- Investigation of the pharmacophore space of Severe Acute Respiratory Syndrome coronavirus (SARS-CoV) NTPase/helicase by dihydroxychromone derivatives
[作者:Lee, C; Lee, JM; Lee, NR; Kim, DE; Jeong, YJ; Chong, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4538-4541 , 文章类型: Article,,卷期:2009年19-16]
- Aryl diketoacids have been identified as the first SARS-CoV NTPase/helicase inhibitors with a distinct pharmacophore featuring an arylmethyl group attached to a diketoacid. In order to search for the pharmacophore space ...
- Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: Relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity
[作者:Wang, XF; Creek, DJ; Schiaffo, CE; Dong, YX; Chollet, J; Scheurer, C; Wittlin, S; Charman, SA; Dussault, PH; Wood, JK; Vennerstrom, JL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4542-4545 , 文章类型: Article,,卷期:2009年19-16]
- These data suggest that iron(II) reactivity for a set of homologous spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane peroxide heterocycles is a necessary, but insufficient, property of animalarial pe...
- 3,4-Disubstituted benzofuran P1 ' MMP-13 inhibitors: Optimization of selectivity and reduction of protein binding
[作者:Li, W; Hu, YH; Li, JC; Thomason, JR; DeVincentis, D; Du, XM; Wu, JJ; Hotchandani, R; Rush, TS; Skotnicki, JS; Tam, S; Chockalingam, PS; Morris, EA; Levin, JI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4546-4550 , 文章类型: Proceedings Paper,,卷期:2009年19-16]
- Potent 3,4-disubstituted benzofuran P1' MMP-13 inhibitors have been prepared. Selectivity over MMP-2 was achieved through a substituent at the C4 position of the benzofuran P1' moiety of the molecule. By replacing a back...
- Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents
[作者:Chekler, ELP; Butera, JA; Di, L; Swillo, RE; Morgan, GA; Rossman, EI; Huselton, C; Larsen, BD; Hennan, JK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4551-4554 , 文章类型: Article,,卷期:2009年19-16]
- In an effort to discover potent, orally bioavailable compounds for the treatment of atrial fibrillation (AF) and ventricular tachycardia (VT), we developed a class of gap-junction modifiers typified by GAP-134 (1, R-1 = ...
- The P-1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
[作者:Yamaguchi, Y; Menear, K; Cohen, NC; Mah, R; Cumin, F; Schnell, C; Wood, JM; Maibaum, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4863-4867 , 文章类型: Article,,卷期:2009年19-16]
- Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P-1 motif were designed based on initial lead structures 1 and aliskiren (2). (P-3-P-1)-Benzamide derivatives such as 9a and 34, as well as the corr...
- Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5)
[作者:Li, XZ; Wang, LL; Long, L; Xiao, JH; Hu, YD; Li, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4868-4872 , 文章类型: Article,,卷期:2009年19-16]
- Two series of nitrogenous heterocycle compounds-1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles have been synthesized and evaluated for their ALK5 inhibitory activity and cytotoxicity in TGF beta-Smad2...
- Synthesis and evaluation of novel F-18 labeled fluoroarylvaline derivatives: Potential PET imaging agents for tumor detection
[作者:Qiao, YL; He, Y; Zhang, ST; Li, GX; Liu, H; Xu, JL; Wang, X; Qi, CM; Peng, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4873-4877 , 文章类型: Article,,卷期:2009年19-16]
- Two F-18 labeled fluoroarylvaline derivatives, methyl 2-(2-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoate ([F-18]1, [F-18]MFNBMB) and its corresponding acid 2-(2-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoic acid ([F...
- Benzothiophene inhibitors of MK2. Part 1: Structure-activity relationships, assessments of selectivity and cellular potency
[作者:Anderson, DR; Meyers, MJ; Kurumbail, RG; Caspers, N; Poda, GI; Long, SA; Pierce, BS; Mahoney, MW; Mourey, RJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4878-4881 , 文章类型: Article,,卷期:2009年19-16]
- Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular poten...
- Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency
[作者:Anderson, DR; Meyers, MJ; Kurumbail, RG; Caspers, N; Poda, GI; Long, SA; Pierce, BS; Mahoney, MW; Mourey, RJ; Parikh, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4882-4884 , 文章类型: Article,,卷期:2009年19-16]
- Optimization of kinase selectivity for a set of benzothiophene MK2 inhibitors provided analogs with potencies of less than 500 nM in a cell based assay. The selectivity of the inhibitors can be rationalized by examinatio...
- Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists
[作者:Didiuk, MT; Griffith, DA; Benbow, JW; Liu, KKC; Walker, DP; Bi, FC; Morris, J; Guzman-Perez, A; Gao, H; Bechle, BM; Kelley, RM; Yang, XJ; Dirico, K; Ahmed, S; Hungerford, W; DiBrinno, J; Zawistoski, MP; Bagley, SW; Li, JK; Zeng, Y; Santucci, S; Oliver, R; Corbett, M; Olson, T; Chen, CL; Li, M; Paralkar, VM; Riccardi, KA; Healy, DR; Kalgutkar, AS; Maurer, TS; Nguyen, HT; Frederick, KS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4555-4559 , 文章类型: Article,,卷期:2009年19-16]
- Synthesis and structure-activity relationship (SAR) studies on 5-trifluoromethylpyrido[4,3-d] pyrimidin-4(3H)-ones, a novel class of calcium receptor antagonists is described with particular emphasis on optimization of t...
- Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD
[作者:Wan, ZH; Laine, DI; Yan, HX; Zhu, CJ; Widdowson, KL; Buckley, PT; Burman, M; Foley, JJ; Sarau, HM; Schmidt, DB; Webb, EF; Belmonte, KE; Palovich, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4560-4562 , 文章类型: Article,,卷期:2009年19-16]
- Design and syntheses of a novel series of muscarinic antagonists are reported. These efforts have culminated in the discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide (4...
- The discovery of azepane sulfonamides as potent 11 beta-HSD1 inhibitors
[作者:Neelamkavil, SF; Boyle, CD; Chackalamannil, S; Greenlee, WJ; Zhang, LL; Terracina, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4563-4565 , 文章类型: Article,,卷期:2009年19-16]
- Discovery of a series of azepine sulfonamides as potent inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discov...
- Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors
[作者:Chioua, M; Samadi, A; Soriano, E; Lozach, O; Meijer, L; Marco-Contelles, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4566-4569 , 文章类型: Article,,卷期:2009年19-16]
- The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b] pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kina...
- Synthesis and evaluation of novel substituted 5-hydroxycoumarin and pyranocoumarin derivatives exhibiting significant antiproliferative activity against breast cancer cell lines
[作者:Mao, WW; Wang, TT; Zeng, HP; Wang, ZY; Chen, JP; Shen, JG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4570-4573 , 文章类型: Article,,卷期:2009年19-16]
- A library of novel 5-hydroxycoumarin and pyranocoumarin derivatives was constructed via silica sulfuric acid-catalyzed pechmann reaction and Pd(0)-catalyzed suzuki coupling in tandem, and their antiproliferative activiti...
- The discovery of a structurally novel class of inhibitors of the type 1glycine transporter (vol 19, pg 2974, 2009)
[作者:Lowe, JA; Hou, XJ; Schmidt, C; Tingley, FD; McHardy, S; Kalman, M; DeNinno, S; Sanner, M; Ward, K; Lebel, L; Tunucci, D; Valentine, J; Bronk, BS; Schaeffer, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4885-4885 , 文章类型: Correction,,卷期:2009年19-16]
-
- Bis-neonicotinoid insecticides: Observed and predicted binding interactions with the nicotinic receptor (vol 19, pg 3449, 2009)
[作者:Ohno, I; Tomizawa, M; Durkin, KA; Casida, JE; Kagabu, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4886-4886 , 文章类型: Correction,,卷期:2009年19-16]
-
|