| pubmed-article:10579842 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C2003941 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C1524075 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0870883 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C1883695 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0243076 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C1707689 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C1292724 | lld:lifeskim |
| pubmed-article:10579842 | lifeskim:mentions | umls-concept:C0070698 | lld:lifeskim |
| pubmed-article:10579842 | pubmed:issue | 23 | lld:pubmed |
| pubmed-article:10579842 | pubmed:dateCreated | 1999-12-17 | lld:pubmed |
| pubmed-article:10579842 | pubmed:abstractText | Dihydropyrimidinones, such as 1, represent a novel class of alpha(1a) adrenoceptor antagonists with potential for the treatment of benign prostatic hyperplasia (BPH) (see part 1 of this series). Analysis of the metabolites of 1 revealed that 4-methoxycarbonyl-4-phenylpiperidine is formed as the major metabolite and is an agonist at the mu-opioid receptor. To circumvent any potential liability resulting from the metabolite, we decided to identify alternate templates devoid of agonist activity at the mu-opioid receptor to replace the 4-methoxycarbonyl-4-phenylpiperidine moiety. The present study describes the synthesis and SAR of dihydropyrimidinones linked to substituted 4-phenylpiperazine containing side chains. Compound (+)-38 was identified as a lead compound with a binding and functional profile comparable to that of 1. The putative metabolite 2-carboxamidophenylpiperazine has negligible affinity for the mu-opioid receptor. | lld:pubmed |
| pubmed-article:10579842 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10579842 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10579842 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10579842 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:10579842 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:ChangR SRS | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:WongW CWC | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:ChiuGG | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:VyasK PKP | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:ZhangKK | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:SumPP | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:ZhangFF | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:RansomR WRW | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:ForrayCC | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:MiaoS WSW | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:MarzabadiM... | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:TianDD | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:FangJJ | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:DiazV PVP | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:O'MalleySS | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:NagarathnamDD | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:GluchowskiCC | lld:pubmed |
| pubmed-article:10579842 | pubmed:author | pubmed-author:LaheSS | lld:pubmed |
| pubmed-article:10579842 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10579842 | pubmed:day | 18 | lld:pubmed |
| pubmed-article:10579842 | pubmed:volume | 42 | lld:pubmed |
| pubmed-article:10579842 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10579842 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10579842 | pubmed:pagination | 4794-803 | lld:pubmed |
| pubmed-article:10579842 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:10579842 | pubmed:meshHeading | pubmed-meshheading:10579842... | lld:pubmed |
| pubmed-article:10579842 | pubmed:meshHeading | pubmed-meshheading:10579842... | lld:pubmed |
| pubmed-article:10579842 | pubmed:meshHeading | pubmed-meshheading:10579842... | lld:pubmed |
| pubmed-article:10579842 | pubmed:meshHeading | pubmed-meshheading:10579842... | lld:pubmed |
| pubmed-article:10579842 | pubmed:year | 1999 | lld:pubmed |
| pubmed-article:10579842 | pubmed:articleTitle | Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains. | lld:pubmed |
| pubmed-article:10579842 | pubmed:affiliation | Departments of Chemistry and Pharmacology, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, USA. | lld:pubmed |
| pubmed-article:10579842 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:10579842 | pubmed:publicationType | In Vitro | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:10579842 | lld:chembl |
