- Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R
[作者:Wagner, E; Wittmann, HJ; Elz, S; Strasser, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6274-6280 , 文章类型: Article,,卷期:2011年21-21]
- In literature, a synergism between histamine H(1) and H(4) receptor is discussed. Furthermore, it was shown, that the combined application of mepyramine, a H(1) antagonist and JNJ7777120, a H(4) receptor ligand leads to ...
- Cell fingerprint patterns using designed alpha-helical peptides to screen for cell-specific toxicity
[作者:Usui, K; Kakiyama, T; Tomizaki, K; Mie, M; Kobatake, E; Mihara, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6281-6284 , 文章类型: Article,,卷期:2011年21-21]
- We conducted cell-based cytotoxicity screening of a 101-membered alpha-helical peptide library using cell fingerprints (CFPs). The CFP data suggested that there is a relationship between cytotoxicity and peptide characte...
- Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981
[作者:Luker, T; Bonnert, R; Brough, S; Cook, AR; Dickinson, MR; Dougall, I; Logan, C; Mohammed, RT; Paine, S; Sanganee, HJ; Sargent, C; Schmidt, JA; Teague, S; Thom, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6288-6292 , 文章类型: Article,,卷期:2011年21-21]
- Novel indole-3-thio-, 3-sulfonyl- and 3-oxy-aryl-1-acetic acids are reported which are potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). Optimi...
- Design and synthesis of biotinylated DHMEQ for direct identification of its target NF-kappa B components
[作者:Saitoh, T; Takeiri, M; Gotoh, Y; Ishikawa, Y; Umezawa, K; Nishiyama, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6293-6296 , 文章类型: Article,,卷期:2011年21-21]
- The design and synthesis of dehydroxymethylepoxyquinomicin (DHMEQ) derivatives were carried out to investigate the intracellular targets. The synthetic biotin probe exhibited membrane permeability and combined selectivel...
- Design, synthesis and insight into the structure-activity relationship of 1,3-disubstituted indazoles as novel HIF-1 inhibitors
[作者:An, H; Kim, NJ; Jung, JW; Jang, H; Park, JW; Suh, YG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6297-6300 , 文章类型: Article,,卷期:2011年21-21]
- Design, synthesis and insight into the structure-activity relationship (SAR) of 1,3-disubstituted indazoles as novel HIF-1 inhibitors are described. In particular, the substituted furan moiety on indazole skeleton as wel...
- Synthesis, stereochemistry and in vitro antimicrobial evaluation of novel 2-[(2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazono]-4-phenyl-2,3-dihydrothiazoles
[作者:Ramachandran, R; Parthiban, P; Rani, M; Jayanthi, S; Kabilan, S; Jeong, YT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6301-6304 , 文章类型: Article,,卷期:2011年21-21]
- 2-[(2,4-Diaryl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazono]-4-phenyl-2,3-dihydrothiazoles (3a-3k) have been synthesized by the cyclization of 2-[(2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-one thiosemicarbazones with phenacy...
- Identification of novel plasmin inhibitors possessing nitrile moiety as warhead
[作者:Teno, N; Gohda, K; Wanaka, K; Sueda, T; Tsuda, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6305-6309 , 文章类型: Article,,卷期:2011年21-21]
- Lysine-nitrile derivatives having a trisubstituted benzene, which belongs to a new chemical class, were prepared and tested for inhibitory activities against plasmin and the highly homologous plasma kallikrein and urokin...
- Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: Structural requirements for better physicochemical and biological properties
[作者:Nagata, N; Miyakawa, M; Amano, S; Furuya, K; Yamamoto, N; Nejishima, H; Inoguchi, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6310-6313 , 文章类型: Article,,卷期:2011年21-21]
- A rationally designed tetrahydroquinoline (1) for nonsteroidal selective androgen receptor modulators was modified for the exploration of promising compounds by Grieco three-component condensation using various dienophil...
- Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors
[作者:Yamashita, T; Kamata, M; Endo, S; Yamamoto, M; Kakegawa, K; Watanabe, H; Miwa, K; Yamano, T; Funata, M; Sakamoto, J; Tani, A; Mol, CD; Zou, H; Dougan, DR; Sang, BC; Snell, G; Fukatsu, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6314-6318 , 文章类型: Article,,卷期:2011年21-21]
- The co-crystal structure of the human acetyl-coenzyme A 2 (ACC2) carboxyl transferase domain and the reported compound CP-640186 (1b) suggested that two carbonyl groups are essential for potent ACC2 inhibition. By focusi...
- Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis)
[作者:Bouchikhi, F; Anizon, F; Brun, R; Moreau, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6319-6321 , 文章类型: Article,,卷期:2011年21-21]
- The biological activities of diversely substituted glycosyl-isoindigo derivatives against the causative agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis) are reported....
- 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase
[作者:Walsh, MJ; Brimacombe, KR; Veith, H; Bougie, JM; Daniel, T; Leister, W; Cantley, LC; Israelsen, WJ; Vander Heiden, MG; Shen, M; Auld, DS; Thomas, CJ; Boxer, MB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6322-6327 , 文章类型: Article,,卷期:2011年21-21]
- Compared to normal differentiated cells, cancer cells have altered metabolic regulation to support biosynthesis and the expression of the M2 isozyme of pyruvate kinase (PKM2) plays an important role in this anabolic meta...
- Antiviral activity of novel 2 '-fluoro-6 '-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants
[作者:Wang, JN; Singh, US; Rawal, RK; Sugiyama, M; Yoo, J; Jha, AK; Scroggin, M; Huang, ZH; Murray, MG; Govindarajan, R; Tanaka, Y; Korba, B; Chu, CK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6328-6331 , 文章类型: Article,,卷期:2011年21-21]
- Novel 2'-fluoro-6'-methylene-carbocyclic adenosine (9) was synthesized and evaluated its anti-HBV activity. The titled compound demonstrated significant antiviral activity against wild-type as well as lamivudine, adefovi...
- Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP(4) receptor
[作者:Stasi, LP; Bhimani, K; Borriello, M; Canciani, L; Caselli, G; Colace, F; Ferioli, C; Kaswala, M; Mennuni, L; Piepoli, T; Pucci, S; Salvi, M; Shirsath, V; Zanelli, T; Zerbi, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6336-6340 , 文章类型: Article,,卷期:2011年21-21]
- The construction of a EP(4) antagonists pharmacophore model and the discovery of a highly potent oxepinic series of EP(4) antagonists is discussed. Compound 1a exhibits an excellent selectivity profile toward EP2 recepto...
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