- The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
[作者:Harrington, PE; Jean, DJS; Clarine, J; Coulter, TS; Croghan, M; Davenport, A; Davis, J; Ghiron, C; Hutchinson, J; Kelly, MG; Lott, F; Lu, JYL; Martin, D; Morony, S; Poon, SF; Portero-Larragueta, E; Reagan, JD; Regal, KA; Tasker, A; Wang, MH; Yang, YH; Yao, GM; Zeng, QP; Henley, C; Fotsch, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5544-5547 , 文章类型: Article,,卷期:2010年20-18]
- The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in ...
- Discovery of biphenylketones as dual modulators of inflammation and bone loss
[作者:Greig, IR; Coste, E; Ralston, SH; van't Hof, RJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5548-5551 , 文章类型: Article,,卷期:2010年20-18]
- Biphenylketones were identified as novel inhibitors of NF kappa B activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 mu M), showed oral...
- Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach
[作者:Mony, L; Triballeau, N; Paoletti, P; Acher, FC; Bertrand, HO,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5552-5558 , 文章类型: Article,,卷期:2010年20-18]
- We report the identification of a novel NR2B-selective NMDAR antagonist with an original scaffold, LSP10-0500. This compound was identified by a virtual high-throughput screening approach on the basis of a quantitative p...
- Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain
[作者:Lucas, MC; Weikert, RJ; Carter, DS; Cai, HY; Greenhouse, R; Iyer, PS; Lin, CJ; Lee, EK; Madera, AM; Moore, A; Ozboya, K; Schoenfeld, RC; Steiner, S; Zhai, YS; Lynch, SM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5559-5566 , 文章类型: Article,,卷期:2010年20-18]
- Two new series of monoamine triple reuptake inhibitors (TRIs) have been discovered through scaffold homologation of our recently reported series of 3,3-disubstituted pyrrolidine TRIs. The regioisomeric 2- and 3-ketopyrro...
- Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
[作者:Lee, KH; Park, CE; Min, KH; Shin, YJ; Chung, CM; Kim, HH; Yoon, HJ; Won-Kim; Ryu, EJ; Shin, YJ; Nam, HS; Cho, JW; Lee, HY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5567-5571 , 文章类型: Article,,卷期:2010年20-18]
- A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug intera...
- Synthesis and antimicrobial activity of novel fluorine containing 4-(substituted-2-hydroxybenzoyl)-1H-pyrazoles and pyrazolyl benzo[d]oxazoles
[作者:Gadakh, AV; Pandit, C; Rindhe, SS; Karale, BK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5572-5576 , 文章类型: Article,,卷期:2010年20-18]
- A series of fluorine containing 4-(substituted-2-hydroxybenzoyl) pyrazoles and pyrazolyl benzo[d]oxazoles were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, P...
- Lanostane triterpenes from Ganoderma lucidum suppress the adipogenesis in 3T3-L1 cells through down-regulation of SREBP-1c
[作者:Lee, I; Kim, J; Ryoo, I; Kim, Y; Choo, S; Yoo, I; Min, B; Na, M; Hattori, M; Bae, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5577-5581 , 文章类型: Article,,卷期:2010年20-18]
- Several lanostane triterpenes [butyl ganoderate A (1), butyl ganoderate B (2), butyl lucidenate N (3), and butyl lucidenate A (4)] bearing a butyl ester side chain from the fruiting bodies of Ganoderma lucidum exhibited ...
- Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors (vol 20, pg 3606, 2010)
[作者:Mohamed, T; Rao, PPN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5582-5582 , 文章类型: Correction,,卷期:2010年20-18]
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- A novel sesquiterpene quinone from Hainan sponge Dysidea villosa (vol 19, pg 390, 2009)
[作者:Li, Y; Zhang, Y; Shen, X; Guo, YW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5583-5583 , 文章类型: Correction,,卷期:2010年20-18]
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- Japonicones A-D, bioactive dimeric sesquiterpenes from Inula japonica Thunb. (vol 19, pg 710, 2009)
[作者:Qin, JJ; Jin, HZ; Fu, JJ; Hu, XJ; Wang, Y; Yan, SK; Zhang, WD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5584-5584 , 文章类型: Correction,,卷期:2010年20-18]
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- Semisynthesis and pharmacological activities of thyroxine analogs: Development of new angiogenesis modulators (vol 20, pg 3394, 2010)
[作者:Bridoux, A; Cui, HD; Dyskin, E; Schmitzer, AR; Yalcin, M; Mousa, SA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5585-5585 , 文章类型: Correction,,卷期:2010年20-18]
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- Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands
[作者:Jean, M; Renault, J; Levoin, N; Danvy, D; Calmels, T; Berrebi-Bertrand, I; Robert, P; Schwartz, JC; Lecomte, JM; Uriac, P; Capet, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5376-5379 , 文章类型: Article,,卷期:2010年20-18]
- Isosteric replacement of the amide function and modulation of the arylpiperazine moiety of known dopamine D3 receptor ligands led to potent and selective compounds. Enhanced bioavailability and preferential brain distrib...
- Iminoheterocycles as gamma-secretase modulators
[作者:Caldwell, JP; Bennett, CE; McCracken, TM; Mazzola, RD; Bara, T; Buevich, A; Burnett, DA; Chu, I; Cohen-Williams, M; Josein, H; Hyde, L; Lee, J; McKittrick, B; Song, LX; Terracina, G; Voigt, J; Zhang, LL; Zhu, ZN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5380-5384 , 文章类型: Article,,卷期:2010年20-18]
- The synthesis of a novel series of iminoheterocycles and their structure-activity relationship (SAR) as modulators of gamma-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a s...
- Lactarane sesquiterpenoids from Lactarius subvellereus and their cytotoxicity
[作者:Kim, KH; Noh, HJ; Choi, SU; Park, KM; Seok, SJ; Lee, KR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5385-5388 , 文章类型: Article,,卷期:2010年20-18]
- Subvellerolactones B (1), D (2), and E (3), structurally unusual lactarane sesquiterpenoids, were isolated from the fruiting bodies of Lactarius subvellereus together with four known lactarane sesquiterpenes (4-7). The c...
- Synthesis, proapoptotic screening, and structure-activity relationships of novel aza-lupane triterpenoids
[作者:Mar, AA; Szotek, EL; Koohang, A; Flavin, WP; Eiznhamer, DA; Flavin, MT; Xu, ZQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5389-5393 , 文章类型: Article,,卷期:2010年20-18]
- Apoptosis is a highly regulated process by which excessive cells are eliminated in order to maintain normal cell development and tissue homeostasis. Resistance to apoptosis often contributes to failure in cancer preventi...
- Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists
[作者:Letourneau, JJ; Riviello, CM; Li, H; Cole, AG; Ho, KK; Zanetakos, HA; Desai, H; Zhao, JQ; Auld, DS; Napier, SE; Thomson, FJ; Goan, KA; Morphy, JR; Ohlmeyer, MHJ; Webb, ML,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5394-5397 , 文章类型: Article,,卷期:2010年20-18]
- The discovery, synthesis, and preliminary structure-activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse...
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