- Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712
[作者：Chen, H; Blizzard, TA; Kim, S; Wu, J; Young, K; Park, YW; Ogawa, AM; Raghoobar, S; Painter, RE; Wisniewski, D; Hairston, N; Fitzgerald, P; Sharma, N; Scapin, G; Lu, J; Hermes, J; Hammond, ML,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4267-4270 , 文章类型： Article，,卷期：2011年21-14]
- The bridged monobactam beta-lactamase inhibitor MK-8712 (1) effectively inhibits class C beta-lactamases. Side chain N-alkylated and ring-opened analogs of 1 were prepared and evaluated for combination with imipenem to o...
- SAR studies of 9-norbornylpurines as Coxsackievirus B3 inhibitors
[作者：Sala, M; De Palma, AM; Hrebabecky, H; Dejmek, M; Dracinsky, M; Leyssen, P; Neyts, J; Mertlikova-Kaiserova, H; Nencka, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4271-4275 , 文章类型： Article，,卷期：2011年21-14]
- Coxsackievirus and related enteroviruses are important human pathogens that cause various diseases with clinical manifestations ranging from trivial flu-like syndromes to dangerous or even fatal diseases such as myocardi...
- Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: Optimization of drug-like properties and target independent parameters
[作者：Zindell, R; Walker, ER; Scott, J; Amouzegh, P; Wu, LF; Ermann, M; Thomson, D; Fisher, MB; Fullenwider, CL; Grbic, H; Kaplita, P; Linehan, B; Patel, M; Patel, M; Lobbe, S; Block, S; Albrecht, C; Gemkow, MJ; Shih, DT; Riether, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4276-4280 , 文章类型： Article，,卷期：2011年21-14]
- A high throughput screening campaign identified aryl 1,4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-...
- Synthesis of useful fragments in drug discovery: 2-Amino-5-tert-butylpyridine and its oxidised analogues
[作者：Thomson, CG; Reilly, J; Sandham, DA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4281-4283 , 文章类型： Article，,卷期：2011年21-14]
- A novel and robust synthesis of the fragment, 2-amino-5-tert-butylpyridine, has been described, which has been shown to have improved physicochemical properties over 4-tert-butylaniline, when considering drug-like proper...
- Optimisation of a novel series of selective CNS penetrant CB(2) agonists
[作者：Watson, C; Owen, DR; Harding, D; Kon-I, K; Lewis, ML; Mason, HJ; Matsumizu, M; Mukaiyama, T; Rodriguez-Lens, M; Shima, A; Takeuchi, M; Tran, I; Young, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4284-4287 , 文章类型： Article，,卷期：2011年21-14]
- A series of benzimidazole CB(2) receptor agonists were prepared and their properties investigated. Optimisation of the three benzimidazole substituents led to the identification of compound 23, a potent CB2 full agonist ...
- Substituent effect on the preferred DNA binding mode and affinity of a homologous series of naphthalene diimides
[作者：McKnight, RE; Reisenauer, E; Pintado, MV; Polasani, SR; Dixon, DW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4288-4291 , 文章类型： Article，,卷期：2011年21-14]
- A combination of isothermal titration calorimetry (ITC), topoisomerase I DNA unwinding assays, and ethidium bromide displacement studies were employed to investigate the binding of a homologous series of naphthalene diim...
- New muramyl dipeptide (MDP) mimics without the carbohydrate moiety zas potential adjuvant candidates for a therapeutic hepatitis B vaccine (HBV)
[作者：Zhao, N; Ma, Y; Zhang, SM; Fang, X; Liang, ZL; Liu, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4292-4295 , 文章类型： Article，,卷期：2011年21-14]
- A series of new muramyl dipeptide (MDP) mimics were designed and synthesized via a solid-phase synthetic route. Their adjuvant activities were evaluated ex vivo for investigation of the synergism of the S(28-39) peptide,...
