Search Results - "Woerner, Francis"
-
1
Control of Mechanical Stability of Hollow Silica Particles, and Its Measurement by Mercury Intrusion Porosimetry
Published in Langmuir (16-05-2017)“…Hollow silica particles (HSPs) have become the focus of interest in many laboratories recently, because of their versatility, stemming from the ability to…”
Get full text
Journal Article -
2
Phenyltriazolinones as potent factor Xa inhibitors
Published in Bioorganic & medicinal chemistry letters (15-02-2010)“…We have discovered that phenyltriazolinone is a novel and potent P 1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a…”
Get full text
Journal Article -
3
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds
Published in Bioorganic & medicinal chemistry letters (19-01-2004)“…Analogues of isoxazoline α vβ 3 antagonist 1 designed to further restrict the four carbon alkyl tether were prepared by incorporating two spirocyclic…”
Get full text
Journal Article -
4
Cyclic Urea Amides: HIV-1 Protease Inhibitors with Low Nanomolar Potency against both Wild Type and Protease Inhibitor Resistant Mutants of HIV
Published in Journal of medicinal chemistry (17-01-1997)“…Cyclic urea amides, a novel series of HIV-1 protease (HIV PR) inhibitors, have increased activity against drug-resistant mutants of the HIV PR. The design…”
Get full text
Journal Article -
5
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors
Published in Bioorganic & medicinal chemistry letters (10-02-2003)“…Factor Xa (fXa) is an important serine protease that holds the central position linking the intrinsic and extrinsic activation mechanisms in the blood…”
Get full text
Journal Article -
6
Nonpeptide Cyclic Cyanoguanidines as HIV-1 Protease Inhibitors: Synthesis, Structure−Activity Relationships, and X-ray Crystal Structure Studies
Published in Journal of medicinal chemistry (23-04-1998)“…Comparison of the high-resolution X-ray structures of the native HIV-1 protease and its complexes with the inhibitors suggested that the enzyme flaps are…”
Get full text
Journal Article -
7
Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors
Published in Journal of medicinal chemistry (13-02-2014)“…Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to demonstrate robust efficacy with a low bleeding risk profile. Herein, we…”
Get full text
Journal Article -
8
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
Published in Bioorganic & medicinal chemistry letters (01-11-2006)“…The bicyclic tetrahydropyrazolopiperidinone scaffold allowed for the incorporation of multiple neutral P1 moieties with subnanomolar binding affinities for…”
Get full text
Journal Article -
9
Synthesis of 8-membered cyclic sulfamides: Novel HIV-1 protease inhibitors
Published in Tetrahedron letters (04-09-1995)“…One pot synthesis of pseudo C2 symmetric (2S,6S)-2,6-dihydroxy-1,7-diphenylhept-4-one in high enantiomeric purity has been developed and the intermediate was…”
Get full text
Journal Article -
10
Calculated and Experimental Low-Energy Conformations of Cyclic Urea HIV Protease Inhibitors
Published in Journal of the American Chemical Society (20-05-1998)“…One important factor influencing the affinity of a flexible ligand for a receptor is the internal strain energy required to attain the bound conformation…”
Get full text
Journal Article -
11
Synthesis of 7-membered cyclic hydroxyguanidines: Novel HIV-1 protease inhibitors
Published in Bioorganic & medicinal chemistry letters (09-09-1997)“…Novel cyclic 7-membered hydroxyguanidine based HIV-1 protease inhibitors have been synthesized from 7-membered cyclic thiourea. Graphic…”
Get full text
Journal Article -
12
Synthesis of water soluble prodrug of DMP323
Published in Bioorganic & medicinal chemistry letters (08-10-1996)“…A water soluble bisphosphate prodrug of DMP323 was synthesized from DMP323. Pharmacokinetic studies of the prodrug indicate that it is orally absorbed as the…”
Get full text
Journal Article