| pubmed-article:10715167 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0282519 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0023175 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0268563 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0596988 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C1707919 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0121925 | lld:lifeskim |
| pubmed-article:10715167 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
| pubmed-article:10715167 | pubmed:issue | 5 | lld:pubmed |
| pubmed-article:10715167 | pubmed:dateCreated | 2000-4-13 | lld:pubmed |
| pubmed-article:10715167 | pubmed:abstractText | Through computationally directed broad screening, a novel 1, 5-diphenylpyrazole (DPP) class of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) has been discovered. Compound 2 (PNU-32945) was found to have good activity versus wild-type (IC(50) = 2.3 microM) and delavirdine-resistant P236L (IC(50) = 1.1 microM) reverse transcriptase (RT). Also, PNU-32945 has an ED(50) for inhibition of viral replication in cell cultures of 0.1 microM and was shown to be noncytotoxic with a CC(50) > 10 microM. Structure-activity relationship studies on the 3- and 4-positions of PNU-32945 led to interesting selectivity and activity within the class. In particular, the 3-hydroxyethyl-4-ethyl congener 29 is a potent inhibitor of the P236L mutant (IC(50) = 0.65 microM), whereas it is essentially inactive versus the wild-type enzyme (IC(50) > 50 microM). Furthermore, this compound was significantly more active versus the P236L mutant than delavirdine. The synthesis and RT inhibitory activity of various 3- and 4-substituted analogues are discussed. | lld:pubmed |
| pubmed-article:10715167 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10715167 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:10715167 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10715167 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10715167 | pubmed:month | Mar | lld:pubmed |
| pubmed-article:10715167 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:YagiYY | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:BilesCC | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:TarpleyW GWG | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:RomeroD LDL | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:PoppeS MSM | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:SwaneyS MSM | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:GeninM JMJ | lld:pubmed |
| pubmed-article:10715167 | pubmed:author | pubmed-author:KeiserB JBJ | lld:pubmed |
| pubmed-article:10715167 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10715167 | pubmed:day | 9 | lld:pubmed |
| pubmed-article:10715167 | pubmed:volume | 43 | lld:pubmed |
| pubmed-article:10715167 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10715167 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10715167 | pubmed:pagination | 1034-40 | lld:pubmed |
| pubmed-article:10715167 | pubmed:dateRevised | 2007-11-15 | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:meshHeading | pubmed-meshheading:10715167... | lld:pubmed |
| pubmed-article:10715167 | pubmed:year | 2000 | lld:pubmed |
| pubmed-article:10715167 | pubmed:articleTitle | Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. | lld:pubmed |
| pubmed-article:10715167 | pubmed:affiliation | Combinatorial and Medicinal Chemistry Research, Infectious Diseases Research, Discovery Technologies, Pharmacia & Upjohn, Inc., Kalamazoo, Michigan 49001, USA. michael.j.genin@am.pnu.com | lld:pubmed |
| pubmed-article:10715167 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:10715167 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10715167 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:10715167 | lld:pubmed |