- Indolin-2-one p38 alpha inhibitors I: Design, profiling and crystallographic binding mode
[作者：Eastwood, P; Gonzalez, J; Gomez, E; Vidal, B; Caturla, F; Roca, R; Balague, C; Orellana, A; Dominguez, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4130-4133 , 文章类型： Article，,卷期：2011年21-14]
- The use of structure-based design and molecular modeling led to the discovery of indolin-2-one derivatives as potent and selective p38 alpha inhibitors. The predicted binding mode was confirmed by X-ray crystallography. ...
- Synthesis and anti-inflammatory activity of some novel 3-phenyl-N-[3-(4-phenylpiperazin-1yl)propyl]-1H-pyrazole-5-carboxamide derivatives
[作者：Nagarapu, L; Mateti, J; Gaikwad, HK; Bantu, R; Rani, MS; Subhashini, NJP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4138-4140 , 文章类型： Article，,卷期：2011年21-14]
- A new series of 3-phenyl-N-[3-(4-phenylpiperazin-1yl)propyl]-1H-pyrazole-5-carboxamide derivatives were synthesized and investigated their anti-inflammatory activities using carrageenan-induced rat paw edema model in viv...
- Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase
[作者：Ngu, K; Weinstein, DS; Liu, W; Langevine, C; Combs, DW; Zhuang, SB; Chen, X; Madsen, CS; Harper, TW; Ahmad, S; Robl, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4141-4145 , 文章类型： Article，,卷期：2011年21-14]
- A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted i...
- Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1)
[作者：Wang, HX; Robl, JA; Hamann, LG; Simpkins, L; Golla, R; Li, YX; Seethala, R; Zvyaga, T; Gordon, DA; Li, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4146-4149 , 文章类型： Article，,卷期：2011年21-14]
- A series of pyridyl amide/sulfonamide inhibitors of 11 beta-HSD-1 were modified to incorporate a novel 1,2,4-triazolopyridine scaffold. Optimization of substituents at the 3 and 8 position of the TZP core, with a special...
- Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide
[作者：Robinson, RP; Bartlett, JA; Bertinato, P; Bessire, AJ; Cosgrove, J; Foley, PM; Manion, TB; Minich, ML; Ramos, B; Reese, MR; Schmahai, TJ; Swick, AG; Tess, DA; Vaz, A; Wolford, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4150-4154 , 文章类型： Article，,卷期：2011年21-14]
- Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associ...
- N-Acylhydrazones as inhibitors of PDE10A
[作者：Gage, JL; Onrust, R; Johnston, D; Osnowski, A; MacDonald, W; Mitchell, L; Urogdi, L; Rohde, A; Harbol, K; Gragerov, S; Dorman, G; Wheeler, T; Florio, V; Cutshall, NS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4155-4159 , 文章类型： Article，,卷期：2011年21-14]
- Cyclic nucleotide phosphodiesterases (PDEs) are represented by a large superfamily of enzymes. A series of hydrazone-based inhibitors was synthesized and shown to be novel, potent, and selective against PDE10A. Optimized...
- 2-Phenylimidazo[1,2-b]pyridazine derivatives highly active against Haemonchus contortus
[作者：Ali, A; Cablewski, T; Francis, CL; Ganguly, AK; Sargent, RM; Sawutz, DG; Winzenberg, KN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4160-4163 , 文章类型： Article，,卷期：2011年21-14]
- A series of 2-phenylimidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD(99) values of 30 nM...
- A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold
[作者：Kemp, MM; Wang, Q; Fuller, JH; West, N; Martinez, NM; Morse, EM; Weiwer, M; Schreiber, SL; Bradner, JE; Koehler, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4164-4169 , 文章类型： Article，,卷期：2011年21-14]
- Histone deacetylases (HDACs) are enzymes involved in many important biological functions. They have been linked to a variety of cancers, psychiatric disorders, and other diseases. Since small molecules can serve as probe...
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