197573-17-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as potential PDE4 inhibitors
Song, Gaopeng,Zhao, Dongsheng,Hu, Dekun,Li, Yasheng,Jin, Hongwei,Cui, Zining
, p. 4610 - 4614 (2015)
The design, synthesis, and biological evaluation of new phosphodiesterase type 4 (PDE4) inhibitors, which possessed 7-(cyclopentyloxy)-6-methoxy 1,2,3,4-tetrahydroisoquinoline ring, were described. Compound 8 [(7-cyclopentyloxy)-6-methoxy-3,4-dihydroisoqu
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors
Song, Gaopeng,Zhu, Xiang,Li, Junhua,Hu, Dekun,Zhao, Dongsheng,Liao, Yixian,Lin, Juntong,Zhang, Lian-Hui,Cui, Zi-Ning
, p. 5709 - 5717 (2017)
Improvement of subtype selectivity of an inhibitor's binding activity using the conformational restriction approach has become an effective strategy in drug discovery. In this study, we applied this approach to PDE4 inhibitors and designed a series of nov
Cyclopentyl: A novel protective group for phenols
Gajera, Jitendra M.,Gharat, Laxmikant A.,Farande, Aniket V.
, p. 4309 - 4312 (2007)
We have discovered cyclopentyl as a novel group for the protection of hydroxyl functionality of phenols. The key steps involved are cyclopentylation and decyclopentylation. Copyright Taylor & Francis Group, LLC.
Cyclopentyl: A novel protective group for phenols
Gajera, Jitendra M.,Gharat, Laxmikant A.,Farande, Aniket V.
, p. 2877 - 2880 (2007)
We have discovered cyclopentyl as a novel group for the protection of hydroxyl functionality of phenols. The key steps involved are cyclopentylation and decyclopentylation. Copyright Taylor & Francis Group, LLC.
TETRAHYDROISOQUINOLINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
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Paragraph 0077-0078, (2020/12/22)
Disclosed are a novel tetrahydroisoquinoline compound, a method for preparing intermediates thereof, a pharmaceutical composition thereof and the use thereof. The tetrahydroisoquinoline compound of the present invention has a good inhibitory effect on phosphodiesterase (PDE4), and can be used in the prevention, treatment or auxiliary treatment of multiple diseases associated with the activity or expression of phosphodiesterase, especially PDE4-associated immune and inflammatory diseases, such as psoriasis and arthritis. (I)
Tetrahydroisoquinoline and carbamate containing compound, preparation method therefor and application of compound
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Paragraph 0053; 0055; 0056, (2017/05/19)
The invention discloses a tetrahydroisoquinoline and carbamate containing compound. The tetrahydroisoquinoline and carbamate containing compound has a structure represented by a formula I shown in the description, wherein R1 is H, cycloalkyl, alkyl or sub
C3-substituted tetrahydroisoquinoline derivative and preparation method and application thereof
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Paragraph 0066; 0067; 0068; 0069; 0070; 0071, (2017/08/29)
The invention discloses a C3-substituted tetrahydroisoquinoline derivative. A structure formula of the derivative is shown in formula I or formula II, wherein an R1 group is hydrogen, a naphthenic group, an alkyl group, a phenyl group or a substituted phe
BICYCLIC FUSED PYRAZOLE DERIVATIVES FOR THE TREATMENT OF RSV
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Page/Page column 87, (2017/12/05)
Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and method
Chemical assembly systems: Layered control for divergent, continuous, multistep syntheses of active pharmaceutical ingredients
Ghislieri, Diego,Gilmore, Kerry,Seeberger, Peter H.
supporting information, p. 678 - 682 (2015/03/04)
While continuous chemical processes have attracted both academic and industrial interest, virtually all active pharmaceutical ingredients (APIs) are still produced by using multiple distinct batch processes. To date, methods for the divergent multistep continuous production of customizable small molecules are not available. A chemical assembly system was developed, in which flow-reaction modules are linked together in an interchangeable fashion to give access to a wide breadth of chemical space. Control at three different levels - choice of starting material, reagent, or order of reaction modules - enables the synthesis of five APIs that represent three different structural classes (γ-amino acids, γ-lactams, β-amino acids), including the blockbuster drugs Lyrica and Gabapentin, in good overall yields (49-75%).
Imidazole derivatives show anticancer potential by inducing apoptosis and cellular senescence
Sharma, Gangavaram V. M.,Ramesh, Adepu,Singh, Ashita,Srikanth, Gourishetty,Jayaram, Vankudoth,Duscharla, Divya,Jun, Jung Ho,Ummanni, Ramesh,Malhotra, Sanjay V.
, p. 1751 - 1760 (2014/12/11)
Imidazole-based compounds are attractive targets in the design of novel chemical structures for the discovery of new drugs. In the current study, we have synthesized a series of new 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles by multicomponent reaction (MCR). Vanillin and isovanillin derivatives were reacted with benzil/pyridil and diverse amines and ammonium acetate in acetic acid at 50-110 °C for 24 h to afford respective imidazoles in 55-70% yields. The series of molecules were evaluated for anti-cancer potential against the National Cancer Institute's 60 human cancer cell line panel. Preliminary screening highlighted the anticancer potential of 2,2′-(2-(3-(cyclopentyloxy)-4-methoxyphenyl)-1-isobutyl-1H-imidazole-4,5-diyl)dipyridine (NSC 771432) against different cancer cell types. A549 cells were treated in vitro to determine the mode of action of NSC 771432 on growth of these cells. This compound inhibits anchorage independent growth and cell migration, and induces cell cycle arrest in the G2/M phase. Also, the exposure of A549 cells to NSC 771432 leads to cellular senescence. This journal is
