- A three-step protocol for lead optimization: Quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors
[作者:Huang, XH; Zhu, XH; Chen, X; Zhou, W; Xiao, D; Degrado, S; Aslanian, R; Fossetta, J; Lundell, D; Tian, F; Trivedi, P; Palani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:65-70 , 文章类型: Article,,卷期:2012年22-1]
- A three-step protocol for SAR development was introduced and applied to the SAR studies of the MK2 inhibitor program. Following this protocol, key conformational features and functional groups for improving MK2 inhibitor...
- Identification of biaryl sulfone derivatives as antagonists of the histamine H-3 receptor: Discovery of (R)-1-(2-(4 '-(3-methoxypropylsulfonyl)biphenyl-4-yl) ethyl)-2-methylpyrrolidine (APD916)
[作者:Semple, G; Santora, VJ; Smith, JM; Covel, JA; Hayashi, R; Gallardo, C; Ibarra, JB; Schultz, JA; Park, DM; Estrada, SA; Hofilena, BJ; Smith, BM; Ren, A; Suarez, M; Frazer, J; Edwards, JE; Hart, R; Hauser, EK; Lorea, J; Grottick, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:71-75 , 文章类型: Article,,卷期:2012年22-1]
- The design of a new clinical candidate histamine-H-3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide comp...
- Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway
[作者:Theriault, JR; Felts, AS; Bates, BS; Perez, JR; Palmer, M; Gilbert, SR; Dawson, ES; Engers, JL; Lindsley, CW; Emmitte, KA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:76-81 , 文章类型: Article,,卷期:2012年22-1]
- Hypoxia and ischemia are linked to several serious public health problems that affect most major organ systems. Specific examples include diseases of the cardiovascular, pulmonary, renal, neurologic, and musculoskeletal ...
- Combination of two chromophores: Synthesis and PDT application of porphyrin-pentamethinium conjugate
[作者:Briza, T; Kralova, J; Cigler, P; Kejik, Z; Pouckova, P; Vasek, P; Moserova, I; Martasek, P; Kral, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:82-84 , 文章类型: Article,,卷期:2012年22-1]
- A general method for the synthesis of a novel porphyrin with pentamethine periphery substitution is described. The combination of two chromophoric systems, a porphyrin macrocycle and a polymethine moiety was achieved by ...
- Discovery of bacterial NAD(+)-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series
[作者:Stokes, SS; Gowravaram, M; Huynh, H; Lu, M; Mullen, GB; Chen, B; Albert, R; O'Shea, TJ; Rooney, MT; Hu, HQ; Newman, JV; Mills, SD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:85-89 , 文章类型: Article,,卷期:2012年22-1]
- Optimization of clearance of adenosine inhibitors of bacterial NAD(+)-dependent DNA ligase is discussed. To reduce Cytochrome P-450-mediated metabolic clearance, many strategies were explored; however, most modifications...
|