- Steroidal C-21 mercapto derivatives as dissociated steroids: Discovery of an inhaled dissociated steroid
[作者:Biju, P; McCormick, K; Aslanian, R; Berlin, M; Solomon, D; Chapman, R; McLeod, R; Prelusky, D; Eckel, S; Kelly, G; Natiello, M; House, A; Fernandez, X; Bitar, R; Phillips, J; Anthes, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6343-6347 , 文章类型: Article,,卷期:2011年21-21]
- A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated...
- Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region
[作者:Hughes, RO; Maddux, T; Rogier, DJ; Lu, SR; Walker, JK; Jacobsen, EJ; Rumsey, JM; Zheng, Y; MacInnes, A; Bond, BR; Han, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6348-6352 , 文章类型: Article,,卷期:2011年21-21]
- We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pha...
- Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H(3) receptor antagonists with robust wake-promoting activity
[作者:Dandu, RR; Gruner, JA; Mathiasen, JR; Aimone, LD; Hostetler, G; Benfield, C; Bendesky, RJ; Marcy, VR; Raddatz, R; Hudkins, RL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6362-6365 , 文章类型: Article,,卷期:2011年21-21]
- A series of pyridazinone-phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H(3)R are described. These analogs exhibited excellent selectivity and metabolic stability, with acceptable ra...
- Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
[作者:Nishiguchi, GA; Atallah, G; Bellamacina, C; Burger, MT; Ding, Y; Feucht, PH; Garcia, PD; Han, W; Klivansky, L; Lindvall, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6366-6369 , 文章类型: Article,,卷期:2011年21-21]
- A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a pr...
- Synthesis, iron(III)-binding affinity and in vitro evaluation of 3-hydroxypyridin-4-one hexadentate ligands as potential antimicrobial agents
[作者:Xu, B; Kong, XL; Zhou, T; Qiu, DH; Chen, YL; Liu, MS; Yang, RH; Hider, RC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6376-6380 , 文章类型: Article,,卷期:2011年21-21]
- Iron is a critical element for the survival of bacteria. We have designed and synthesized two novel 3-hydroxypyridin-4-one hexadentate ligands with high affinity for iron(III), which disrupt bacterial iron absorption. Bi...
- Discovery of a novel series of cyclic urea as potent CCR5 antagonists
[作者:Duan, MS; Kazmierski, WM; Tallant, M; Jun, JH; Edelstein, M; Ferris, R; Todd, D; Wheelan, P; Xiong, ZP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6381-6385 , 文章类型: Article,,卷期:2011年21-21]
- A novel series of cyclic urea-based CCR5 antagonists was designed aiming to resolve instability issue in the fasted simulated intestinal fluid (FSIF) associated with the acyclic urea moiety in 1. This class of CCR5 compo...
- Antitumor dinuclear platinum(II) complexes derived from a novel chiral ligand
[作者:Gao, CZ; Xu, G; Gou, SH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6386-6388 , 文章类型: Article,,卷期:2011年21-21]
- A new chiral ligand, 2-(((1R,2R)-2-aminocyclohexyl) amino) acetic acid (HL), was designed and synthesized to prepare a series of novel dinuclear platinum(II) complexes with dicarboxylates or sulfate as bridges. The evalu...
- Design, synthesis, and biological evaluation of benzodiazepine-based SUMO-specific protease 1 inhibitors
[作者:Qiao, ZT; Wang, WW; Wang, L; Wen, DH; Zhao, YX; Wang, Q; Meng, QQ; Chen, GQ; Wu, YL; Zhou, HC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6389-6392 , 文章类型: Article,,卷期:2011年21-21]
- As the best-characterized ubiquitin-like protein (UBL), small ubiquitin-related modifier (SUMO) was found to conjugate with a number of proteins to regulate cellular functions including transcription, signal transduction...
- Synthesis of novel N-(2-hydroxy-2-p-tolylethyl)-amide and N-(2-oxo-2-p-tolylethyl)-amide derivatives and their antidyslipidemic and antioxidant activity
[作者:Narender, T; Rajendar, K; Sarkar, S; Singh, VK; Chaturvedi, U; Khanna, AK; Bhatia, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6393-6397 , 文章类型: Article,,卷期:2011年21-21]
- In continuation of our drug discovery program on metabolic diseases, we identified an alkaloidal amide, that is, Aegeline (V) from the plant Aegle marmelos leaves as a dual acting agent (antihyperlipidemic and antihyperg...
- Micelles catalyzed chemoselective synthesis 'in water' and biological evaluation of oxygen containing hetero-1,4-naphthoquinones as potential antifungal agents
[作者:Tandon, VK; Maurya, HK; Mishra, NN; Shukla, PK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6398-6403 , 文章类型: Article,,卷期:2011年21-21]
- Various oxygen containing 1,4-naphthoquinone derivatives have been synthesized chemoselectively by an economical, viable green methodology approach using water as solvent with or without surfactants such as Triton X-100,...
- Homo- and hetero-dimers of inactive organophosphorous group binding at dual sites of AChE
[作者:Zhao, QF; Xie, RL; Zhang, T; Fang, J; Mei, XD; Ning, J; Tang, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6404-6408 , 文章类型: Article,,卷期:2011年21-21]
- Homo- and hetero-dimers of inactive organophosphorous group(s) dramatically enhanced the acetylcholinesterase (AChE; EC 3.1.1.7) inhibiting potency, with the highest potency observed at a tether length of 6 methylene gro...
- Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists
[作者:Fujimoto, T; Tomata, Y; Kunitomo, J; Hirozane, M; Marui, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6409-6413 , 文章类型: Article,,卷期:2011年21-21]
- To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine based scaffold was designed and a SAR study was carried out. Compound 4f possessed the highest OX2R antagonistic activity with an IC(50) val...
- Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists
[作者:Fujimoto, T; Kunitomo, J; Tomata, Y; Nishiyama, K; Nakashima, M; Hirozane, M; Yoshikubo, S; Hirai, K; Marui, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6414-6416 , 文章类型: Article,,卷期:2011年21-21]
- During our efforts to identify a series of potent, selective, orally active human Orexin-2 Receptor (OX2R) antagonists, we elucidated structure-activity relationship (SAR) on the 7-position of a benzoxazepine scaffold by...
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