability to induce the membranous web replication platform, RNA binding and NTPase activity. In order to maximize antiviral efficacy and prevent the emergence of resistance, novel NS4B inhibitors have been subjected to pharmacological studies. In this review, we discussed current understanding of the structure and function of NS4B, and novel drug discoveries targeting NS4B as anti-hepatitis C virus such as sulfonamide, piperidine, carboxamide, piperazinone and quinoline derivatives within the last three years.
    No preview · Article · Nov 2015 · Current topics in medicinal chemistry
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    ABSTRACT: Hepatitis C virus (HCV) infected up to 3% of global human population. More than 350 thousand die annually due to liver cirrhosis and hepatocellular carcinoma, developed at the late stages of the disease. The typical ways of HCV transmission are: transfusion of contaminated blood and blood products; sharing syringes among intravenous drug users; use of poorly sterilized medical instruments in certain countries with bad sterilization practice. HCV is hard to identify, at early stages the disease is asymptomatic and progresses slowly. HCV RNA genome is highly variable, and thus interferes developing of a vaccine. HCV NS3 protease has received close attention as the promising drug target. Recent approval of Boceprevir and Telaprevir, the first inhibitors of HCV NS3 protease, has let increase effectiveness of anti-HCV therapy. Though these new medicines show drawbacks in drug resistance and genotype coverage, second and third generation of HCV protease inhibitors will overcome them. Computational modelling had an impact role in these discoveries. Involvement of modelling in studies for Hepatitis C (HCV) NS3 protease is considered in this review.
    No preview · Article · Nov 2015 · Current topics in medicinal chemistry
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    ABSTRACT: Hepatitis C virus is one of the major causative pathogens of chronic hepatitis and the second most common cause of hepatocellular cancer. The virally encoded NS5B RNA-dependent RNA polymerase is a vital component of the replicase complex that orchestrates the replication process leading to the production of progeny virus. In recent years, developing novel drugs to target NS5B polymerase has become one of the important strategies for the treatment of chronic hepatitis C infection. This review highlights the structure and scaffold of the non-nucleoside NS5B inhibitors represented in the past five years.
    No preview · Article · Nov 2015 · Current topics in medicinal chemistry

  • No preview · Article · Nov 2015 · Current topics in medicinal chemistry

  • No preview · Article · Oct 2015 · Current topics in medicinal chemistry

  • No preview · Article · Oct 2015 · Current topics in medicinal chemistry