- Synthesis, in vitro and in vivo evaluation of [C-11]MMTP: A potential PET ligand for mGluR1 receptors
[作者:Prabhakaran, J; Majo, VJ; Milak, MS; Kassir, SA; Palner, M; Savenkova, L; Mali, P; Arango, V; Mann, JJ; Parsey, RV; Kumar, JSD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3499-3501 , 文章类型: Article,,卷期:2010年20-12]
- Synthesis, in vitro and in vivo evaluation of [O-methyl-C-11]dimethylamino-3(4-methoxyphenyl)-3H-pyrido[ 30',20': 4,5]thieno[3,2-d]pyrimidin-4-one (1), a potential imaging agent for mGluR1 receptors using PET are describ...
- Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II)
[作者:Ye, XM; Konradi, AW; Smith, J; Aubele, DL; Garofalo, AW; Marugg, J; Neitzel, ML; Semko, CM; Sham, HL; Sun, MH; Truong, AP; Wu, J; Zhang, HB; Goldbach, E; Sauer, JM; Brigham, EF; Bova, M; Basi, GS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3502-3506 , 文章类型: Article,,卷期:2010年20-12]
- Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy. (C) 2010 Elsevier Ltd. A...
- Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors
[作者:Tang, GZ; Qiu, ZX; Lin, XF; Li, WT; Zhu, L; Li, SH; Li, HD; Wang, LS; Chen, L; Wu, JZ; Yang, WG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3507-3510 , 文章类型: Article,,卷期:2010年20-12]
- A novel class of HA inhibitors (4a) was identified based on ligand similarity search of known HA inhibitors. Parallel synthesis and further structural modifications resulted in 1-phenyl-cyclopentanecarboxylic acid (4-cya...
- Investigation of Beckett-Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology
[作者:Nagase, H; Imaide, S; Tomatsu, M; Hirayama, S; Nemoto, T; Sato, N; Nakajima, M; Nakao, K; Mochizuki, H; Gouda, H; Hirono, S; Fujii, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3801-3804 , 文章类型: Article,,卷期:2010年20-12]
- Novel naltrexone derivatives 7 and 8 with contracted and expanded D-rings were synthesized to investigate the importance of orientation of lone electron pair on the nitrogen for binding abilities to the opioid receptor. ...
- 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors
[作者:Yu, H; Jung, Y; Kim, H; Lee, J; Oh, CH; Yoo, KH; Sim, T; Hah, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3805-3808 , 文章类型: Article,,卷期:2010年20-12]
- The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds...
- New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists
[作者:Shinagawa, Y; Inoue, T; Hirata, K; Katsushima, T; Nakagawa, T; Matsuo, Y; Shindo, M; Hashimoto, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3809-3813 , 文章类型: Article,,卷期:2010年20-12]
- Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS ...
- Total synthesis of (+/-)-elegansidiol, (+/-)-farnesiferol B, and (+/-)-farnesiferol D
[作者:Yadav, JS; Satyanarayana, K; Sreedhar, P; Srihari, P; Shaik, TB; Kalivendi, SV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3814-3817 , 文章类型: Article,,卷期:2010年20-12]
- The racemic total synthesis of elegansidiol, farnesiferol B, and farnesiferol D has been obtained following a Diels-Alder approach. Gillman addition, cross metathesis reaction are the other key steps involved in the targ...
- Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors
[作者:Bennett, SNL; Campbell, AD; Hancock, A; Johnstone, C; Kenny, PW; Pickup, A; Plowright, AT; Selmi, N; Simpson, I; Stocker, A; Whalley, DP; Whittamore, PRO,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3511-3514 , 文章类型: Article,,卷期:2010年20-12]
- A series of carboxylic acid glycogen phosphorylase inhibitors, which have potential as oral antidiabetic agents, is described. Defining and applying simple physicochemical design criteria was used to assess the opportuni...
