Current Medicinal Chemistry Journal Impact Factor & Information

Publisher: Bentham Science Publishers

Journal description

Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each bi-weekly issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

Current impact factor: 3.85

Impact Factor Rankings

2015 Impact Factor Available summer 2016
2014 Impact Factor 3.853
2013 Impact Factor 3.715
2012 Impact Factor 4.07
2011 Impact Factor 4.859
2010 Impact Factor 4.63
2009 Impact Factor 4.708
2008 Impact Factor 4.823
2007 Impact Factor 4.944
2006 Impact Factor 5.207
2005 Impact Factor 4.904
2004 Impact Factor 4.382
2003 Impact Factor 4.409
2002 Impact Factor 4.966
2001 Impact Factor 5.76
2000 Impact Factor 4.909
1999 Impact Factor 3
1998 Impact Factor 1.522
1997 Impact Factor 2.269

Impact factor over time

Impact factor

Additional details

5-year impact 4.12
Cited half-life 5.80
Immediacy index 0.85
Eigenfactor 0.03
Article influence 1.00
Website Current Medicinal Chemistry website
Other titles Current medicinal chemistry (Online)
ISSN 1875-533X
OCLC 55201153
Material type Document, Periodical, Internet resource
Document type Internet Resource, Computer File, Journal / Magazine / Newspaper

