Results 11 to 20 of about 10,671 (149)

2-Phenylquinolines Exhibit Anti-Severe Acute Respiratory Syndrome Coronavirus-2 Activity Through the Nonstructural Protein 13 Helicase Inhibition. [PDF]

ChemMedChem
A SAR study led to the identification of new 2‐phenylquinoline‐based derivatives that exhibit anti‐Severe Acute Respiratory Syndrome Coronavirus‐2 (SARS‐CoV‐2) activity by acting as ATP‐competitive inhibitors of nonstructural protein 13 (nsp13) helicase.
Cernicchi G, Nizi MG, Emmolo R, Persoons L, Laporte M, Jochmans D, Romeo I, Pepe G, Milite C, Campiglia P, Spezzini J, Martelli A, Brogi S, Esposito F, Felicetti T, Massari S, Manfroni G, Sabatini S, Sbardella G, Alcaro S, Neyts J, Corona A, Tramontano E, De Jonghe S, Tabarrini O.   +24 more
europepmc   +2 more sources

A Streamlined Synthesis of Adenosine Vinylsulfonamide Probes for Aminoacyl-AMP Mimicry in NRPS. [PDF]

Chembiochem
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
Haraguchi N, Suto A, Matsui T, Kodera Y, Tanaka Y, Tanifuji R, Oguri H.   +6 more
europepmc   +2 more sources

Transaminase and Norcoclaurine Synthase One-Pot Cascades Towards (1S)-Tetrahydroisoquinolines. [PDF]

Chembiochem
A TAm‐NCS cascade towards THIQs has been established, starting from amines with the in situ production of aldehydes. The cascade was used with a variety of nonfunctionalized and functionalized amines, and reaction conditions modified to enhance formation of the desired cross‐products.
Zhao J, Ni Y, Wang Y, Ward JM, Jeffries JWE, Hailes HC.   +5 more
europepmc   +2 more sources

Crystal structure of (1′S,2′S,3S)-1′-benzoyl-2′-(4-methoxyphenyl)-1-methyl-2′,5′,6′,10b′-tetrahydro-1′H-spiro[indoline-3,3′-pyrrolo[2,1-a]isoquinolin]-2-one

Acta Crystallographica Section E: Crystallographic Communications, 2020
In the title spiro compound, C34H30N2O3, the central pyrrolidine ring is fused with the tetrahydroisoquinoline ring, both having distorted envelope conformations, with the flap atoms being C and N, respectively. The methoxyphenyl group is attached to the
Janet Priyavathani Selvaraj, Stella Mary, Jyoti Boruah Dhruba, Birkumar Singh Huidrom, Yuvaraj Panneerselvam, Kannan Piskala Subburaman   +5 more
doaj   +1 more source

Synthesis of new substituted 7,12-dihydro-6,12-methanodibenzo[c,f]azocine-5-carboxylic acids containing a tetracyclic tetrahydroisoquinoline core structure

Beilstein Journal of Organic Chemistry, 2021
A convenient and simple protocol has been developed for the synthesis of a series of new tetracyclic tetrahydroisoquinoline derivatives, 7,12-dihydro-6,12-methanodibenzo[c,f]-azocine-5-carboxylic acids by three component Petasis reaction with the use of ...
Agnieszka Grajewska, Maria Chrzanowska, Wiktoria Adamska   +2 more
doaj   +1 more source

Fusion Molecules Between the STAT5b Inhibitor Stafib-2-CR and a Cereblon Ligand. [PDF]

ChemistryOpen
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
Münzel T, Seidenstücker KC, Protzel C, Berg A, Berg T.   +4 more
europepmc   +2 more sources

Crystallographic and spectroscopic characterization of 2-[(7-acetyl-4-cyano-6-hydroxy-1,6-dimethyl-8-phenyl-5,6,7,8-tetrahydroisoquinolin-3-yl)sulfanyl]-N-phenylacetamide

Acta Crystallographica Section E: Crystallographic Communications, 2021
In the title molecule, C28H27N3O3S, the heterocyclic portion of the tetrahydroisoquinoline unit is planar and an intramolecular N—H...N hydrogen bond and a C—H...π(ring) interaction help to determine the overall conformation.
Elham A. Al-Taifi, Islam S. Maraei, Etify A. Bakhite, Güneş Demirtas, Joel. T. Mague, Shaaban K. Mohamed, Youssef Ramli   +6 more
doaj   +1 more source

Synthesis and reactions of 1-amino-1,5,6,10b-tetrahydroimidazo[2,1-a]isoquinolin-2(3H)-ones [PDF]

, 2008
1-Amino-1,5,6,10b-tetrahydroimidazo[2,1-a]isoquinolin-2(3H)-ones, as previously unknown ring-annelated isoquinolines with a 3-aminoimidazolidin-4-one scaffold, were selectively prepared upon reacting 2-carbamoylmethyl- or 2-ethoxycarbonylmethyl-3,4 ...
De Kimpe, Norbert, Holzer, Wolfgang, Mangelinckx, Sven, Martynaitis, Vytas, Solovjova, Joana, Šačkus, Algirdas   +5 more
core   +2 more sources

N-Methylimidazole Promotes The Reaction Of Homophthalic Anhydride With Imines [PDF]

, 2014
The addition of N-methylimidazole (NMI) to the reaction of homophthalic anhydride with imines such as pyridine-3-carboxaldehyde-N-trifluoroethylimine (9) reduces the amount of elimination byproduct and improves the yield of the formal cycloadduct ...
Aaron Levin, Bally T., Bogdanov M. G., David M. Floyd, Deng W., Flannery E. L., González-López M., Guibe-Jampel E., Guiguemde W. A., Haimova M. A., Höfle G., Jain R., Jian Liu, Kandinska M. I., Lenarcik B., Lindner C., Lutnæs O. B., Pattawong O., Paul R. Rablen, Scriven E. F. V., Spencer Knapp, Taydakov I. V., Thomas J. Emge, Vara Y., Yu N., Zheng Wang   +25 more
core   +3 more sources

Iridium-Catalyzed Asymmetric Intramolecular Allylic Amidation:Enantioselective Synthesis of Chiral Tetrahydroisoquinolines and Saturated Nitrogen Heterocycles [PDF]

, 2011
For the first time iridium catalysis has been used for the synthesis of chiral tetrahydroisoquinolines with excellent yields and high enantioselectivities (see scheme; cod=1,5-cyclooctadiene, DBU=1,8-diazabicyclo[5.4.0]undec-7-ene).
Bartels, Chrzanowska, Defieber, Dewick, Dübon, Förster, Gnamm, Helmchen, Ito, Kiener, Kinderman, Li, Lipowsky, Lyothier, Marković, Ohmura, Pouy, Pouy, Royer, Scott, Shu, Siengalewicz, Singh, Singh, Spiess, Szawkalo, Taylor, Teichert, Teichert, Tissot-Croset, Vicario, Welter, Zhou   +32 more
core   +6 more sources