- Synthesis of the Cyanine 7 labeled neutrophil-specific agents for noninvasive near infrared fluorescence imaging
[作者:Xiao, L; Zhang, Y; Liu, ZQ; Yang, M; Pu, L; Pan, DF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3515-3517 , 文章类型: Article,,卷期:2010年20-12]
- A neutrophil-binding peptide, cinnamoyl-F(D)LF(D)LF (cFLFLF), was labeled with the near infrared (NIR) fluorophore, Cyanine 7 (Cy7). This construct was modified with a polyethylene glycol (PEG, M-W 3.4 kDa) moiety in ord...
- Potent antimicrobial activity of 3-(4,5-diaryl-1H-imidazol-2-yl)-1H-indole derivatives against methicillin-resistant Staphylococcus aureus
[作者:Al-Qawasmeh, RA; Huesca, M; Nedunuri, V; Peralta, R; Wright, J; Lee, Y; Young, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3518-3520 , 文章类型: Article,,卷期:2010年20-12]
- A new series of antimicrobial derivatives [3-(4,5-diaryl-1H-imidazol-2-yl)-1H-indole)] have been synthesized with potent activity against strains of Staphylococcus aureus, including methicillin-resistant strains (MRSA). ...
- Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
[作者:Cho, TP; Gang, LZ; Long, YF; Yang, W; Qian, W; Lei, Z; Jing, LJ; Ying, F; Ke, YP; Ying, L; Jun, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3521-3525 , 文章类型: Article,,卷期:2010年20-12]
- A series of novel bicyclo[3.3.0]octane derivatives have been synthesized and found to be dipeptidyl peptidase 4 (DPP-4) inhibitors. Compounds 10a and 10b demonstrate good efficacies in oral glucose tolerance tests. (C) 2...
- The oxidation of 8-oxo-7,8-dihydroguanine by iodine
[作者:Kino, K; Morikawa, M; Kobayashi, T; Kobayashi, T; Komori, R; Sei, Y; Miyazawa, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3818-3820 , 文章类型: Article,,卷期:2010年20-12]
- 8-Oxo-7,8-dihydroguanine was specifically oxidized by iodine with aqueous KI. Under acidic conditions, the major product was dehydro-guanidinohydantoin. Under basic conditions, two diastereoisomers of spirohydantoin were...
- Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKK beta inhibitors
[作者:Crombie, AL; Sum, FW; Powell, DW; Hopper, DW; Torres, N; Berger, DM; Zhang, YX; Gavriil, M; Sadler, TM; Arndt, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3821-3825 , 文章类型: Article,,卷期:2010年20-12]
- A series of tricyclic anilinopyrimidines were synthesized and evaluated as IKK beta inhibitors. Several analogues, including tricyclic phenyl (10, 18a, 18c, 18d, and 18j) and thienyl (26 and 28) derivatives were shown to...
- Two new asterosaponins, archasterosides A and B, from the Vietnamese starfish Archaster typicus and their anticancer properties
[作者:Kicha, AA; Ivanchina, NV; Huong, TTT; Kalinovsky, AI; Dmitrenok, PS; Fedorov, SN; Dyshlovoy, SA; Long, PQ; Stonik, VA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3826-3830 , 文章类型: Article,,卷期:2010年20-12]
- New asterosaponins archasterosides A (1), B (2), and the known regularoside A (3) were isolated from the Vietnamese starfish Archaster typicus and structurally elucidated by extensive NMR techniques and chemical transfor...
- Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2 alpha (HRI) kinase (vol 19, 6548, 2009)
[作者:Rosen, MD; Woods, CR; Goldberg, SD; Hack, MD; Bounds, AD; Yang, Y; Wagaman, PC; Phuong, VK; Ameriks, AP; Barrett, TD; Kanelakis, KC; Chuang, JC; Shankley, NP; Rabinowitz, MH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3834-3834 , 文章类型: Correction,,卷期:2010年20-12]
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