Structure, properties and obtention routes of flaxseed lignan secoisolariciresinol

in Biotechnologie, Agronomie, Société et Environnement = Biotechnology, Agronomy, Society and Environment [=BASE] (2012), 16(1), 115-124

Following a brief description of the structure and nomenclature of the lignan family, this review focuses on the flaxseed lignan secoisolariciresinol (SECO). The main properties, the analysis methods and ... [more ▼]

Following a brief description of the structure and nomenclature of the lignan family, this review focuses on the flaxseed lignan secoisolariciresinol (SECO). The main properties, the analysis methods and two routes for the preparation of SECO, i.e. extraction from renewable raw material and (hemi)-synthesis, are reviewed. Green methods recently developed for the first route and chemical syntheses inspired from biosyntheses for the second one are the main subjects of this paper. [less ▲]

Structure-activity relationship (SAR) of new torasemide derivatives on Na-K-2Cl cotransporter in perfused rabbit thick ascending limb (cTAL) of Henle's loop.

Poster (1990, June 08)

Structure-activity relationships in platelet-activating factor (PAF).7. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors. Synthesis and PAF-antagonist activity

in Journal of Lipid Mediators and Cell Signalling (1996), 13

Structure-Activity Relationships in the Beta-Lactam Family: An Impossible Dream

in Biochemical Pharmacology (1988), 37(1), 125-32

The difficulty of establishing structure-activity relationships in the beta-lactam family of antibiotics stems from the fact that: (1) The targets in various bacteria exhibit widely different ... [more ▼]

The difficulty of establishing structure-activity relationships in the beta-lactam family of antibiotics stems from the fact that: (1) The targets in various bacteria exhibit widely different sensitivities. (2) Some bacteria produce beta-lactamases, enzymes capable of destroying the antibiotics. The rates of the reactions with the beta-lactamases and the target enzymes are not necessarily related. (3) In Gram-negative bacteria, the diffusion rate through the outer membrane varies independently from the two other factors. [less ▲]

Structure-activity relationships on adrenoceptors and imidazoline-preferring binding sites (I(1,2)-PBSs). Part 1: Weak intramolecular H-bond and conformational flexibility in a new I1-PBS-selective imidazoline analogue, trans1-(4',5'-dihydro-1'H-imidazol-2'-yl)methyl-2-hydroxyindane (PMS 952).

in Bioorganic & Medicinal Chemistry (2000), 8(8), 1861-9

The highly selective I1-PBS imidazoline analogue PMS 952 has been selected to study the incidence of intramolecular hydrogen bond and molecular flexibility on its biological activity. On one hand, the ... [more ▼]

The highly selective I1-PBS imidazoline analogue PMS 952 has been selected to study the incidence of intramolecular hydrogen bond and molecular flexibility on its biological activity. On one hand, the weak energy difference between three calculated conformers does not support the stabilization of one conformer by an internal hydrogen bond. The 3-D electrostatic map confirms this feature and the solvent effect does not significantly modify the relative energy of these conformers. On the other hand, the conformational spaces of the neutral and ionized forms present a great number of equilibrium structures, in a short energetic range (20 Kcal). The results are representative of an exceptional conformational flexibility due to a cooperative effect between several parts of the molecule. [less ▲]

Structure-based design of selective high-affinity telomeric quadruplex-binding ligands

in Chemical Communications (2010), 46

A library of triazole-based telomeric quadruplex-selective ligands has been developed that mimic an established family of tri-substituted acridine-based ligands, using crystal structure data as a starting ... [more ▼]

A library of triazole-based telomeric quadruplex-selective ligands has been developed that mimic an established family of tri-substituted acridine-based ligands, using crystal structure data as a starting-point for computer-based design. Binding affinities, estimated by electrospray mass spectrometry, are in accord with the design concept [less ▲]

Structure-function analysis of amyloid peptide and prion protein by molecular modeling

Conference (1997, April)

Structure-function analysis of amyloid peptide and prion protein by molecular modeling : prediction and demonstration of tilted fusogenic fragments

Conference (1997, March)

Structure-Guided Design of Cell Wall Biosynthesis Inhibitors That Overcome beta-Lactam Resistance in Staphylococcus aureus (MRSA).

in ACS Chemical Biology (2011)

beta-Lactam antibiotics have long been a treatment of choice for bacterial infections since they bind irreversibly to Penicillin-Binding Proteins (PBPs), enzymes that are vital for cell wall biosynthesis ... [more ▼]

beta-Lactam antibiotics have long been a treatment of choice for bacterial infections since they bind irreversibly to Penicillin-Binding Proteins (PBPs), enzymes that are vital for cell wall biosynthesis. Many pathogens express drug-insensitive PBPs rendering beta-lactams ineffective, revealing a need for new types of PBP inhibitors active against resistant strains. We have identified alkyl boronic acids that are active against pathogens including methicillin-resistant S. aureus (MRSA). The crystal structures of PBP1b complexed to 11 different alkyl boronates demonstrate that in vivo efficacy correlates with the mode of inhibitor side chain binding. Staphylococcal membrane analyses reveal that the most potent alkyl boronate targets PBP1, an autolysis system regulator, and PBP2a, a low beta-lactam affinity enzyme. This work demonstrates the potential of boronate-based PBP inhibitors for circumventing beta-lactam resistance and opens avenues for the development of novel antibiotics that target Gram-positive pathogens. [less ▲]

Structure-modifying drugs in osteoarthritis

in Osteoporosis International (2002, November), 13(Suppl.3), 9