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. Explore journal content Latest issue Articles in press Article collections All issues. In high-fat diet-fed mice, 23a reduced body weight gain, body fat, and hepatic lipid accumulation. Consequently, inhibition of the Hsp90 protein folding machinery results in a combinatorial attack on numerous oncogenic pathways. There is a critical unmet need for therapeutics to treat the epidemic of comorbidities associated with obesity and type 2 diabetes, ideally devoid of nausea/emesis. Der Journal Impact, deutsch Impact-Faktor, ist eine errechnete Zahl, deren Höhe den Einfluss einer wissenschaftlichen Fachzeitschrift wiedergibt. You have to login with your ACS ID befor you can login with your Mendeley account. Das Journal of Medicinal Chemistry ist das höchstrangige Publikationsorgan des Wissenschaftszweigs Medizinische Chemie.Der ursprüngliche Titel hieß "Journal of Medicinal and Pharmaceutical Chemistry" und wurde 1963 auf den heutigen Titel verkürzt. Direct-acting agents, targeting protease and polymerase functionalities, represent a milestone in antiviral therapy. About this journal. 4.673 An international and interdisciplinary open access journal, ... Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 36, Issue 1 (2021) Issue In Progress. The journal publishes original research, full-length/mini-review articles and guest edited thematic issues covering recent research and developments in the field. Volumes and issues listings for Medicinal Chemistry Research. Organic and Medicinal Chemistry Letters was merged with Chemistry Central Journal in 2015, becoming the 'Organic and Medicinal Chemistry' section. The Journal of Medicinal Chemistry is a peer-reviewed medical journal covering research in medicinal chemistry. A novel peptide, GEP44, was obtained via in vitro receptor screens, insulin secretion in islets, stability assays, and in vivo rat and shrew studies of glucoregulation, weight loss, nausea, and emesis. Submit an article. The 3C-like (or Main) protease (3CLpro) and the nsp12 RNA-dependent RNA-polymerase (RdRp) are the best characterized SARS-CoV-2 targets and show the highest degree of conservation across coronaviruses fostering the identification of broad-spectrum inhibitors. Analysis of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamide as a JAK1-selective scaffold, and the synthesis of various methyl amide derivatives provided 4-((cis-1-(4-chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide (31g) as a potent JAK1-selective inhibitor. Coronaviruses also possess a papain-like protease, another essential enzyme, still poorly characterized and not equally conserved, limiting the identification of broad-spectrum agents. The editorial board is very professional. Herein, we provide an exhaustive comparative analysis of SARS-CoV-2 proteases and RdRp with respect to other coronavirus homologues. The essential eukaryotic chaperone Hsp90 regulates the form and function of diverse client proteins, many of which govern thermotolerance, virulence, and drug resistance in fungal species. Several novel glucose-lowering strategies are currently under clinical investigation, highlighting the need for more robust treatments. This double peer-reviewed and indexed journal aim to provide a platform for researchers around the world to share their latest findings in all field of Medicinal and Chemistry. Export articles to Mendeley. Archives of Natural and Medicinal Chemistry is an online, open access journal covers various aspects like pharmaceutical chemistry, natural products, organic compounds along with biological products such as biochemistry, molecular biology, pharmacognosy, pharmacology, toxicology setting altogether for safety and efficacy of drugs in treatment of diseases. View aims and scope Submit your article Guide for authors. Studies in tau and Aβ plaque transgenic mouse models demonstrated that brain-penetrant microtubule (MT)-stabilizing compounds, including the 1,2,4-triazolo[1,5-a]pyrimidines, hold promise as candidate treatments for Alzheimer’s disease and related neurodegenerative tauopathies. The biologically oriented synthesis yielded several nanomolar inhibitors. It was established in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry and obtained its current name in 1963. We recently described resorcylate aminopyrazoles (RAPs) as the first class of Hsp90 inhibitors capable of discriminating between fungal (Cryptococcus neoformans, Candida albicans) and human isoforms of Hsp90 in biochemical assays. Librarians & Account Managers. Click here > Special Issue Title: * Email Address: * ... Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Mazandaran, Iran. Additionally, 7e prevented scopolamine-induced learning deficits in the novel object recognition test in rats. Latest Articles . Preclinical studies revealed that dosimertinib demonstrated robust in vivo antitumor efficacy and favorable PK profiles, but with lower toxicity than osimertinib. Herein, we report the discovery of a potent and novel OGA inhibitor, compound 5i, comprising an aminopyrimidine scaffold, identified by virtual screening based on multiple methodologies combining structure-based and ligand-based approaches, followed by sequential optimization with a focus on ligand lipophilicity efficiency. It is published by the American Chemical Society. 