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

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: Peptidyl arginine deiminases (PADs) are a small group of isozymes that convert Arg residues on the surface of proteins into citrulline residues, typically as a part of posttranslational processing. PADs are present in most of the tissues, and the isozyme distribution is tissue-specific. In the past 15 years, it is becoming apparent that PADs are either upregulated or their catalytic activity is enhanced in certain disease conditions, including neurological diseases. In particular, hypercitrullinated proteins and elevated PAD activities are discovered in neurodegenerative conditions such as multiple sclerosis, Alzheimer's disease etc. This review article reviews the status of PAD enzymes as targets in neurodegenerative conditions, and briefly outlines the efforts in medicinal chemistry to identify PAD inhibitors for the treatment of various neurodegenerative conditions.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: The Amaryllidaceae occupies a privileged status amongst medicinal plants in having delivered the Alzheimer‟s drug galanthamine to the clinical market. Following its resounding success, there have been several positive indicators for the emergence of an anticancer drug from the family due to the potent antiproliferative activities manifested by several of its alkaloid constituents. Of these, the phenanthridones such as pancratistatin hold most promise as potential chemotherapeutics having succumbed to various phases of clinical trials. Other cytotoxic targets of the Amaryllidaceae are to be found within the lycorane and crinane groups, as exemplified by crinine and lycorine. Although the molecular targets of these alkaloids still remain elusive, much effort has gone into understanding their mode of action in cancer cells. Recent findings have shown that the apoptotic pathway may be a key factor in cancer cell death instigated by Amaryllidaceae alkaloids. As such, this review seeks to: (a) examine the apoptotic effects of Amaryllidaceae alkaloids in cancer cells; (b) explore the molecular basis to these effects; and
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: The PDE4 enzyme has been proven to be a versatile drug target for therapeutics to treat diverse disease conditions such as asthma, COPD, diabetes, Huntington's disease, and various other inflammatory disorders. The treatment of COPD is the most studied utility for PDE4 inhibitors due to their ability to inhibit inflammatory cell responses. Roflumilast is the only approved drug belonging to this class to treat COPD and has shown significant results in the treatment of asthmatic patients. This perspective highlights the pharmacological details of roflumilast and cilomilast. Moreover, efforts have been made to justify the superiority of roflumilast over cilomilast by detailed comparison of their pharmacological, pharmacokinetic, pharmacodynamic properties and structural features. Several other molecules, with promising PDE4 inhibitory activity have also been highlighted. Commonly associated side effects with this class of compounds, their management, and future direction towards the development of PDE4 inhibitors with improved therapeutic index is the focus of this perspective. More emphasis has been given towards the future development strategies to achieve better risk to limit the side effects such as emesis and to achieve better benefit to risk ratio.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: Familial Mediterranean Fever (FMF) is rare autosomal recessive autoinflammatory disorder involving the innate immunity and affecting almost exclusively populations with Mediterranean origin. Clinical features include recurrent episodes of fever, leukocitosis, serositis (peritonitis or pleuritis, arthritis), myalgia or erysipelas-like skin lesions, lasting 12-72 hrs. The MEFV gene mutations on chromosome 16p13.3 encodes the abnormal pyrin (marenostrin), a protein expressed in granulocytes, monocytes, serosal and synovial fibroblasts and involved in the activation of caspase-1 and the processing and release of active pro-inflammatory IL-1β. Since the first report in 1972, maintenance therapy with colchicine, a tricyclic neutral alkaloid, remains the mainstay of treatment in symptomatic FMF patients since it reduces the disease activity and prevents the development of secondary amyloidosis and renal damage. Adjunctive symptomatic therapy to colchicine includes nonsteroideal antinflammatory drugs and corticosteroids. In a small group of colchicine-intolerant or colchicine-resistant FMF patients, alternative treatments must be considered. Evolving experiences have focussed on the potential effectiveness of biologic agents working as TNF-α inhibitors (etanercept, infliximab), IL-1 trap (Rilonacept), IL-1 inhibitors (Anakinra, Canakinumab) and IL-6 receptor antibody (Tocilizumab). Interferon-α and thalidomide have also been employed in FMF patients. Still, clinical trials are mainly uncontrolled and restricted to few cases, thus requiring definitive conclusions. Old, and new treatments are discussed in the rare FMF disease, with the concept that any ideal treatment has to stand the test of time.