Results 61 to 70 of about 4,486 (199)

Accessing simply-substituted 4-hydroxytetrahydroisoquinolines via Pomeranz–Fritsch–Bobbitt reaction with non-activated and moderately-activated systems

Beilstein Journal of Organic Chemistry, 2017
Background: 1,2,3,4-Tetrahydroisoquinolines (THIQs) are common motifs in alkaloids and in medicinal chemistry. Synthetic access to THIQs via the Pomeranz–Fritsch–Bobbit (PFB) methodology using mineral acids for deactivated, electron-poor aromatic systems,
Marco Mottinelli, Mathew P. Leese, Barry V. L. Potter   +2 more
doaj   +1 more source

Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase [PDF]

, 2015
Objectives (S)-Leucoxine, isolated from the Colombian Lauraceae tree Rhodostemonodaphne crenaticupula Madriñan, was found to inhibit the growth of Mycobacterium tuberculosis H37Rv. A biomimetic approach for the chemical synthesis of a wide array of 1-
Angell, R, Barrera, DA, Bhakta, S, Cuca, LE, Davies, HM, Evangelopoulos, D, Gershater, MC, Guzman, JD, Hailes, HC, Lamming, ED, Maitra, A, McMahon, E, Mortazavi, PN, Munshi, T, Needham, D, Pesnot, T, Redmond, JM, Ward, JM   +17 more
core   +1 more source

Fusion Molecules Between the STAT5b Inhibitor Stafib‐2‐CR and a Cereblon Ligand

ChemistryOpen, Volume 15, Issue 5, May 2026.
The design and synthesis of fusion molecules between the selective STAT5b inhibitor Stafib‐2‐CR and a ligand of the E3 ubiquitin ligase cereblon is reported. Activity analysis in fluorescence polarization assays and isothermal titration calorimetry indicated that the chosen attachment point for the linker is well‐suited to retain activity of the fusion
Theresa Münzel, Karl Christian Seidenstücker, Christoph Protzel, Angela Berg, Thorsten Berg   +4 more
wiley   +1 more source

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

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  

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

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

A Streamlined Synthesis of Adenosine Vinylsulfonamide Probes for Aminoacyl‐AMP Mimicry in NRPS

ChemBioChem, Volume 27, Issue 7, 14 April 2026.
A concise three‐step synthesis enables access to amino acid‐derived adenosine vinylsulfonamide (AVS) probes under mild conditions. Ba(OH)2‐mediated coupling suppresses epimerization, affording stereochemically defined probes that covalently capture nonribosomal peptide synthetase (NRPS) thioesterification states. LC–MS/MS confirms functional engagement
Naoto Haraguchi, Arisa Suto, Takashi Matsui, Yoshio Kodera, Yoshikazu Tanaka, Ryo Tanifuji, Hiroki Oguri   +6 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

A simple two-step synthesis of 2-(alkylamino)-1-arylethanols, including racemic adrenaline, from aromatic aldehydes via 5-aryloxazolidines [PDF]

, 2013
Benzaldehydes react smoothly with nonstabilized azomethine ylides, generated in situ from sarcosine/formaldehyde or N-(methoxymethyl)-N- (trimethylsilylmethyl)benzylamine, to give 5-aryloxazolidines as intermediates.
Moshkin, V. S., Sosnovskikh, V. Y.
core   +1 more source