5.572 Impact Factor. Submission Checklist You can use this list to carry out a final check of your submission before you send it to the journal for review. 2019 Impact Factor. Please note: If you switch to a different device, you may be asked to login again with only your ACS ID. The Medicinal and Pharmaceutical Chemistry section publishes pioneering research across all aspects of medicinal chemistry and drug discovery science. (1R,2R)-Ifenprodil ((1R,2R)-1c) showed the highest affinity toward GluN2B-NMDA receptors (Ki = 5.8 nM) and high inhibition of ion flux in two-electrode voltage clamp experiments (IC50 = 223 nM). Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Meet Our Editorial Board Member. Compound 23a inhibited TPH1 in the peripheral tissue with limited BBB penetration. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure–activity relationship (SAR) study. Author(s): Paolo Guglielmi Pages: 341-341 (1) Free. Authors' Comments. Medicinal chemistry journal target Researchers, Scientists, and Students who seek to advance the technical knowledge and practical applications related to pharmaceutical chemistry. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments. Here we present the synthesis of new inhibitors of Aurora B kinase, which is an important target for cancer therapy through mitosis regulation. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. Therefore, as a novel prodrug of the coibamide A analogue, conjugate 2 has great potential for further exploration in cancer drug discovery. The CCK-8 assay enabled us to identify a novel compound, 14g, which strongly inhibited HepG2 and A549 cell growth with IC50 values of 0.54 and 0.47 μM, respectively. RSC Medicinal Chemistry is the new name for MedChemComm. Meet Our Editorial Board Member. Editor-in-Chief: Hervé Galons. Es werden Artikel veröffentlicht, die sich mit molekularen Wechselwirkungen in Rezeptoren, Kanälen, Enzymen, Nukleotiden, Lipiden und Sacchariden der Botanik beschäftigen. Michael Kassiou University of Sydney, Australia. Supports open access. Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. The Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action. 28 th of 59 in Chemistry, Medicinal. The Journal of Medicinal Chemistry and Drug Design (JMCDD) (ISSN 2578-9589) presents up-to-date coverage of advanced drug systems and their applications in medicine. It covers a broad range of topics including rational drug design and optimization, target identification and validation, imaging agents, drug delivery and pharmacology of bioactive molecules. Editorial Board Members. It is recommended to all scientists working in this field." As per available reports about 372 journals, 150 Conferences, 83 workshops are presently dedicated exclusively to Medicinal Chemistry and about 344000 articles are being published on the current trends in Medicinal Chemistry.In terms of research annually, USA, India, Japan, Brazil and Canada are some of the leading countries where maximum studies related to proteomics are being carried out. Significant inhibition of Aurora B was achieved by the synthesis of simplified fragments of benzosceptrins and oroidin belonging to the marine pyrrole-2-aminoimidazoles metabolites isolated from sponges. Search. Ranking and Category. Pair your accounts. Med.Chem., ist eine wissenschaftliche Fachzeitschrift des Wissenschaftszweigs medizinische Chemie, die von der American Chemical Society veröffentlicht wird. 67 th of 261 in Pharmacology & Pharmacy. G-protein coupled receptors (GPCRs) exist in an equilibrium of multiple conformational states, including different active states, which depend on the nature of the bound ligand. O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Mechanism studies revealed that the reversion of drug resistance was due to downregulation of the expression of the azole target gene ERG11 and efflux gene CDR1. 4.673 An international and interdisciplinary open access journal, publishing new knowledge and findings on enzyme inhibitors and inhibitory processes, and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents. The European Journal of Medicinal Chemistry publishes studies on all aspects of medicinal chemistry: organic synthesis; biological behavior; pharmacological activity; drug design; QSAR; molecular modeling; drug-receptor interactions; molecular aspects of drug metabolism; prodrug synthesis and drug targeting. Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. There is a critical unmet need for therapeutics to treat the epidemic of comorbidities associated with obesity and type 2 diabetes, ideally devoid of nausea/emesis. "Medicinal Chemistry is an invaluable journal, which contains the latest outstanding developments in medicinal chemistry. Herein, we developed a series of novel TNBG analogues with improved water solubility and antiproliferative activities. Get article recommendations from ACS based on references in your Mendeley library. View aims and scope. Medicinal chemistry and pharmaceutical chemistry are disciplines 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, or bio-active molecules ().. The linker forms favorable interactions with PCSK9 as evidenced by thermodynamics, structure–activity relationship (SAR), NMR, and molecular dynamics (MD) studies. I would highly recommend the journal Current Topics in Medicinal Chemistry to my colleagues." These probe molecules may lead to a new therapeutic approach to treat T2D either as a single agent or in combination therapy. Search. Das Journal of Medicinal Chemistry, abgekürzt J. Moreover, we highlight the most promising inhibitors of these proteins reported so far, including the possible strategies for their further development. Please note: If you switch to a different device, you may be asked to login again with only your ACS ID. You’ve supercharged your research process with ACS and Mendeley! It covers a broad range of topics including rational drug design and optimization, target identification and validation, imaging agents, drug delivery and pharmacology of bioactive molecules. We propose 7e as a probe for further understanding of the functional outcomes of different states of the 5-HT6R. Together, these initial studies support the development of Hsp90β-selective inhibitors as a method for overcoming the detriments associated with pan-inhibition. Article. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation. Scope . Description of the properties and applications of new medicinal products, drug delivery and targeting, multifunctional nanosystems, genomics, proteomics, and metabolonomics of new phramaceutical agents, nanobiotechnology of SiRNA, microRNAs, antibodies … This Viewpoint discusses the discovery, published in this journal, that a highly potent and specific GPR52 antagonist was identified through high-throughput screening and structure–activity relationship study, which diminishes not only mHTT protein levels, but also ameliorates HD-like phenotypes in the animal disease models. To further elucidate the structure–activity relationship (SAR) and to identify potentially improved MT-stabilizing candidates for neurodegenerative disease, a comprehensive set of 68 triazolopyrimidine congeners bearing structural modifications at C6 and/or C7 was designed, synthesized, and evaluated. Authors are now encouraged to submit their paper to Chemistry Central Journal.All articles published in Organic and Medicinal Chemistry Letters during its time with SpringerOpen are archived and fully searchable. Sign in to set up alerts . Meet Our Associate Editorial Board Member . Thank you for your mail. However, use of Hsp90 inhibitors as antifungal therapeutics has been precluded by human host toxicities and suppression of immune responses. Furthermore, the in vitro antiproliferative activity was verified in an in vivo xenograft model in which 14g strongly reduced tumor growth at a dose of 10 mg/kg. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. Tetrazanbigen (TNBG) is a novel sterol isoquinoline derivative with poor water solubility and moderate inhibitory effects on human cancer cell lines via lipoapoptosis induction. We engineered a peptide inhibitor of PCSK9, a target for clinical management of hypercholesterolemia, to demonstrate this concept. Abstract; Full text; PDF; ABSTRACT Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities. (1R,2R)-Configured ifenprodil (1R,2R)-1c exhibited high selectivity for GluN2B-NMDA receptors over adrenergic, serotonergic, and σ1 receptors. The Journal of Medicinal Chemistry is a peer-reviewed medical journal covering research in medicinal chemistry. Notably, (2) in the detection of bioactive species, fluorophores with relatively lower fluorescence quantum yield favor the detection sensitivity. Previously, we have shown that suppressing peroxisome proliferator-activated receptor gamma coactivator 1-alpha activity with a small molecule (SR18292, 16) can reduce glucose release from hepatocytes and ameliorate hyperglycemia in diabetic mouse models. Two iterative rounds of docking of a carefully selected set of natural-product-derived cores led to the discovery of an uncharged macrocyclic inhibitor of the Keap1-Nrf2 protein–protein interaction, a particularly challenging target due to its highly polar binding site. Your Mendeley pairing has expired. Search Log in; Search SpringerLink. Described herein, is a structure-based approach to develop isoform-selective inhibitors of Hsp90β, which induces the degradation of select Hsp90 clients without concomitant induction of Hsp90 levels. Scope . Skip to main content. The Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action. 16 th of 59 in Chemistry & Medicinal. You’ve supercharged your research process with ACS and Mendeley! 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