(1R,2R)-Configured ifenprodil (1R,2R)-1c exhibited high selectivity for GluN2B-NMDA receptors over adrenergic, serotonergic, and σ1 receptors. Organic and Medicinal Chemistry Letters was merged with Chemistry Central Journal in 2015, becoming the 'Organic and Medicinal Chemistry' section. 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. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry.The journal also publishes reviews on recent patents. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Mazandaran, Iran View All Browse journals by subject Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. Direct-acting agents, targeting protease and polymerase functionalities, represent a milestone in antiviral therapy. Volume 21 Issue 4 . Osimertinib is a highly potent and selective third-generation epidermal growth factor receptor (EGFR) inhibitor, which provides excellent clinical benefits and is now a standard-of-care therapy for advanced EGFR mutation-positive non-small-cell lung cancer (NSCLC). Med.Chem., ist eine wissenschaftliche Fachzeitschrift des Wissenschaftszweigs medizinische Chemie, die von der American Chemical Society veröffentlicht wird. The linker forms favorable interactions with PCSK9 as evidenced by thermodynamics, structure–activity relationship (SAR), NMR, and molecular dynamics (MD) studies. To address this unmet medical need, we initiated an iterative program focusing on structural optimizations of osimertinib and preclinical characterization, leading to the discovery of a highly potent, selective, and orally efficacious deuterated EGFR-targeting clinical candidate, dosimertinib. It is recommended to all scientists working in this field." This study developed monomeric peptide agonists of glucagon-like peptide 1 receptor (GLP-1R) and neuropeptide Y2 receptor (Y2-R) based on exendin-4 (Ex-4) and PYY3–36. Among them, compound 23a was the most active in vitro, with an IC50 (half-maximal inhibitory concentration) value of 42 nM, showed good liver microsomal stability, and showed no significant inhibition of CYP and hERG. Abstract; Full text; PDF; ABSTRACT Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities. Get article recommendations from ACS based on references in your Mendeley library. Search. Scope . Please note: If you switch to a different device, you may be asked to login again with only your ACS ID. International contributors cover the entire spectrum of new drug research, including methods of synthesis; results of pharmacological, … 67 th of 261 in Pharmacology & Pharmacy. Submit your article Opens in new window Information and templates for authors Search this journal Read the latest articles of European Journal of Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly literature It provides a medium for publication … Due to the evolution and development of antifungal drug resistance, limited efficacy of existing drugs has led to high mortality in patients with serious fungal infections. It is published by the American Chemical Society. 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. These suggest that targeting the activated conformational state of the 5-HT6R with neutral antagonists implicates the protecting properties of astrocytes. 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. Longer manuscripts or full papers may be more suited to the companion journal Bioorganic and Medicinal Chemistry. Find out more about the change.. Until now, the primary focus has been on the use of inert peptide linkers. Experimental, theoretical and applied original research studies in all fields of medicinal and chemistry are welcomed for submission. Bioorganic & Medicinal Chemistry publishes complete accounts of research of outstanding significance and timeliness on all aspects of molecular interactions at the interface of chemistry and biology, together with critical review articles. In consequence, different conformational states can initiate specific signal transduction pathways. We engineered a peptide inhibitor of PCSK9, a target for clinical management of hypercholesterolemia, to demonstrate this concept. Reviewers, Librarians Journal of Medicinal Chemistry, Articles ASAP (Featured Article) Publication Date (Web): November 13, 2020. (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). Please check the relevant section in this Guide for Authors for more details. However, AZ5104, a primary toxic metabolite of osimertinib, has caused unwanted toxicities. 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. Michael Kassiou University of Sydney, Australia. To develop novel antifungal therapeutic strategies, herein a series of carboline fungal histone deacetylase (HDAC) inhibitors were designed and synthesized, which had potent synergistic effects with fluconazole against resistant Candida albicans infection. 