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Last update 08 May 2025

Levodopa Methyl Ester Hydrochloride

Last update 08 May 2025

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Translational Medicine

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Small molecule drug

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Drug Highest PhasePendingIND Application

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Structure/Sequence

Molecular FormulaC12H15ClN2O2

InChIKeyXNFNGGQRDXFYMM-PPHPATTJSA-N

CAS Registry7524-52-9

100 Clinical Results associated with Levodopa Methyl Ester Hydrochloride

100 Translational Medicine associated with Levodopa Methyl Ester Hydrochloride

100 Patents (Medical) associated with Levodopa Methyl Ester Hydrochloride

1,091

Literatures (Medical) associated with Levodopa Methyl Ester Hydrochloride

01 Apr 2025·Bioorganic Chemistry

Discovery of novel oleanolic acid glycoside derivatives targeting PTP1B/PI3K/AKT signaling pathway for the treatment of breast cancer

Article

Author: Song, Xiaoping ; Wang, Lina ; Xu, Kefan ; Cai, Panpan ; Fan, Daidi ; Liu, Yao ; Liu, Qingchao ; Liu, Jinqiu

Protein tyrosine phosphatase 1B (PTP1B) has been identified as a key drug target for anti-tumor drug development. Oleanolic acid (OA) has been proved to be an inhibitor of PTP1B, but its poor water solubility, low bioavailability and poor activity in vivo limit its clinical efficacy. In this study, a total of 47 new OA derivatives including heteroatom derivatives, ester derivatives, amino substitution derivatives and Schiff base derivatives were designed and synthesized. Among them, OA-Br-1 had stronger inhibition and selectivity on PTP1B than OA, with IC₅₀ value of 7.08 ± 5.05 μM for PTP1B and 222.28 ± 0.11 μM for TCPTP. In addition, OA-Br-1 significantly inhibited the proliferation and induced apoptosis of breast cancer cells, and in vivo nude mice experiments also showed that OA-Br-1 could inhibit the growth of breast tumors. Then network pharmacology was used to predict the targets of OA-Br-1, and the PPI network map between compound - breast cancer - target was constructed. The results showed that the probability value of PTPN1 ranked first among all predicted targets, which was consistent with the results of enzyme activity experiments in vitro. The enrichment results of KEGG pathway and GO functional annotation analysis showed that the effect of OA-Br-1 on breast cancer was significantly correlated with the PI3K/AKT pathway. Subsequent Western Blot results also proved that OA-Br-1 could significantly inhibit the expression of PTP1B, p-PI3K and p-AKT, indicating that OA-Br-1 played an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway. Collectively, these findings identify OA-Br-1 as a promising PTP1B inhibitor for breast cancer treatment.

25 Mar 2025·Chemistry – A European Journal

Visible‐Light Photoredox Catalytic Direct N‐(Het)Arylation of Lactams

Article

Author: Intini, Niccolò ; Benaglia, Maurizio ; König, Burkhard ; Ghosh, Indrajit ; Fattalini, Marco ; Puglisi, Alessandra ; Boselli, Monica Fiorenza

AbstractLactam rings are essential structural motifs in organic chemistry, widely present in natural products and clinically important drugs, such as antibiotics and antiepileptics. Existing methods for synthesizing N‐functionalized lactams often require harsh conditions, toxic reagents, or complex catalytic systems. Here, we report a mild and efficient photochemical approach for generating N‐centered radicals, enabling straightforward N‐heteroarylation of lactams. This versatile method enables the synthesis of a range of N‐(het)arylated lactams and is effective even in aqueous media, facilitating the functionalization of biomolecules. Furthermore, the photochemical reaction is easily scalable under continuous flow conditions, making it highly suitable for large‐scale applications.

24 Mar 2025·Angewandte Chemie International Edition

Enzymatic Cascades for Stereoselective and Regioselective Amide Bond Assembly

Article

Author: Angiolini, Stuart M. ; Shepherd, Sarah A. ; Yates, Luke R. L. ; Cuesta‐Hoyos, Sebastian ; Micklefield, Jason ; Bering, Luis ; Torri, Daniele ; Xu, Guangcai

AbstractAmide bond formation is fundamental in nature and is widely used in the synthesis of pharmaceuticals and other valuable products. Current methods for amide synthesis are often step and atom inefficient, requiring the use of protecting groups, deleterious reagents and organic solvents that create significant waste. The development of cleaner and more efficient catalytic methods for amide synthesis remains an urgent unmet need. Herein, we present novel biocatalytic cascade reactions for synthesising various amides under mild aqueous conditions from readily available organic nitriles combining nitrile hydrolysing enzymes and amide bond synthetase enzymes. These cooperative biocatalytic cascades enable kinetic resolution of racemic nitriles and provide a highly enantioselective biocatalytic extension of the Strecker reaction. The regioselective non‐directed C−H bond amidation of simple arenes was demonstrated through the incorporation of photoredox catalysis to the front end of the cascade. C−H bond amidation of simple aromatic precursors was also achieved via a CO2 fixation cascade combining enzymatic carboxylation and amide bond synthesis in one‐pot.

100 Deals associated with Levodopa Methyl Ester Hydrochloride

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Levodopa Methyl Ester Hydrochloride

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