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Featured researches published by Martin Nylöf.


Bioorganic & Medicinal Chemistry Letters | 2012

Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship

Inger Kers; Istvan Macsari; Gabor Csjernyik; Martin Nylöf; Karin Skogholm; Lars Sandberg; Alexander Minidis; Tjerk Bueters; Jonas Malmborg; Anders Eriksson; Per-Eric Lund; Elisabet Venyike; Lei Luo; Jan-Erik Nyström; Yevgeni Besidski

The Na(V)1.7 ion channel is an attractive target for development of potential analgesic drugs based on strong genetic links between mutations in the gene coding for the channel protein and inheritable pain conditions. The (S)-N-chroman-3-ylcarboxamide series, exemplified by 1, was used as a starting point for development of new channel blockers, resulting in the phenethyl nicotinamide series. The structure and activity relationship for this series was established and the metabolic issues of early analogues were addressed by appropriate substitutions. Compound 33 displayed acceptable overall in vitro properties and in vivo rat PK profile.


Bioorganic & Medicinal Chemistry Letters | 2012

Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers

Inger Kers; Gabor Csjernyik; Istvan Macsari; Martin Nylöf; Lars Sandberg; Karin Skogholm; Tjerk Bueters; Anders Eriksson; Sandra Oerther; Per-Eric Lund; Elisabet Venyike; Jan-Erik Nyström; Yevgeni Besidski

Recent findings showing a relation between mutations in the Na(V)1.7 channel in humans and altered pain sensation has contributed to increase the attractiveness of this ion channel as target for development of potential analgesics. Amido chromanes 1 and 2 were identified as blockers of the Na(V)1.7 channel and analogues with modifications of the 5-substituent and the carboxamide part of the molecule were prepared to establish the structure-activity relationship. Compounds 13 and 29 with good overall in vitro and in vivo rat PK profile were identified. Furthermore, 29 showed in vivo efficacy in a nociceptive pain model.


Bioorganic & Medicinal Chemistry Letters | 2012

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.

Yevgeni Besidski; William Brown; Johan Bylund; Michael Dabrowski; Sophie Dautrey; Magali Harter; Lucy Horoszok; Yin Hu; Dean Johnson; Shawn Johnstone; Paul Jones; Sandrine Leclerc; Karin Kolmodin; Inger Kers; Maryse Labarre; Denis Labrecque; Jennifer M.A. Laird; Therese Lundström; John Martino; Mickaël Maudet; Alexander Munro; Martin Nylöf; Andrea Penwell; Didier Rotticci; Andis Slaitas; Anna K. Sundgren-Andersson; Mats Svensson; Gitte Terp; Huascar Villanueva; Christopher Walpole

Benzothiazole amides were identified as TRPV1 antagonists from high throughput screening using recombinant human TRPV1 receptor and structure-activity relationships were explored to pinpoint key pharmacophore interactions. By increasing aqueous solubility, through the attachment of polar groups to the benzothiazole core, and enhancing metabolic stability, by blocking metabolic sites, the drug-like properties and pharmokinetic profiles of benzothiazole compounds were sufficiently optimized such that their therapeutic potential could be verified in rat pharmacological models of pain.


Journal of Biological Chemistry | 2003

Structural Insights and Biological Effects of Glycogen Synthase Kinase 3-specific Inhibitor AR-A014418

Ratan Bhat; Yafeng Xue; Stefan Berg; Sven Hellberg; Mats Ormö; Yvonne Nilsson; Ann-Cathrin Radesäter; Eva Jerning; Per-Olof Markgren; Thomas Borgegård; Martin Nylöf; Alfredo Giménez-Cassina; Félix Hernández; José J. Lucas; Javier Díaz-Nido; Jesús Avila


Archive | 1998

Substituted chroman derivatives

Stefan Berg; Martin Nylöf; Svante Ross; Seth-Olov Thorberg


Archive | 2004

New benzimidazole derivatives

Yevgeni Besidski; Inger Kers; Martin Nylöf; Didier Rotticci; Andis Slaitas; Mats Svensson


Archive | 2013

COMPOUNDS AND THEIR USE AS BACE INHIBITORS

Gabor Csjernyik; Sofia Karlström; Annika Kers; Karin Kolmodin; Martin Nylöf; Liselotte Öhberg; Laszlo Rakos; Lars Sandberg; Fernando Sehgelmeble; Peter Söderman; Britt-Marie Swahn; Stefan Berg


Journal of Medicinal Chemistry | 2000

Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.

Eva Maria Hammarberg; Gunnar Nordvall; Robert Leideborg; Martin Nylöf; Sverker Hanson; Lars Johansson; Seth-Olov Thorberg; Bo-Ragnar Tolf; Eva Jerning; Gun Torell Svantesson; Nina Mohell; Charlotte Ahlgren; Anita Westlind-Danielsson; Ingeborg Csöregh; Rolf Johansson


Archive | 2005

New heterocyclic amides

Yevgeni Besidski; Inger Kers; Martin Nylöf; Andis Slaitas


Archive | 2012

New Compounds 806

Yevgeni Besidki; Inger Kers; Martin Nylöf; Lars Sandberg; Karin Skogholm

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