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: Trichothecenes are sesquiterpenoid metabolites produced by fungi and species of the plant genus Baccharis, family Asteraceae. They comprise a tricyclic core with an epoxide at C-12 and C-13 and can be grouped into non-macrocyclic and macrocyclic compounds. While many of these compounds are of concern in agriculture, the macrocyclic metabolites have been evaluated as antiviral, anti-cancer, antimalarial and antifungal compounds. Some known cytotoxic responses on eukaryotic cells include inhibition of protein, DNA and RNA syntheses, interference with mitochondrial function, effects on cell division and membranes. These targets however have been elucidated essentially employing non-macrocyclic trichothecenes and only one or two closely related macrocyclic compounds. For several macrocyclic trichothecenes high selectivity against fungal species and against cancer cell lines have been reported suggesting that the macrocycle and its stereochemistry are of crucial importance regarding biological activity and selectivity. This review is focused on compounds belonging to the macrocyclic type, where a cyclic diester or triester ring binds to the trichothecane moiety at C-4 and C-15 leading to natural products belonging to the groups of satratoxins, verrucarins, roridins, myrotoxins and baccharinoids. Their biological activities, cytotoxic mechanisms and structure-activity relationships (SAR) are discussed. From the reported data it becomes evident that even small changes in the molecules can lead to pronounced effects on biological activity or selectivity against cancer cells lines. Understanding the underlying mechanisms may help to design highly specific drugs for cancer therapy.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: Flavonoids are natural plant-derived polyphenolic compounds with extensive biological properties particularly in the cardiovascular system, including antiatherogenic, antioxidant, vasodilator, antihypertensive, and antiplatelet properties. These biological properties have been evaluated in several experimental and clinical studies. In addition, extensive reviews have discussed the antiatherogenic effect of these polyphenols. However, limited studies have investigated the potential therapeutic vasodilator effects of these compounds. This review brings together some recent studies, to establish the different signaling pathways involved in the molecular mechanisms that underlie the vasodilator effect promoted by flavonoids.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: TB drug development pipeline represents varied structural classes of molecules. Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR. They act by inhibiting translation at the initiation phase of protein synthesis. Linezolid was the first oxazolidinone to reach the market in the year 2000 for the treatment of methicillin-resistant staphylococcal and vancomycin-resistant enterococcal infections. Oxazolidinones have shown very good anti-mycobacterial activities. Several oxazolidinones are currently in development for their possible use in TB therapy. Oxazolidinones are classified on the basis of C-ring modifications. DuP-721 was the first oxazolidinone having good anti-TB activity. Linezolid, sutezolid and AZD5489 are in clinical development. Several other C-ring modifications have shown promising results. The usefulness of these oxazolidinones in the drug resistant TB is already established. Toxicity, especially myelosuppression, has been an important limiting factor for their development.
    Current Medicinal Chemistry 11/2015; 23(999). DOI:10.2174/0929867323666151106125759
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    ABSTRACT: Nasopharyngeal carcinoma (NPC) is a cancer of the nasopharyngeal epithelium with distinct geographical, ethnic and racial distribution. Several genetic, ethnic and environmental risk factors, have been implicated in nasopharyngeal pathogenesis and of significance, is the Epstein - Barr virus (EBV)-latent infection observed in most patients. Patients with NPC are typically diagnosed only in advanced stages due to non-specific symptoms, and hence, they respond poorly to therapy. Currently, low survival rates, severe complications, tumour metastasis and recurrence following chemo-radiotherapy, delineate the need for better therapeutic options to combat the disease. Recent studies have shown that epigenetic mechanisms such as DNA methylation, histone modifications and microRNAs, which are altered in the EBV genome as well as in the host cells, which may underlie the initiation and progression of NPC. Histone acetylation and deacetylation which are mediated by enzymes, namely histone acetyl transferases (HATs) and histone deacetylases (HDACs), are known to regulate gene expression and several cellular processes. HDACs are also involved in maintaining EBV latent cycle and thus, HDAC inhibitors (HDACi) are potent inducers of EBV reactivation, which is critical for the expression of the lytic proteins, thereby providing novel targets for therapy, as well as mediate enhanced killing of cancer cells, when used alone or along with additional anti-cancer agents in EBV associated malignancies. Recently, three FDA- approved HDACi have been used for the treatment of T-cell lymphoma, while several others are in clinical trials, making histone modifications excellent candidates for targeted therapy. In this review, we summarize the epigenetic mechanisms altered in NPC, with the focus on histone modifications for targeted therapy.
    Current Medicinal Chemistry 11/2015; 23(999). DOI:10.2174/0929867323666151106125631
