| pubmed-article:11563929 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:11563929 | lifeskim:mentions | umls-concept:C0018320 | lld:lifeskim |
| pubmed-article:11563929 | lifeskim:mentions | umls-concept:C0074785 | lld:lifeskim |
| pubmed-article:11563929 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:11563929 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:11563929 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:11563929 | pubmed:issue | 20 | lld:pubmed |
| pubmed-article:11563929 | pubmed:dateCreated | 2001-9-20 | lld:pubmed |
| pubmed-article:11563929 | pubmed:abstractText | A novel series of arylcyclopropanecarboxyl guanidines was synthesized and evaluated for activity against the sodium hydrogen exchanger isoform-1 (NHE-1). In biological assays conducted in an AP1 cell line expressing the human NHE-1 isoform, the starting cyclopropane 3a (IC(50) = 3.5 microM) shows inhibitory activity comparable to cariporide (IC(50) = 3.4 microM). Structure-activity relationships are used to optimize the affinity of various acyl guanidines for NHE-1 by screening the effect of substituents at both aryl and cyclopropyl rings. It is demonstrated that introduction of appropriate hydrophobic groups at the phenyl ring and a gem-dimethyl group at the cyclopropane ring enhances the NHE-1 inhibitory activity by up to 3 orders of magnitude (compound 7f, IC(50) = 0.003 microM). In addition, the gem-dimethyl series of analogues seem to display improved oral bioavailability and longer plasma half-life in rats. Furthermore, the lead benzodihydrofuranyl analogue 1 (BMS-284640) shows over 380-fold increased NHE-1 inhibitory activity as well as improved selectivity for NHE-1 over NHE-2 compared to cariporide. | lld:pubmed |
| pubmed-article:11563929 | pubmed:language | eng | lld:pubmed |
| pubmed-article:11563929 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11563929 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:11563929 | pubmed:month | Sep | lld:pubmed |
| pubmed-article:11563929 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:LanS JSJ | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:AhmadSS | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:WuS CSC | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:YostK JKJ | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:KirbyMM | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:ChenB CBC | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:NgoAA | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:DoweykoL MLM | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:SerafinoRR | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:GavinB JBJ | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:GougoutasJ... | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:AtwalK SKS | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:ChenA YAY | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:DorsoC RCR | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:DuganWW | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:DiMarcoJ DJD | lld:pubmed |
| pubmed-article:11563929 | pubmed:author | pubmed-author:GrazierNN | lld:pubmed |
| pubmed-article:11563929 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:11563929 | pubmed:day | 27 | lld:pubmed |
| pubmed-article:11563929 | pubmed:volume | 44 | lld:pubmed |
| pubmed-article:11563929 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:11563929 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:11563929 | pubmed:pagination | 3302-10 | lld:pubmed |
| pubmed-article:11563929 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:meshHeading | pubmed-meshheading:11563929... | lld:pubmed |
| pubmed-article:11563929 | pubmed:year | 2001 | lld:pubmed |
| pubmed-article:11563929 | pubmed:articleTitle | Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1. | lld:pubmed |
| pubmed-article:11563929 | pubmed:affiliation | Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, NJ 08543, USA. saleem.ahmad@bms.com | lld:pubmed |
| pubmed-article:11563929 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:11563929 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:11563929 | lld:chembl |
