- Discovery of diphenylmethane analogs as anti-bovine diarrhea viral agents
[作者:Hosoda, S; Aoyama, H; Goto, Y; Salim, MTA; Okamoto, M; Hashimoto, M; Baba, M; Hashimoto, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3157-3161 , 文章类型: Article,,卷期:2009年19-12]
- Based on antiviral screening of our diphenylmethane derivatives prepared as steroid substitutes, we identified a 1,1-diphenylcyclobutane analog (9) and two diethyldiphenylsilane analogs (12 and 13) as superior lead compo...
- Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors
[作者:Zebardast, T; Zarghi, A; Daraie, B; Hedayati, M; Dadrass, OG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3162-3165 , 文章类型: Article,,卷期:2009年19-12]
- A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro CO...
- Carbonic anhydrase inhibitors. Phenacetyl-, pyridylacetyl- and thienylacetyl-substituted aromatic sulfonamides act as potent and selective isoform VII inhibitors
[作者:Guzel, O; Innocenti, A; Scozzafava, A; Salman, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3170-3173 , 文章类型: Article,,卷期:2009年19-12]
- A series of aromatic/heterocyclic sulfonamides incorporating phenyl(alkyl), halogenosubstituted-phenylor 1,3,4-thiadiazole-sulfonamide moieties and thienylacetamido; phenacetamido- and pyridinylacetamido tails were prepa...
- Discovery of selective PDE4B inhibitors
[作者:Naganuma, K; Omura, A; Maekawara, N; Saitoh, M; Ohkawa, N; Kubota, T; Nagumo, H; Kodama, T; Takemura, M; Ohtsuka, Y; Nakamura, J; Tsujita, R; Kawasaki, K; Yokoi, H; Kawanishi, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3174-3176 , 文章类型: Article,,卷期:2009年19-12]
- In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a goo...
- Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: Retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct detection using linear ion trap/orbitrap mass spectrometry
[作者:Sun, H; Sharma, R; Bauman, J; Walker, DP; Aspnes, GE; Zawistoski, MP; Kalgutkar, AS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3177-3182 , 文章类型: Article,,卷期:2009年19-12]
- Previous studies have demonstrated the CYP3A4 mediated oxidation of the 5-aminooxindole motif, present in the trifluoromethylpyrimidine class of PYK-2 inhibitors, to a reactive bis-imine species, which can be trapped wit...
- Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists
[作者:Ivachtchenko, AV; Frolov, EB; Mitkin, OD; Kysil, VM; Khvat, AV; Okun, IM; Tkachenko, SE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3183-3187 , 文章类型: Article,,卷期:2009年19-12]
- Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon (TM) are described. Among the studied compounds, gamma-carbolines 3{8} and 3{14} have been ...
- Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay
[作者:Xu, WJ; Chen, G; Liew, OW; Zuo, ZL; Jiang, HL; Zhu, WL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3188-3192 , 文章类型: Article,,卷期:2009年19-12]
- This Letter describes an efficient approach by integrating virtual screening with bioassay technology for finding small organic inhibitors targeting beta-secretase (BACE-1). Fifteen hits with inhibitory potencies ranging...
- Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents
[作者:Dong, XW; Qi, LL; Jiang, CY; Chen, J; Wei, EQ; Hu, YZ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3196-3198 , 文章类型: Article,,卷期:2009年19-12]
- A series of prenylflavonoids with multiple hydroxyl groups were synthesized and evaluated for their vasorelaxant activities against rat aorta rings pre-contracted by phenylephrine (PE), as well as their neuroprotective e...
- Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain
[作者:Sasikumar, TK; Qiang, L; Burnett, DA; Greenlee, WJ; Li, C; Heimark, L; Pramanik, B; Grilli, M; Bertorelli, R; Lozza, G; Reggiani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3199-3203 , 文章类型: Article,,卷期:2009年19-12]
- Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Comp...
- Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype
[作者:Rodriguez, AL; Williams, R; Zhou, Y; Lindsley, SR; Le, U; Grier, MD; Weaver, CD; Conn, PJ; Lindsley, CW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3209-3213 , 文章类型: Article,,卷期:2009年19-12]
- This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype. This work demonstrates fu...
- Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands
[作者:Liu, KG; Lo, JR; Comery, TA; Zhang, GM; Zhang, JY; Kowal, DM; Smith, DL; Di, L; Kerns, EH; Schechter, LE; Robichaud, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3214-3216 , 文章类型: Article,,卷期:2009年19-12]
- Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimer's disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, ...
- Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors
[作者:Nakamura, H; Watanabe, M; Ban, HS; Nabeyama, W; Asai, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3220-3224 , 文章类型: Article,,卷期:2009年19-12]
- A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Com...
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