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    ABSTRACT: T helper (Th) cells belong to the adaptive immune system and provide an effective and antigen-specific means of host protection. Th17 cells are a subset of Th cells, characterized by the production of the inflammatory cytokines interleukin (IL)-17A (IL-17A) and IL-17F, which bind to a receptor complex comprised of IL-17RA and IL-17RC subunits. Th17 cells combat extracellular and fungal infections, but have been implicated in autoimmune diseases. In many autoimmune conditions, the dysregulated immune response involves several parts of the immune system, including autoantibodies, B and T cells. Targeted biological therapies are appealing, as they may prevent unwanted side effects in patients. There is evolving evidence that Th17 cells are important in the kidney, mediating injury in response to vascular or chemical insults to the renal tubules, and in autoimmune diseases of the glomerulus, either through a specific attack on the glomerular basement membrane or as part of a generalized systemic inflammatory disease. Therapies targeting IL-17A, IL-12p40 and IL-17RA are being explored in clinical trials or are being utilized in clinical practice for the treatment of other IL-17 mediated diseases, such as psoriasis. This review explores the current evidence that IL-17A and Th17 cells may be pathogenic in immune kidney disease, including anti-glomerular basement membrane disease, anti-neutrophil cytoplasmic antibody associated vasculitis and lupus nephritis, as well as in acute kidney injury. It will discuss the place that biological agents against IL-17A, IL-12p40 and IL-17RA may have in the treatment of these conditions.
    Current Medicinal Chemistry 11/2015;
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    ABSTRACT: Ion channel dysfunction has been identified as a contributor to symptom development and neurodegeneration in multiple sclerosis (MS). The molecular insights have been translated into new lines of research, with ion channel modulation now representing a therapeutic approach in MS. Studies of Na+ channel function have demonstrated pathological blockade of Na+ channels during an acute inflammatory attack. Relapses are typically associated with subsequent alterations in Na+ channel expression and structure. However, these compensatory changes may also be deleterious. Specifically, increased Na+ channel expression may contribute to neuronal energy insufficiency and a cascade of events that may ultimately lead to neurodegeneration and apoptosis. Pharmacological blockade of Na+ channels in animal models of MS demonstrated encouraging results, although mixed results were obtained in subsequent clinical trials in MS patient cohorts. The process involved in demyelination, a characteristic event in MS pathology, may also induce complex structural changes mediated by K+ channels that may in turn hinder neural transmission. From a therapeutic perspective, the potent K+ channel blocker, 4-aminopyridine (4-AP), has demonstrated neurophysiological and functional improvements in animal models of demyelination. Clinical translation of these results was recently achieved with the advent of Fampridine PR, a modified release form of 4-AP, with phase III clinical trials that demonstrated improvement in neurological symptoms including fatigue, walking speed and strength in MS patients.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029104452
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    ABSTRACT: Passage into the brain has always been a major challenge for medicine in order to treat malfunctions of the central nervous system (CNS). The blood-brain-barrier (BBB) is a physical obstacle that controls the entrance of substances -including pharmaceuticals- into the brain. The application of nanotechnology in medicine, namely nanomedicine, is rapidly evolving and opens new prospects for brain imaging and drug delivery into the brain. Nanomedicine when combined with nuclear medicine can offer new, promising and innovative means towards this direction through radiolabeled nanoparticles. Nanoparticles radiolabeled with β--, γ- or β+-emitters can cross the BBB and play major role in CNS imaging and/or drug delivery.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029105302
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    ABSTRACT: Curcumin (1) is a secondary metabolite of turmeric, derived from Curcuma longa L.. and was shown to have many biological activities. One of the most interesting properties of curcumin (1) is the antitumour activity allied with the ability to act as a multidrug resistance (MDR) modulator. Several curcumin derivatives have been synthesized with the purpose of discovering more information about the mechanisms of action, to establish structure-activity relationships (SAR), and to overcome pharmacokinetic problems. Over the past few decades, more potent and more stable curcumin derivatives have emerged with potential as drug candidates. Some important SAR studies pointed out that the unstable α,β-unsaturated diketone linker present in curcumin (1) may not be necessary for the antitumour activity; generally, shorter linkers result in more potent compounds than curcumin (1); the type of substituents and their substitution pattern are crucial regarding the biological activities of interest. Overall, the structure of curcumin (1) may represent an important basis for the development of more effective therapeutic agents, particularly in chemotherapy, as reflected by ongoing clinical trials. This article aims to review the synthesis and biological activities of curcumin (1) and derivatives, highlighting the MDR modulation properties of curcumin (1), since these effects makes this natural product a promising lead compound for the development of new anticancer drugs.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029104611
