Results 41 to 50 of about 1,536 (171)

Herstellung diastereomerenreiner l- oder u-konfigurierter 1-hydroxybenzylierter Tetrahydroisochinolin-Vorläufer für Aporphin-, Protoberberin-, Quettamin- und Phthalid-Alkaloide (Stereoselektive Synthese von (±)-Ushinsunin und (±)-Oliverolin)

CHIMIA, 1985
6,7-Dialkoxy-1-bromomagnesio-2-pivaloyl-tetrahydroisoquinolines (THIQ), prepared as previously described for the unsubstituted reagent, are added to bromo-, methoxy-, and ethoxycarbonyl-substituted benzaldehydes to give 1-hydroxybenzylated THIQs of u ...
Dieter Seebach, Isabelle M.P. Huber
doaj   +1 more source

Retro‐Hetero‐Michael Addition Strategies in Organic Synthesis

European Journal of Organic Chemistry, EarlyView.
In this review, synthetic approaches to carbo‐ and heterocyclic compounds, including natural products, published in the last 15 years (2011–2025) which have either relied upon or included a retro‐hetero‐Michael addition step at any stage are discussed.
Dina Scarpi, Ernesto G. Occhiato
wiley   +1 more source

Synthesis and antimicrobial activity of chiral quaternary N-spiro ammonium bromides with 3',4'-dihydro-1'H-spiro[isoindoline-2,2'-isoquinoline] skeleton

Drug Design, Development and Therapy, 2017
Krzysztof Bielawski,1 Katarzyna Leszczyńska,2 Zbigniew Kałuża,3 Anna Bielawska,4 Olga Michalak,3 Tamara Daniluk,2 Olga Staszewska-Krajewska,3 Anna Czajkowska,4 Natalia Pawłowska,1 Agnieszka Gornowicz4 1Department of Synthesis and Technology of Drugs ...
Bielawski K, Leszczyńska K, Kałuża Z, Bielawska A, Michalak O, Daniluk T, Staszewska-Krajewska O, Czajkowska A, Pawłowska N, Gornowicz A   +9 more
doaj  

Design, synthesis and activity evaluation of tetrahydroisoquinoline‐based programmed cell death ligand 1 inhibitors

Smart Molecules, EarlyView.
Based on a 3D‐quantitative structure‐activity relationship pharmacophore model, structural optimization of Y6 yielded Y7f. Mechanistic studies revealed that Y7f acted as a programmed death receptor 1/programmed cell death ligand 1 (PD‐L1) interaction inhibitor by inducing PD‐L1 dimerization. Y7f restored T‐cell function.
Menglin Yu, Sen Cai, Yanyan Pan, Heshuang Wang, Fengwu Zhang, Aiyu Ma, Shixuan Lv, Xiuhan Guo, Shisheng Wang, Qiling Song, Chunyan Ma, Shuai Wang, Li Zhang, Jian Wang, Qingwei Meng, Yueqing Li   +15 more
wiley   +1 more source

Synthesis of Some Novel 11b-Substituted Pyrimido[6,1-a]-isoquinoline Derivatives

Molecules, 2004
A series of novel 11b-substituted 1,6,7,11b-tetrahydropyrimido[6,1-a]- isoquinoline-2,4-diones and 4-thioxo-1,3,4,6,7,11b-hexahydropyrimido[6,1-a]isoquinolin-2- ones were synthesized, utilizing two alternative strategies for ring closure of ...
Atanas P. Venkov, Iliyan I. Ivanov, Plamen A. Angelov   +2 more
doaj   +1 more source

Nomenclature on Immune‐Mediated Drug Reactions: An EAACI Position Paper

Allergy, EarlyView.
ABSTRACT Over the past several decades, there have been significant advances in our understanding of both immunological and pharmacological mechanisms of adverse drug reactions (ADRs). Immune‐mediated drug reactions (IMDRs) represent a small proportion of ADRs and are caused by a pathological activation of the immune system or inflammatory pathways ...
Maria J. Torres, Cristobalina Mayorga, Elizabeth J. Phillips, Adriana Ariza, Annick Barbaud, Patrizia Bonadonna, Mariana Castells, Gülfem Çelik, Knut Brockow, Lene H. Garvey, Inmaculada Doña, Jean C. Caubet, Francesca Mori, Jason Trubiano, Giorgia Marta, Antonino Romano, Ingrid Terreehorst, Asli Gelincik, Philip H. Li, Vito Sabato   +19 more
wiley   +1 more source

Engineering a norcoclaurine synthase for one-step synthesis of (S)-1-aryl-tetrahydroisoquinolines

Bioresources and Bioprocessing, 2023
Tetrahydroisoquinoline alkaloids (THIQAs) are ubiquitous compounds with important pharmaceutical and biological activity. Their key N-heterocyclic structural motifs are synthesised via Pictet–Spengler (P–S) reaction by norcoclaurine synthases (NCS) in ...
Man Zhang, Zheng-Yu Huang, Ying Su, Fei-Fei Chen, Qi Chen, Jian-He Xu, Gao-Wei Zheng   +6 more
doaj   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Tetrahydroisoquinolines as novel histone deacetylase inhibitors for treatment of cancer

Acta Pharmaceutica Sinica B, 2016
Histone acetylation is a critical process in the regulation of chromatin structure and gene expression. Histone deacetylases (HDACs) remove the acetyl group, leading to chromatin condensation and transcriptional repression. HDAC inhibitors are considered
Danqi Chen, Aijun Shen, Guanghua Fang, Hongchun Liu, Minmin Zhang, Shuai Tang, Bing Xiong, Lanping Ma, Meiyu Geng, Jingkang Shen   +9 more
doaj   +1 more source

Number and Position of Methoxy Substituents Govern Photophysics and Visible‐Light Photocatalysis in Earth‐Abundant Cu(I) Complexes

ChemSusChem, Volume 19, Issue 16, 27 August 2026.
The number and position of methoxy substituents provide a versatile molecular toolbox for tuning the photophysics and visible‐light photocatalytic performance of heteroleptic Cu(I) photosensitizers. Earth‐abundant Cu(I) photosensitizers are promising systems for visible‐light‐driven photocatalysis, but further design guidelines are required to relate ...
Kurt J. Haseloff, Max Wolf, Katharina Rediger, Christian Kleeberg, Maria Wächtler, Stefanie Tschierlei, Michael Karnahl   +6 more
wiley   +1 more source