Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Hasse Kromann"'
Autor:
Thomas Boesen, Anders Hallberg, Hans-Erik Claesson, Benjamin Pelcman, Wesley Schaal, Christian Krog-Jensen, Pontus Forsell, Mats Larhed, Hasse Kromann, Kristofer Olofsson, Andrei Sanin, Peter M. Nilsson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3017-3023
High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1
Autor:
Anders Hallberg, Peter M. Nilsson, Kiyo No, Mats Larhed, Thomas Boesen, Andrei Sanin, Wesley Schaal, Pontus Forsell, Stine B. Vogensen, Thomas Groth, Sara Öhrman, Hasse Kromann, Hans-Erik Claesson, Benjamin Pelcman, Christian Krog-Jensen
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(15)
Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, in
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:3047-3054
Hydroxy chalcones, for example, Licochalcone A, has for several years been known to be antibacterial. The low aqueous solubility and the medium antibacterial potency have limited the usefulness of the compounds. We describe the bioisosteric replaceme
Autor:
Jakob Felding, Finn Junager, Peter Uhlmann, Povl Krogsgaard-Larsen, Tine B. Stensbøl, Per Vedsø, Mikael Begtrup, Hasse Kromann, Sandrine Morel, Birgitte Langer Eriksen, Hans Bräuner-Osborne, Mette B. Hermit, Ulf Madsen, Jeremy R. Greenwood
Publikováno v:
Journal of Medicinal Chemistry. 45:19-31
A number of 1-hydroxyazole derivatives were synthesized as bioisosteres of (S)-glutamic acid (Glu) and as analogues of the AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA, 3b). All compounds were subjected
Publikováno v:
Tetrahedron. 57:2195-2201
The coupling reactions were performed using 3-ethoxy-4-iodo-5-methylisoxazole (4) as the key intermediate. Coupling of 4 under Suzuki–Miyaura or Stille conditions using Pd(PPh3)2Cl2 and arylboronic acids or aryltin analogues, respectively, gave 4-a
Publikováno v:
FEBS Letters. 439:127-132
Thapsigargin is a highly potent and selective inhibitor of sarco-endoplasmic reticulum (SERCA) family of Ca2+-ATPases and a useful tool in research concerning the function of intracellular Ca2+ stores. We describe here a novel fluorescent derivative
Publikováno v:
ChemInform. 32
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(21)
Chalcones can exist as Z- or E-isomers and it is generally anticipated that both isomers are equipotent. In order to determine the active isomer of anti-plasmodial chalcones a series of analogues locked in the Z- or the E-form were prepared and evalu
Publikováno v:
Journal of medicinal chemistry. 48(7)
This paper describes how the introduction of "cationic" aliphatic amino groups in the chalcone scaffold results in potent antibacterial compounds. It is shown that the most favorable position for the aliphatic amino group is the 2-position of the B-r
Autor:
Anne J. Andersen, Povl Krogsgaard-Larsen, Jerzy W. Jaroszewski, Sonata Krikstolaityte, Kristian Strømgaard, Kim Andersen, Jan Egebjerg, Hasse Kromann
Publikováno v:
Journal of medicinal chemistry. 45(26)
The wasp toxin philanthotoxin-433 (PhTX-433) is a nonselective and noncompetitive antagonist of ionotropic receptors, such as ionotropic glutamate receptors and nicotinic acetylcholine receptors. Polyamine toxins are extensively used for the characte