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. You have to login with your ACS ID befor you can login with your Mendeley account. On investigating the effect of 31g on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-β-induced hepatic stellate cells (HSCs). In particular, compound D12 showed excellent in vitro and in vivo synergistic antifungal efficacy with fluconazole to treat azole-resistant candidiasis. Here, we report an iterative structure–property optimization toward RAPs capable of inhibiting C. neoformans growth in culture. 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. Perspectives in Medicinal Chemistry (PMC) is an international, open access journal, developed to help medicinal chemists keep apace with the expanding volume of information published in their field.PMC calls upon researchers to summarize observations from numerous original publications as hybrid review-commentaries, although extensive reviews will also be … 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 … 2019 Impact Factor. The Medicinal and Pharmaceutical Chemistry section publishes pioneering research across all aspects of medicinal chemistry and drug discovery science. 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. The Journal of Medicinal Chemistry is a peer-reviewed medical journal covering research in medicinal chemistry. 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. Editorial Board Members. Er dient zum bibliometrischen Vergleich verschiedener Zeitschriften. Preclinical studies revealed that dosimertinib demonstrated robust in vivo antitumor efficacy and favorable PK profiles, but with lower toxicity than osimertinib. Despite structural similarities in 16 to known β-blockers, detailed structure–activity relationship studies described herein have led to the identification of analogues lacking β-adrenergic activity that still maintain the ability to suppress glucagon-induced glucose release from hepatocytes and ameliorate hyperglycemia in diabetic mouse models. The identification of drugs to treat COVID-19 and other coronavirus diseases is an urgent global need, thus different strategies targeting either virus or host cell are still under investigation. 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. Sign in to set up alerts . 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. Editor-in-Chief: Hervé Galons. Ranking and Category. Choose a journal from the journal list. 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. The anticancer effects might be explained by the partial activation and upregulation of PPARγ expression, as indicated by the transactivation assay and western blotting evaluation. Maite Sylla-Iyarreta Veitia (Equipe de chimie moleculaire, Laboratoire de Chimie moleculaire, genie des procedes chimiques et energetiques, EA7341, Conservatoire national des arts et metiers, 2 rue Conte, 75003, Paris, France) 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. Journal of Enzyme Inhibition and Medicinal Chemistry. Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. International Scientific Journal & Country Ranking. Explore journal content Latest issue Articles in press Article collections All issues. Furthermore, (3) in enzymatic assays employing fluorescence, the key parameter is the binding affinity between the fluorophore and the enzyme. Volumes and issues. 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. Read the latest articles of Bioorganic & Medicinal Chemistry at ScienceDirect.com, Elsevier’s leading platform of peer-reviewed scholarly literature Journal of Enzyme Inhibition and Medicinal Chemistry. Here, we show that affinity can be significantly improved by enriching the linker with functional amino acids. "Medicinal Chemistry is an invaluable journal, which contains the latest outstanding developments in medicinal chemistry. Latest Articles . This is a Transformative Journal. Only Open Access Journals Only SciELO Journals Only WoS Journals In addition, we report the first X-ray crystal structures of C. neoformans Hsp90 nucleotide binding domain (NBD), as the apoprotein and in complexes with the non-species-selective Hsp90 inhibitor NVP-AUY922 and three RAPs revealing unique ligand-induced conformational rearrangements, which reaffirm the hypothesis that intrinsic differences in protein flexibility can confer selective inhibition of fungal versus human Hsp90 isoforms. Journal of Enzyme Inhibition and Medicinal Chemistry Journal Impact Quartile: Q2. 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. The Open Medicinal Chemistry Journal is an Open Access online journal, which publishes research articles, reviews, and letters in all areas of Drug Safety. 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. Taken together, compound 23a shows promise as a therapeutic agent for the treatment of obesity and fatty liver diseases. Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. Bioorganic & Medicinal Chemistry publishes complete accounts of research of outstanding significance and timeliness on all aspects of molecular interactions at the interface of chemistry and biology, together with critical review articles. Taken together, fungal HDAC inhibitor D12 offered a promising lead compound for combinational treatment of azole-resistant candidiasis. 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