排序方式: 共有114条查询结果,搜索用时 15 毫秒
1.
2.
3.
Angus R. Brown Maryanne Covington Robert C. Newton Robert Ramage Patricia Welch 《Journal of peptide science》1996,2(1):40-46
The affinity-based Nα-amino protecting group tetrabenzo [a,c,g,i]fluorenyl-17-methoxycarbonyl (Tbfmoc) has been utilized as a hydrophobic probe to allow the simple, quick and highly effective isolation of a 76 residue cysteine-containing protein (MCP-1). The base-labile Tbfmoc group can be removed under very mild conditions, which preserve the thiol-con taining protein in the reduced state. Oxidative folding was then used to furnish the biologically active β-chemokine MCP-1. 相似文献
4.
Varnes JG Gardner DS Santella JB Duncia JV Estrella M Watson PS Clark CM Ko SS Welch P Covington M Stowell N Wadman E Davies P Solomon K Newton RC Trainor GL Decicco CP Wacker DA 《Bioorganic & medicinal chemistry letters》2004,14(7):1645-1649
The discovery of novel and selective small molecule antagonists of the CC Chemokine Receptor-3 (CCR3) is presented. Simple conversion from a 4- to 3-benzylpiperidine gave improved selectivity for CCR3 over the serotonin 5HT(2A) receptor. Chiral resolution and exploration of mono- and disubstitution of the N-propylurea resulted in several 3-benzylpiperidine N-propylureas with CCR3 binding IC(50)s under 5 nM. Data from in vitro calcium mobilization and chemotaxis assays for these compounds ranged from high picomolar to low nanomolar EC(50)s and correlated well with antagonist binding IC(50)s. 相似文献
5.
Acute toxoplasmosis was diagnosed in 2 captive dik-dik (Madoqua guentheri smithi) in the Houston Zoo. Both animals became ill suddenly and died in spite of supportive therapy. Toxoplasma gondii was identified in tissues of both animals immunohistochemically, and antibodies to T. gondii were found in titers of 1:800 or more in both animals upon examination by the modified agglutination rest. The cause of death was considered to be toxoplasmic pneumonia. This is the first report of toxoplasmosis in M. g. smithi. 相似文献
6.
Wacker DA Santella JB Gardner DS Varnes JG Estrella M DeLucca GV Ko SS Tanabe K Watson PS Welch PK Covington M Stowell NC Wadman EA Davies P Solomon KA Newton RC Trainor GL Friedman SM Decicco CP Duncia JV 《Bioorganic & medicinal chemistry letters》2002,12(13):1785-1789
CCR3 antagonist leads with IC(50) values in the microM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl-n-propylureas and erythro-3-(4-benzyl-2-(alpha-hydroxyalkyl)piperidin-1-yl)-n-propylureas (obtained via Beak reaction of N-BOC-4-benzylpiperidine) exhibited single digit nanomolar IC(50) values for CCR3. 相似文献
7.
Daniel?J.?KrugerEmail author Maryanne?Fisher Ian?Jobling 《Human nature (Hawthorne, N.Y.)》2003,14(3):305-317
Empirical tests described in this article support hypotheses derived from evolutionary theory on the perceptions of literary
characters. The proper and dark heroes in British Romantic literature of the late eighteenth and early nineteenth centuries
respectively represent long-term and short-term mating strategies. Recent studies indicate that for long-term relationships,
women seek partners with the ability and willingness to sustain paternal investment in extended relationships. For short-term
relationships, women choose partners whose features indicate high genetic quality. In hypothetical scenarios, females preferred
proper heroes for long-term relationships. The shorter the relationship under consideration, the more likely women were to
choose dark heroes as partners. 相似文献
8.
Xue CB He X Roderick J Corbett RL Duan JJ Liu RQ Covington MB Qian M Ribadeneira MD Vaddi K Christ DD Newton RC Trzaskos JM Magolda RL Wexler RR Decicco CP 《Bioorganic & medicinal chemistry letters》2003,13(24):4299-4304
Modifications of the lead TACE inhibitor 1 (N-hydroxy-trans-2-[[4-(4-quinolinyloxymethyl)anilinyl]carbonyl]-1-cyclohexanecarboxamide) at the cyclohexyl ring and the quinoline moiety led to the identification of a series of piperidine containing TACE inhibitors with potent activity in the inhibition of TNF-alpha release in the whole blood assay (WBA). The most potent analogue IM491 [N-hydroxy-(5S,6S)-1-methyl-6-[[4-(2-methyl-4-quinolinylmethoxy)anilinyl]carbonyl]-5-piperidinecarboxamide] exhibited an IC(50) value of 20 nM in WBA with excellent selectivity over MMP-1, -2 and -9 and is orally bioavailable with an F value of 43% in beagle dogs. 相似文献
9.
Sheppeck JE Gilmore JL Yang A Chen XT Xue CB Roderick J Liu RQ Covington MB Decicco CP Duan JJ 《Bioorganic & medicinal chemistry letters》2007,17(5):1413-1417
A series of novel hydantoins was designed and synthesized as structural alternatives to hydroxamate inhibitors of TACE. 5-Mono- and di-substituted hydantoins exhibited activity with IC50 values of 11-60 nM against porcine TACE in vitro and excellent selectivity against other MMPs. 相似文献
10.
Pruitt JR Batt DG Wacker DA Bostrom LL Booker SK McLaughlin E Houghton GC Varnes JG Christ DD Covington M Das AM Davies P Graden D Kariv I Orlovsky Y Stowell NC Vaddi KG Wadman EA Welch PK Yeleswaram S Solomon KA Newton RC Decicco CP Carter PH Ko SS 《Bioorganic & medicinal chemistry letters》2007,17(11):2992-2997
DPC168, a benzylpiperidine-substituted aryl urea CCR3 antagonist evaluated in clinical trials, was a relatively potent inhibitor of the 2D6 isoform of cytochrome P-450 (CYP2D6). Replacement of the cyclohexyl central ring with saturated heterocycles provided potent CCR3 antagonists with improved selectivity against CYP2D6. The favorable preclinical profile of DPC168 was maintained in an acetylpiperidine derivative, BMS-570520. 相似文献