Results 121 to 130 of about 103,451 (274)

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

, 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., Becker, Daniel P, Bedell, Louis J., Boehm, Terri L.   +3 more
core   +1 more source

On the Planarity of Heterocyclic Bay‐Substituted Perylenediimides: Insight into the Fluorescent Photoinduced Electron Transfer Sensing Framework

European Journal of Organic Chemistry, EarlyView.
Near‐infrared fluorescent pH indicators based on perylenediimide were constructed in a modular receptor–spacer–fluorophore–spacer–receptor format with heterocyclic amino moieties at the bay positions. Counterintuitively, the dibrominated intermediate with two heavy atoms is more emissive than the heterocyclic compounds.
Luke Camenzuli, Davide Benedetto Tiz, Nicola’ Agius, Konrad Szaciłowski, David C. Magri   +4 more
wiley   +1 more source

Stereoselective nucleophilic addition reactions to cyclic N-acyliminium ions using the indirect cation pool method: Elucidation of stereoselectivity by spectroscopic conformational analysis and DFT calculations

Beilstein Journal of Organic Chemistry, 2018
In this study, six-membered N-acyliminium ions were generated by the “indirect cation pool” method and reacted with several nucleophiles. These reactions afforded disubstituted piperidine derivatives with high diastereoselectivities and good to excellent
Koichi Mitsudo, Junya Yamamoto, Tomoya Akagi, Atsuhiro Yamashita, Masahiro Haisa, Kazuki Yoshioka, Hiroki Mandai, Koji Ueoka, Christian Hempel, Jun-ichi Yoshida, Seiji Suga   +10 more
doaj   +1 more source

Antimicrobial and antioxidant activities of piperidine derivatives

, 2015
Six novel piperidine derivatives, compounds 5 to 10, have been synthesized and their antimicrobial and anti-oxidant activities evaluated using agar disc diffusion (antimicrobial) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging capacity (antioxidant).
Naicker Leeantha, Katharigatta N. Venugopala, S. Francis, Odhav Bharti   +3 more
semanticscholar   +1 more source

Enantioselective synthesis of non-proteinogenic 2-arylallyl-α-amino acids via Pd/In catalytic cascades [PDF]

, 2006
An efficient synthesis of both R- and S-enantiomers of 2-arylallyl-α-amino acids via a diastereoselective Pd/In mediated catalytic allylation of chiral N-sulfinyl-α-imino esters is described.
Anwar, Anwar, Cleghorn, Cleghorn, Colin Kilner, Colin W.G. Fishwick, Cooper, Cooper, Cooper, Davis, Ellman, Ellman, Evans, Grigg, Grigg, Hodgson, Hohsaka, John Blacker, Kevin Bailey, Najera, Ronald Grigg, Shaun McCaffrey, Stewart Korn, Visuvanathar Sridharan   +23 more
core   +1 more source

Push–Pull Ynamines and Push–Pull Ynamides: Synthesis, Structure, Reactivity, and Application

European Journal of Organic Chemistry, EarlyView.
Push–pull ynamines and push–pull ynamides, which carry an EWG and an amino or amido group as EDG, are highly interesting classes of EDG‐EWG alkynes that have been intensively studied due to their exceptional reactivity. In this review, the synthesis, structure, reactivity, and application of push–pull ynamines, push–pull ynecarbamates, push–pull ...
Hans‐Joachim Gais
wiley   +1 more source

Comparison of In Silico AChE Inhibitory Potentials of Some Donepezil Analogues

Pharmata
Cholinesterases are important in ensuring hemostasis in our body. Excessive increase in cholinesterase function causes various cholinergic dysfunctions. Alzheimer's is a disease characterized by loss of cholinergic activity, which is especially common in
Mehmet Koca
doaj  

Synthesis and in vivo anti-ulcer evaluation of some novel piperidine linked dihydropyrimidinone derivatives

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Dihydropyrimidinone derivatives containing piperidine moiety were synthesised in a good yield. All the compounds were confirmed by elemental analysis and spectral data.
Mashooq Ahmad Bhat, Mohamed A. Al-Omar, Ahmed M. Naglah   +2 more
doaj   +1 more source

The Trypanosoma cruzi enzyme TcGPXI is a glycosomal peroxidase and can be linked to trypanothione reduction by glutathione or tryparedoxin. [PDF]

, 2002
Trypanosoma cruzi glutathione-dependent peroxidase I (TcGPXI) can reduce fatty acid, phospholipid, and short chain organic hydroperoxides utilizing a novel redox cycle in which enzyme activity is linked to the reduction of trypanothione, a parasite ...
Docampo, Flohe, Moreno, Viode, Henderson, Walsh, Krauth-Seigel, Muller, Nogoceke, Tetaud, Wilkinson, Wilkinson, Tetaud, Wilkinson, Boveris, Fairlamb, Mehlotra, Carnieri, Kendall, Kelly, Gibson, Martinez-Calvillo, Kelly, Kelly, Kelly, Cannata, Rutter, Easterby, Gommel, Steinert, Sommer, Opperdoes, Opperdoes, Michels, Parsons, Blattner, Bjornstedt, Sztajer, Horiguchi, Holgren, Fabianek, Shih, Shih, van den Bosch, Subramani, Keller, Singh, Singh, Boveris, Duffieux, Goodman, Knoops, Yamashita, Verdoucq, Seo, Lopez, Krieger   +56 more
core   +3 more sources

1,1‐Disubstituted Vinylbromides: Versatile Building Blocks for the Synthesis of Nitrogen‐Containing Heterocycles

European Journal of Organic Chemistry, EarlyView.
1,1‐Disubstituted vinylbromides are key intermediates for constructing nitrogen‐containing heterocycles. This review provides an overview of the synthetic applications of 1,1‐disubstituted vinylbromides and summarizes recent developments in reaction methodologies, mechanistic insights, and the structural diversity of N‐heterocyclic compounds accessible
Anne Westermeyer, Jun Fang, Chonghuo Liu, Guillaume Lefèvre, Gérard Guillamot, Phannarath Phansavath, Virginie Ratovelomanana‐Vidal   +6 more
wiley   +1 more source