Results 61 to 70 of about 24,641 (321)

HMPA-Catalyzed Transfer Hydrogenation of 3-Carbonyl Pyridines and Other N-Heteroarenes with Trichlorosilane

open access: yesMolecules, 2019
A method for the HMPA (hexamethylphosphoric triamide)-catalyzed metal-free transfer hydrogenation of pyridines has been developed. The functional group tolerance of the existing reaction conditions provides easy access to various piperidines with ester ...
Yun Fu, Jian Sun
doaj   +1 more source

Transaminase triggered aza-Michael approach for the enantioselective synthesis of piperidine scaffolds [PDF]

open access: yes, 2016
The expanding “toolbox” of biocatalysts opens new opportunities to redesign synthetic strategies to target molecules by incorporating a key enzymatic step into the synthesis.
Andrew Gomm   +6 more
core   +3 more sources

Peptomer Linkers Enable Kinetic Control over Co‐Delivery of Multiple Chemotherapeutics

open access: yesAdvanced Healthcare Materials, EarlyView.
A key challenge in combinatorial chemotherapeutic drug delivery is independent control over release kinetics, especially with drugs of similar size and structure. Here, peptoid substitutions to proteolytically degradable peptides enabled the design of fast and slow‐releasing drug linkers.
Carolyn M. Watkins   +3 more
wiley   +1 more source

Thiosulfonate‐Derived BODIPY “Stick and Glue” Strategy for Fluorescent Thiol Labeling

open access: yesAngewandte Chemie, EarlyView.
We present a powerful photochemical strategy for converting disulfide bonds into stable thioether linkages via a [1,2]‐sigmatropic rearrangement. By integrating this reaction into traditional methanethiosulfonate‐based thiol labeling, we enable light‐triggered stabilization of peptide and protein conjugates with enhanced robustness and versatility ...
Lucie Šálková   +4 more
wiley   +2 more sources

Silacyclohexanes, Sila(hetero)cyclohexanes and Related Compounds: Structure and Conformational Analysis

open access: yesMolecules, 2020
Conformational analysis of Si-mono- and Si,Si-disubstituted silacyclohexanes as well as their analogues with a heteroatom(s) in the ring is reviewed with the focus on the recent results.
Bagrat A. Shainyan
doaj   +1 more source

Design and Utilization of Stable Hydrofluoroolefin‐Based Trifluoropropynyl Surrogate for Sonogashira Coupling

open access: yesAdvanced Synthesis &Catalysis, EarlyView.
A novel methodology for the construction of aromatic and heteroaromatic trifluoropropynyl derivatives has been developed. The new protocol is based on a tandem Sonogashira cross‐coupling reaction between a bench‐stable trifluoropropynyl carbinol reagent, generated from the commercially available and inexpensive hydrofluoroolefin‐1234yf gas, and (hetero)
Emma Bodnár   +3 more
wiley   +1 more source

Plasmonic Hot‐Carrier Redox Enables Proton‐Coupled Electron Transfer at C─H Bonds

open access: yesAngewandte Chemie, EarlyView.
Plasmonic hot carriers provide unprecedented control over coupled electron–proton transfer, enabling visible‐light activation of strong C─H bonds. Using an energy‐filter electrode, we reveal a stepwise electron‐then‐proton pathway and directly tune the underlying driving forces.
Daniel Velev Latchev   +3 more
wiley   +2 more sources

Synthesis and Evaluation of Novel Iminosugars Prepared from Natural Amino Acids

open access: yesMolecules, 2021
Cyclopropanated iminosugars have a locked conformation that may enhance the inhibitory activity and selectivity against different glycosidases. We show the synthesis of new cyclopropane-containing piperidines bearing five stereogenic centers from natural
Alejandro Puet   +3 more
doaj   +1 more source

Orally Active MMP-1 Sparing α-tetrahydropyranyl and α-piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease [PDF]

open access: yes, 2010
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP’s-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the ...
Barta, Thomas E.   +3 more
core   +1 more source

Discovery of a Novel and Potent Kir4.1 Inhibitor as a Safe and Rapid‐Onset Antidepressant Agent in Mice

open access: yesAdvanced Science, EarlyView.
The preferred derivative JX3212 demonstrates strong inhibitory activity against Kir4.1 with favorable druggability and shows significant antidepressant efficacy in vivo. Abstract Major depressive disorder is a serious psychiatric disorder for which novel and fast‐acting antidepressants are required.
Sisi Wang   +15 more
wiley   +1 more source

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