[HTML][HTML] The global preclinical antibacterial pipeline

…, K Outterson, A Engel, A Karlén - Nature Reviews …, 2020 - nature.com
Antibacterial resistance is a great concern and requires global action. A critical question is
whether enough new antibacterial drugs are being discovered and developed. A review of the …

Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach

…, F Ax, A Hallberg, H Lennernäs, A Karlén - Journal of medicinal …, 1998 - ACS Publications
The effective permeability (P eff ) in the human jejunum (in vivo) of 22 structurally diverse
compounds was correlated with both experimentally determined lipophilicity values and …

Discovery and preclinical development of new antibiotics

D Hughes, A Karlén - Upsala journal of medical sciences, 2014 - Taylor & Francis
Antibiotics are the medical wonder of our age, but an increasing frequency of resistance among
key pathogens is rendering them less effective. If this trend continues the consequences …

The Innovative Medicines Initiative's New Drugs for Bad Bugs programme: European public–private partnerships for the development of new strategies to tackle …

…, M Winterhalter, RA Stavenger, A Karlén… - Journal of …, 2016 - academic.oup.com
Antibiotic resistance (ABR) is a global public health threat. Despite the emergence of highly
resistant organisms and the huge medical need for new drugs, the development of …

Design, Synthesis, and Biological Evaluation of the First Selective Nonpeptide AT2 Receptor Agonist

…, M Holm, M Botoros, A Karlén… - Journal of medicinal …, 2004 - ACS Publications
The first druglike selective angiotensin II AT 2 receptor agonist (21) with a K i value of 0.4 nM
for the AT 2 receptor and a K i >10 μM for the AT 1 receptor is reported. Compound 21, with …

Relationships between structure and interaction kinetics for HIV-1 protease inhibitors

…, W Schaal, M Hämäläinen, A Karlén… - Journal of medicinal …, 2002 - ACS Publications
The interaction between HIV-1 protease and 58 structurally diverse transition-state
analogue inhibitors has been analyzed by a surface plasmon resonance based biosensor. …

Unexpected binding mode of a cyclic sulfamide HIV-1 protease inhibitor

…, NM Bonham, W Schaal, A Karlén… - Journal of medicinal …, 1997 - ACS Publications
Two cyclic, C 2 -symmetric HIV-1 protease inhibitors, one sulfamide and one urea derivative,
both comprising phenyl ether groups in the P1/P1‘ positions, were cocrystallized with HIV-1 …

[HTML][HTML] Towards the sustainable discovery and development of new antibiotics

…, M Graz, M Lindvall, S Ramurthy, A Karlén… - Nature Reviews …, 2021 - nature.com
An ever-increasing demand for novel antimicrobials to treat life-threatening infections caused
by the global spread of multidrug-resistant bacterial pathogens stands in stark contrast to …

Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities

…, B Classon, UH Danielson, A Karlén… - Journal of Medicinal …, 1997 - ACS Publications
Ten C 2 -symmetric cyclic urea and sulfamide derivatives have been synthesized from l-mannonic
γ-lactone and d-mannitol. The results of experimental measurement of their inhibitory …

Vinyl Sulfide Cyclized Analogues of Angiotensin II with High Affinity and Full Agonist Activity at the AT1 Receptor

…, M Le Greves, F Nyberg, A Karlén… - Journal of medicinal …, 2002 - ACS Publications
Vinyl sulfide cyclized analogues of the octapeptide angiotensin II that are structurally related
to the cyclic disulfide agonist c[Hcy 3,5 ]Ang II have been prepared. The synthesis relies on …