2019 Impact Factor. Pharmaceuticals, an international, peer-reviewed Open Access journal. Several novel glucose-lowering strategies are currently under clinical investigation, highlighting the need for more robust treatments. The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. 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 ().. Scope . 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. Compared with RGD-VC-CA (3), RGD-SS-CA (2) proved to be superior in in vitro drug release and cytotoxicity tests. It was established in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry and obtained its current name in 1963. Der ursprüngliche Titel war Journal of Medicinal and Pharmaceutical Chemistry und wurde 1963 auf den heutigen Titel verkürzt. Er dient zum bibliometrischen Vergleich verschiedener Zeitschriften. View editorial board. 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. It is recommended to all scientists working in this field." The biologically oriented synthesis yielded several nanomolar inhibitors. Here, we report an iterative structure–property optimization toward RAPs capable of inhibiting C. neoformans growth in culture. Together, these results suggest that 14g is a promising anticancer therapeutic that deserves further investigation. Tryptophan hydroxylase 1 (TPH1) has been recently suggested as a promising therapeutic target for treating obesity and fatty liver disease. Taken together, compound 23a shows promise as a therapeutic agent for the treatment of obesity and fatty liver diseases. 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. Es werden Artikel veröffentlicht, die sich mit molekularen Wechselwirkungen in Rezeptoren, Kanälen, Enzymen, Nukleotiden, Lipiden und Sacchariden der Botanik beschäftigen. Authors' Comments. It provides a medium for publication … Volume 19 Issue 4 . Search. 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. 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. 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. Organic and Medicinal Chemistry Letters was merged with Chemistry Central Journal in 2015, becoming the 'Organic and Medicinal Chemistry' section. 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 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. Explore journal content Latest issue Articles in press Article collections All issues. Advertisement. GluN2B affinity, ion channel inhibitory activity, and selectivity over α, σ, and 5-HT receptors were evaluated. Longer manuscripts or full papers may be more suited to the companion journal Bioorganic and Medicinal Chemistry. The absolute configuration of ifenprodil stereoisomers was determined by X-ray crystal structure analysis of (1R,2S)-1a and (1S,2S)-1d. Each issue contains a series of timely in-depth/mini reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in … Michael Kassiou University of Sydney, Australia. Journal of Enzyme Inhibition and Medicinal Chemistry. Editorial Board Members. 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. 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. 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. 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. Compound 23a inhibited TPH1 in the peripheral tissue with limited BBB penetration. These studies expand upon prior understanding of triazolopyrimidine SAR and enabled the identification of novel analogues that, relative to the existing lead, exhibit improved physicochemical properties, MT-stabilizing activity, and pharmacokinetics. Sign in to set up alerts . 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. We found that the selection standard of a suitable fluorophore is variable depending on the application. Aims & Scope. View aims and scope. Taken together, fungal HDAC inhibitor D12 offered a promising lead compound for combinational treatment of azole-resistant candidiasis. 28 th of 59 in Chemistry, Medicinal. 8.3 CiteScore. Das Journal of Medicinal Chemistry, abgekürzt J. About this journal. Latest Articles . Collectively, these data demonstrate that targeting GLP-1R and Y2-R with chimeric single peptides offers a route to new glucoregulatory treatments that are well-tolerated and have improved weight loss when compared directly to Ex-4. We assembled a library of chromone-derived fluorophores with diverse structure–fluorescence properties, which allowed us to choose the fluorophore pairs with similar structures but differing fluorescence properties and compared the performance of the selected fluorophore pairs in three types of commonly used fluorescence applications. In cell-based assays, neutral antagonists of the 5-HT6R (7e and CPPQ), but not inverse agonists (SB-258585, intepirdine, PZ-1444), displayed glioprotective properties against 6-hydroxydopamine-induced and doxorubicin-induced cytotoxicity. 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. 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. 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). Specifically, 31g significantly inhibited TGF-β-induced migration of HSCs at 0.25 μM in wound-healing assays. 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. 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