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    ABSTRACT: Few selective cyclooxygenase-1 (COX-1) inhibitors have been described up to now, although recent studies underlined the involvement of COX-1 in the carcinogenesis, pathogenesis of neuroinflammation, cardiovascular diseases and pain. Among the known COX-1 inhibitors none proved to be a good drug candidate, with the exception of mofezolac, that is clinically used as an analgesic drug. New selective inhibitors were very often discovered as a minor achievement during SAR investigations to discover selective COX-2 inhibitors (COXIBs). After a recognition of the new COX-1 inhibitors synthesized in the last five years, it was attempted to draw, for each chemical class, a structure which might highlight the determinant molecular features able to switch the selectivity towards the COX-1 isoform. Overall, this review could constitute a tool to a better design of novel selective COX-1 inhibitors, to be used in a disease theranostic approach targeting COX-1.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029104717
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    ABSTRACT: Choline is a quaternary ammonium salt, and being an essential component of different membrane phospholipids (PLs) contributes to the structural integrity of cell membranes. Choline-containing phospholipids (CCPLs) include phosphatidylcholine (PC), sphingomyelin (SM), and choline alphoscerate (GPC). PC is the major phospholipid in most eukaryotic cells. It is involved in SM synthesis, choline/choline metabolite re-generation, and fatty acid/GPC formation. This paper has reviewed chemical, biological and therapeutic features of CCPLs by analyzing: a) effects of exogenous CCPLs, b) influence of GPC treatment on brain cholinergic neurotransmission, and c) neuroprotective effects of GPC alone or in association with acetylcholinesterase inhibitors in animal models of brain vascular injury, d) synthesis of the choline analogs, containing a short alkyl chain instead of a methyl group. Cytidine-diphosphocholine and GPC, protect cell membranes and could be helpful in the sequel of cerebrovascular accident treatment. Moreover, cellular membrane breakdown is suggested as a feature of neurodegeneration both in acute (stroke) and in chronic (Alzheimer and vascular dementia) brain disorders. Published data were focused to a larger extent on the biosynthesis, relevant role in cell life, and crucial involvement of CCPLs in cholinergic neurotransmission. The possibility of their use in the treatment of cerebrovascular and neurodegenerative disorders is suggested by published clinical studies. In line with these potential practical applications in pharmacotherapy, the need of further research in the field of the synthesis of new choline derivatives with possible activity in nervous system diseases characterized by cholinergic impairment is discussed.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029104152
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    ABSTRACT: The production of superoxide anion radical (O2•-) is essential for the life of aerobic organisms. This free radical acts as a signaling molecule, regulating numerous biological processes including apoptosis, aging, and senescence. Nevertheless, when overproduction of O2•- occurs and/or antioxidant defences are deficient, oxidative stress may develop, damaging important biomolecules and altering their physiological function. These effects have been associated to the development of several diseases. Scavenging of O2•- has been used as a hallmark to test the antioxidant capacity of several types of compounds in cellular and non-cellular systems. However, despite the pathophysiological importance of O2•-, the information about its endogenous and/or chemical generation and detection is dispersed and there are no reports that concisely cover the information in an integrated form. This gap can explain the limitations attributed to the currently used systems, namely in what concerns the selectivity, specificity and validation. This review attempts to provide a critical assessment of the available O2•- generating and detection, both in endogenous and chemical systems, scrutinizing its advantages and limitations in order to facilitate the choice and implementation of the O2•- generator and/or detection method that better fits the researchers' objectives.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151029104311
