- Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain
[作者：Meyers, MJ; Long, SA; Pelc, MJ; Wang, JL; Bowen, SJ; Schweitzer, BA; Wilcox, MV; McDonald, J; Smith, SE; Foltin, S; Rumsey, J; Yang, YS; Walker, MC; Kamtekar, S; Beidler, D; Thorarensen, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6545-6553 , 文章类型： Article，,卷期：2011年21-21]
- Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase responsible for the degradation of fatty acid amide signaling molecules such as endocannabinoid anandamide (AEA), which has been shown to possess...
- Aminothiazoles as gamma-secretase modulators
[作者：Lubbers, T; Flohr, A; Jolidon, S; David-Pierson, P; Jacobsen, H; Ozmen, L; Baumann, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6554-6558 , 文章类型： Article，,卷期：2011年21-21]
- We herein report the discovery of a new c-secretase modulator class with an aminothiazole core starting from a HTS hit (3). Synthesis and SAR of this series are discussed. These novel compounds demonstrate moderate to go...
- Synthesis and biological evaluation of some novel triazol-3-ones as antimicrobial agents
[作者：Pardeshi, S; Bobade, VD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6559-6562 , 文章类型： Article，,卷期：2011年21-21]
- A new series of triazol-3-one derivatives bearing 4-methyl-4H-thieno[3',2': 5,6] thiopyrano [4,3-d][1,3] thiazolyl or 4-(thiophene-3-yl) thiazolyl moiety at 4-position and alkyl substitution at 2-position are synthesized...
- Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties
[作者：Korabecny, J; Musilek, K; Zemek, F; Horova, A; Holas, O; Nepovimova, E; Opletalova, V; Hroudova, J; Fisar, Z; Jung, YS; Kuca, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6563-6566 , 文章类型： Article，,卷期：2011年21-21]
- Cholinesterase inhibitors are, so far, the only successful strategy for the symptomatic treatment of Alzheimer's disease. Tacrine (THA) is a potent acetylcholinesterase inhibitor that was used in the treatment of Alzheim...
- New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam
[作者：Bihel, FJJ; Justiniano, H; Schmitt, M; Hellal, M; Ibrahim, MA; Lugnier, C; Bourguignon, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6567-6572 , 文章类型： Article，,卷期：2011年21-21]
- Pharmacophoric comparison between papaverine and tofisopam led to identify three new series of micro- to sub-micromolar inhibitors of phosphodiesterase-4, including 7,8-dialkoxy-2,3-benzodiazepin-4-one derivatives, 7,8-d...
- Novel 1-alkynyl substituted 1,2-dihydroquinoline derivatives from nimesulide (and their 2-oxo analogues): A new strategy to identify inhibitors of PDE4B
[作者：Pal, S; Durgadas, S; Nallapati, SB; Mukkanti, K; Kapavarapu, R; Meda, CLT; Parsa, KVL; Pal, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6573-6576 , 文章类型： Article，,卷期：2011年21-21]
- A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesize...
- Tricyclic aminopyrimidine histamine H(4) receptor antagonists
[作者：Savall, BM; Gomez, L; Chavez, F; Curtis, M; Meduna, SP; Kearney, A; Dunford, P; Cowden, J; Thurmond, RL; Grice, C; Edwards, JP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6577-6581 , 文章类型： Article，,卷期：2011年21-21]
- This report discloses the development of a series of tricyclic histamine H(4) receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigat...
- BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells
[作者：Choi, HE; Yoo, MS; Choi, JH; Lee, JY; Kim, JH; Kim, JH; Lee, JK; Kim, GI; Park, Y; Chi, YH; Paik, SH; Lee, JH; Lee, KT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6236-6241 , 文章类型： Article，,卷期：2011年21-21]
- Anti-angiogenesis is regarded as an effective strategy for cancer treatment, and vascular endothelial growth factor (VEGF) plays a key role in the regulations of angiogenesis and vasculogenesis. In the present study, the...
- Stable and orally bio-available pro-drugs of CPS11
[作者：Huo, AH; Zhang, HS; Guan, YB; Zeng, GH; Chen, YW; Li, XW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6242-6244 , 文章类型： Article，,卷期：2011年21-21]
- Stable and orally bio-available pro-drugs of CPS11 were synthesized. They are active on human umbilical vein endothelial cell proliferation assay and tube formation assay. The therapeutic efficacy and safety of 4 as a si...
- Synthesis and evaluation of cytotoxic effects of hanultarin and its derivatives
[作者：Lee, E; Ahamed, VSJ; Kumar, MS; Rhee, SW; Moon, SS; Hong, IS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6245-6248 , 文章类型： Article，,卷期：2011年21-21]
- One of the known cytotoxic lignans is (-)-1-O-feruloyl-secoisolariciresinol designated as hanultarin, which was isolated from the seeds of Trichosanthes kirilowii. In this Letter, we described the first synthesis of 1-O-...
- Design and synthesis of a library of chemokine antagonists
[作者：Bhalay, G; Albrecht, B; Akhlaq, M; Baettig, U; Beer, D; Brown, Z; Charlton, S; Dunstan, A; Bradley, M; Gedeck, P; Glen, A; Howe, T; Keller, T; Leighton-Davies, J; Li, A; McCarthy, C; Mocquet, C; Owen, C; Nicklin, P; Rosethorne, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6249-6252 , 文章类型： Article，,卷期：2011年21-21]
- A library of chemokine antagonists has been synthesized using a combination of solid and solution-phase chemistry. Structures of known chemokine antagonists were used to produce a pharmacophore which served to guide mono...
- Indolin-2-one p38 alpha inhibitors III: Bioisosteric amide replacement
[作者：Eastwood, P; Gonzalez, J; Gomez, E; Caturla, F; Aguilar, N; Mir, M; Aiguade, J; Matassa, V; Balague, C; Orellana, A; Dominguez, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6253-6257 , 文章类型： Article，,卷期：2011年21-21]
- Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38 alpha inhibitors which showed general hydrolytic in...
- Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis
[作者：Kim, KH; Maderna, A; Schnute, ME; Hegen, M; Mohan, S; Miyashiro, J; Lin, L; Li, E; Keegan, S; Lussier, J; Wrocklage, C; Nickerson-Nutter, CL; Wittwer, AJ; Soutter, H; Caspers, N; Han, S; Kurumbail, R; Dunussi-Joannopoulos, K; Douhan, J; Wissner, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6258-6263 , 文章类型： Article，,卷期：2011年21-21]
- Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton's tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure ...
- Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors
[作者：Qian, YM; Ahmad, M; Chen, SQ; Gillespie, P; Le, N; Mennona, F; Mischke, S; So, SS; Wang, H; Burghardt, C; Tannu, S; Conde-Knape, K; Kochan, J; Bolin, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6264-6269 , 文章类型： Article，,卷期：2011年21-21]
- Through high throughput screening and subsequent hit identification and optimization, we synthesized a series of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as the first reported potent and reversible GFAT inhib...
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