Results 61 to 70 of about 25,392 (338)

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

Dual‐Mode Type I/II Photosensitization of a Stable Mesoporous Hydrogen‐Bonded Organic Framework for Antibacterial Therapy

open access: yesAdvanced Science, EarlyView.
A π‐conjugated donor–acceptor PDI monomer undergoes hydrogen‐bonded self‐assembly to form a robust mesoporous framework. The ordered molecular arrangement promotes efficient intersystem crossing and charge separation, leading to simultaneous Type I and Type II reactive oxygen species generation with a high singlet oxygen quantum yield.
Yi‐Lun Cheng   +10 more
wiley   +1 more source

Workers and alate queens of Solenopsis geminata share qualitatively similar but quantitatively different venom alkaloid chemistry [PDF]

open access: yes, 2015
Solenopsis geminata group (Hymenoptera: Formicidae) encompasses ant species commonly called fire ants because of their painful sting. The many physiological effects of the venom are caused by 2-methyl-6-alkyl and/or alkenylpiperidine alkaloids.
Li Chen   +5 more
core   +2 more sources

Sodium piperidine-1-carbodithioate dihydrate [PDF]

open access: yesActa Crystallographica Section E Structure Reports Online, 2011
The asymmetric unit of the title compound, Na(+)·C(6)H(10)NS(2) (-)·2H(2)O, is composed of a sodium cation, a piperidine-dithio-carbamate anion which exhibits positional disorder, and two lattice water mol-ecules. The atoms of the piperidine ring are divided over two sites with occupancy factors of 0.554 (6) and 0.446 (6).
Ana C. Mafud   +1 more
openaire   +3 more sources

Rational Design of Broad‐Spectrum Anti‐Enteroviral Molecular Glues Targeting Enteroviral RNAi Suppressors

open access: yesAdvanced Science, EarlyView.
By leveraging this homodimerization mechanism, molecular glues were rationally designed to induce dysfunctional 3A dimerization, thereby restoring antiviral RNAi. The optimal molecular glue, VTP‐32, demonstrated potent and pan‐enterovirus (groups A, B, D) antiviral effects.
Yuan Fang   +13 more
wiley   +1 more source

Synthesis and potential use of 1,8-naphthalimide type O-1(2) sensor molecules [PDF]

open access: yes, 2013
New double (fluorescent and spin) sensor molecules containing 4-amino substituted 1,8-naphthalimide as a fluorophore and a sterically hindered amine (pre-nitroxide) or pyrroline nitroxide as a quencher and radical capturing moiety were synthesized.
Bognár   +41 more
core   +1 more source

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

open access: yesAdvanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng   +12 more
wiley   +1 more source

Stereoselective, nitro-Mannich/lactamisation cascades for the direct synthesis of heavily decorated 5-nitropiperidin-2-ones and related heterocycles

open access: yesBeilstein Journal of Organic Chemistry, 2012
A versatile nitro-Mannich/lactamisation cascade for the direct stereoselective synthesis of heavily decorated 5-nitropiperidin-2-ones and related heterocycles has been developed. A highly enantioenriched substituted 5-nitropiperidin-2-one was synthesised
Pavol Jakubec   +4 more
doaj   +1 more source

Experimental study of local anesthetic and antiarrhythmic activities of fluorinated ethynylpiperidine derivatives [PDF]

open access: yesBrazilian Journal of Medical and Biological Research
The chemical structure of piperidine has a unique ability to combine with other molecular fragments. This fact makes it possible to actively use it as an effective basis for the creation of new drug-like substances.
E.M. Satbayeva   +10 more
doaj   +1 more source

Efficacy of different dose of dexmedetomidine combined with remifentanil in colonoscopy: a randomized controlled trial

open access: yesBMC Anesthesiology, 2020
Background Dexmedetomidine has advantages during colonoscopy as it allows the patient to cooperate during the procedure. Few studies examined the dexmedetomidine-remifentanil combination.
Li Jia   +5 more
doaj   +1 more source

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