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    ABSTRACT: Hypoxia in tumor cells is characterized by a lack of oxygen resulting from reduced blood supply to the surrounding tissue, and is a common characteristic of solid tumors as a consequence of rapid cell growth. Hypoxia in tumors is a predictor of both resistance to chemotherapy and of a metastatic/aggressive form of cancer, and as a result, development of cancer therapies which target hypoxia is of vital importance. One such targeting strategy is the development of hypoxia-activated prodrugs (HAP) which can preferentially release chemotherapeutic agents within hypoxic tumor regions. This targeting strategy is accomplished by attaching a hypoxia activated trigger to a chemotherapeutic agent and under oxygen-poor conditions, the agent (effector) is released into the tumor, while remaining intact in normal tissue, and leaving non-hypoxic cells undamaged. Overall, this strategy can achieve an increased therapeutic benefit over conventional small molecule chemotherapeutic treatments by concentrating the drugs within hypoxic tumor environments, while simultaneously reducing the side-effects and toxicity issues that surround the systemic distribution of traditional drugs on normoxic cells. In this review, we will describe the factors that should be considered when designing an effective HAP, such as the mechanism of prodrug action, the elements that influence the rational design of HAP (i.e. reduction potential), and the activating enzymes of HAP. As part of this description, we will utilize select examples from the literature to reinforce these factors, and make a case for the intelligent design of new HAPs, leading to the development of novel hypoxia targeting chemotherapeutic agents.
    Current Medicinal Chemistry 10/2015; 22(999). DOI:10.2174/0929867322666151021111016
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    ABSTRACT: Chondroitin sulfate (CS) is a glycosaminoglycan (GAG) composed of alternating N-acetyl galactosamine and glucuronic acid units within disaccharide building blocks. CS is a key functional component in proteoglycans of cartilaginous tissues. Owing to its numerous biological roles, CS is widely explored in the pharmaceutical market as nutraceutical ingredient commonly utilized in fights against arthritis, osteoarthrosis, and sometimes osteoporosis. Mammalian tissues like shark cartilage and bovine trachea are common sources for CS extraction. Nonetheless, a new CS type has been introduced and investigated in the last few decades in what regards its medical potentials. It is named fucosylated chondroitin sulfate (FucCS). This less common CS type is isolated exclusively from the body wall of sea cucumbers. The presence of the fucosyl branching units in the holothurian FucCS gives to this unique GAG, therapeutic properties in various pathophysiological systems which are inexistent in the mammalian-derived CS explored in the market. Examples of these systems are coagulation, thrombosis, hemodialysis, atherosclerosis, cellular growth, angiogenesis, fibrosis, tumor growth, inflammation, viral and protozoan infections, hyperglycemia and diabetes-related pathological events and tissue damage. This report aims at describing the medical benefits gained upon fucosylation of CS. Clinical prospects of these medical benefits are also discussed herein.
    Current Medicinal Chemistry 10/2015; 22(999):1-1. DOI:10.2174/0929867322666151020101335
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    ABSTRACT: Colchicine has recently gained considerable attention in the field of cardiovascular research, after a number of studies showed that it may be of use in several settings of cardiovascular disease, including chronic coronary artery disease and following stent implantation. Its unique anti-inflammatory mechanism of action makes it safe to use in patients with cardiovascular disease, unlike most - if not all - currently available anti-inflammatory agents. While its prophylactic and therapeutic value is well-established in certain conditions involving an acute inflammatory response, e.g. pericarditis, in other conditions, including coronary artery disease and heart failure, which are associated with a chronic low-grade inflammatory state, the evidence regarding its potential use remains sparse. In this concise review, we present key features of this drug and the rationale for colchicine therapy, in the context of acute and chronic coronary artery disease, as well as in ischemic heart failure and critically examine the evidence concerning a possible future role of colchicine treatment in these conditions.
    Current Medicinal Chemistry 10/2015;
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    ABSTRACT: Human American trypanosomiasis, commonly called Chagas disease, is one of the most neglected illnesses in the world and remains one of the most prevalent chronic infectious diseases of Latin America with thousands of new cases every year. The only treatments available have been introduced five decades ago. They have serious, undesirable side effects and disputed benefits in the chronic stage of the disease - a characteristic and debilitating cardiomyopathy and/or megavisceras. Several laboratories have therefore focused their efforts in finding better drugs. Although recent years have brought new clinical trials, these are few and lack diversity in terms of drug mechanism of action, thus resulting in a weak drug discovery pipeline. This fragility has been recently exposed by the failure of two candidates; posaconazole and E1224, to sterilely cure patients in phase 2 clinical trials. Such setbacks highlight the need for continuous, novel and high quality drug discovery and development efforts to discover better and safer treatments. In this article we will review past and current findings on drug discovery for Trypanosoma cruzi made by academic research groups, industry and other research organizations over the last half century. We also analyze the current research landscape that is now better placed than ever to deliver alternative treatments for Chagas disease in the near future.
    Current Medicinal Chemistry 10/2015;