Výsledky vyhledávání - "W W, Mederski"

Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists

Autor: W W, Mederski, M, Osswald, D, Dorsch, M, Christadler, C J, Schmitges, C, Wilm

Publikováno v: Bioorganicmedicinal chemistry letters. 9(4)

The discovery, synthesis and structure-activity relationships of a series of novel benzofuro[3,2-b]pyridines as non-selective endothelin ET(A)/ET(B) as well as selective ET(B) receptor antagonists are described. The most potent non-selective inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::29a4bbada3ab997098be65f62a564921
https://pubmed.ncbi.nlm.nih.gov/10098676

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Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist

Autor: W W, Mederski, D, Dorsch, M, Osswald, S, Anzali, M, Christadler, C J, Schmitges, P, Schelling, C, Wilm, M, Fluck

Publikováno v: Bioorganicmedicinal chemistry letters. 8(13)

The discovery, in vitro and in vivo studies of the highly potent ETA antagonist EMD 122946 are presented. This compound displayed high binding affinity and functional antagonism [IC50 = 3.2 x 10(-11) M, pA2 = 9.5 (ETA)] and inhibited the ET-1 induced

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::72da73ed675d2c33b7056c9c602042fa
https://pubmed.ncbi.nlm.nih.gov/9873432

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Endothelin antagonists: search for surrogates of methylendioxyphenyl by means of a Kohonen neural network

Autor: S, Anzali, W W, Mederski, M, Osswald, D, Dorsch

Publikováno v: Bioorganicmedicinal chemistry letters. 8(1)

The methylendioxyphenyl group, present in a number of potent endothelin receptor antagonists, could have undesirable metabolic interactions with cytochrome P450 in vivo. Using a self-organizing neural network we analysed the features of molecular ele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3a0103f6d31c7a8070938ab6b424c29e
https://pubmed.ncbi.nlm.nih.gov/9871620

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Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster

Autor: W W, Mederski, M, Osswald, D, Dorsch, S, Anzali, M, Christadler, C J, Schmitges, C, Wilm

Publikováno v: Bioorganicmedicinal chemistry letters. 8(1)

The methylendioxyphenyl group is present in a number of endothelin receptor antagonists thus far reported. By means of a Kohonen neural network we discovered with a benzothiadiazole a bioisosteric replacement instead. This group should be devoid of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::675a094897a2c9eada9e5012506ba5be
https://pubmed.ncbi.nlm.nih.gov/9871621

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