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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共61条记录   Pyrazoline-based mycobactin analogues as MAO-inhibitors [作者：Jayaprakash, V; Sinha, BN; Ucar, G; Ercan, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6362-6368 , 文章类型： Article，,卷期：2008年18-24] 3,5-Diaryl carbothioamide pyrazolines designed as mycobactin analogs (mycobacterial siderophore) were reported to be potent antitubercular agents under iron limiting condition in our earlier study. Clinical complications... The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing [作者：Jones, CD; Andrews, DM; Barker, AJ; Blades, K; Daunt, P; East, S; Geh, C; Graham, MA; Johnson, KM; Loddick, SA; McFarland, HM; McGregor, A; Moss, L; Rudge, DA; Simpson, PB; Swain, ML; Tam, KY; Tucker, JA; Walker, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6963-6967 , 文章类型： Article，,卷期：2008年18-24] The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. Optimisation of inhibitory potency against multiple CDK's (1, 2 and 9) resulted in imidazole pyri... alpha-S-GalCer: Synthesis and evaluation for iNKT cell stimulation [作者：Blauvelt, ML; Khalili, M; Jaung, W; Paulsen, J; Anderson, AC; Wilson, SB; Howell, AR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6968-6970 , 文章类型： Article，,卷期：2008年18-24] The synthesis and evaluation for iNKT stimulation of alpha-S-galactosylceramide is reported. Prepared by alkylation of a galactosylthiol, this analog of the potent immunostimulatory agent, KRN7000, did not stimulate iNKT... Triterpene based compounds with potent anti-maturation activity against HIV-1 [作者：Gerrish, D; Kim, IC; Kumar, DV; Austin, H; Garrus, JE; Baichwal, V; Saunders, M; McKinnon, RS; Anderson, MB; Carlson, R; Arranz-Plaza, E; Yager, KM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6971-6380 , 文章类型： Article，,卷期：2008年18-24] Efforts towards developing orally bioavailable HIV-1 maturation inhibitors starting from betulinic acid 1 are described. SAR resulted in improved potency, physicochemical properties, and enhanced oral absorption in rats.... Dihydropyrazolopyrimidine Inhibitors of K(V)1.5 (I-Kur) [作者：Vaccaro, W; Huynh, T; Lloyd, J; Atwal, K; Finlay, HJ; Levesque, P; Conder, ML; Jenkins-West, T; Shi, H; Sun, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6381-6385 , 文章类型： Article，,卷期：2008年18-24] A series of dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I-Kur) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described. (C) 2008 Elsevie... Novel oxime and oxime ether derivatives of 12,14-dichlorodehydroabietic acid: Design, synthesis, and BK channel-opening activity [作者：Cui, YM; Yasutomi, E; Otani, Y; Yoshinaga, T; Ido, K; Sawada, K; Kawahata, M; Yamaguchi, K; Ohwada, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6386-6389 , 文章类型： Article，,卷期：2008年18-24] Oxime ether derivatives of the benzylic ketone of 12,14-dichlorodehydroabietic acid (diCl-DHAA, 4b) were synthesised, and their BK channel-opening activity was evaluated in an assay system of CHO-K1 cells expressing hBK ... Benzimidazole- and benzoxazole-based inhibitors of Rho kinase [作者：Sessions, EH; Yin, Y; Bannister, TD; Weiser, A; Griffin, E; Pocas, J; Cameron, MD; Ruiz, C; Lin, L; Schurer, SC; Schroter, T; LoGrasso, P; Feng, YB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6390-6393 , 文章类型： Article，,卷期：2008年18-24] Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ... N-confused porphyrin possessing glucamine-appendants: Aggregation and acid/base properties in aqueous media [作者：Ikawa, Y; Ogawa, H; Harada, H; Furuta, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6394-6397 , 文章类型： Article，,卷期：2008年18-24] A water-soluble derivative of N-confused porphyrin (NCP: 5,10,15,20-tetraaryl-2-aza-21-carbaporphyrin) was synthesized by introducing glucamine groups at the para-position of meso-aryl groups. The tetraglucamine-appended... Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology [作者：Nemoto, T; Fujii, H; Narita, M; Miyoshi, K; Nakamura, A; Suzuki, T; Nagase, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6398-6401 , 文章类型： Article，,卷期：2008年18-24] A novel 6,14-epoxymorphinan benzamide derivative (NS22) was synthesized, which showed opioid kappa receptor agonistic activity in the [S-35]GTP gamma S binding assay. The antinociceptive effect of NS22 was evaluated in t... Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors [作者：Alhamadsheh, MM; Waters, NC; Sachdeva, S; Lee, P; Reynolds, KA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6402-6405 , 文章类型： Article，,卷期：2008年18-24] A series of analogs of 2-tosylnaphthalene-1,4-diol were prepared and were found to be potent 10-20 nM reversible inhibitors of the Escherichia coli FabH enzyme. The inhibitors were also effective but to a lesser degree (... Chroman-3-amides as potent Rho kinase inhibitors [作者：Chen, YT; Bannister, TD; Weiser, A; Griffin, E; Lin, L; Ruiz, C; Cameron, MD; Schurer, S; Duckett, D; Schroter, T; LoGrasso, P; Feng, YB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6406-6409 , 文章类型： Article，,卷期：2008年18-24] Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase ... Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors [作者：Ahn, JH; Park, WS; Jun, MA; Shin, MS; Kang, SK; Kim, KY; Dal Rhee, S; Bae, MA; Kim, KR; Kim, SG; Kim, SY; Sohn, SK; Kang, NS; Lee, JO; Lee, DH; Cheon, HG; Kim, SS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6525-6529 , 文章类型： Article，,卷期：2008年18-24] Compounds with homopiperazine skeleton are designed to find a potent DPP-IV inhibitor without inhibiting CYP. Thus a series of beta-aminoacyl-containing homopiperazine derivatives was synthesized and evaluated. Compounds... Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents [作者：Kumar, A; Srivastava, K; Kumar, SR; Puri, SK; Chauhan, PMS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6530-6533 , 文章类型： Article，,卷期：2008年18-24] The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazine... Coagulanolide, a withanolide from Withania coagulans fruits and antihyperglycemic activity [作者：Maurya, R; Akanksha; Jayendra; Singh, AB; Srivastava, AK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6534-6537 , 文章类型： Article，,卷期：2008年18-24] One new withanolide, (17S,20S,22R)-14 alpha,15 alpha,17 beta,20 beta-tetrahydroxy-1-oxowitha-2,5,24-trienolide) named coagulanolide (4) along with four known withanolides 1-3 and 5 have been isolated from Withania coagul... Carbon analogs of antifungal dioxane-triazole derivatives: Synthesis and in vitro activities [作者：Uchida, T; Somada, A; Kagoshima, Y; Konosu, T; Oida, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6538-6541 , 文章类型： Article，,卷期：2008年18-24] A new series of triazole compounds possessing a carbon atom in place of a sulfur atom were efficiently synthesized and their in vitro antifungal activities were investigated. The carbon analogs showed excellent in vitro ... A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives [作者：Aridoss, G; Amirthaganesan, S; Kumar, NA; Kim, JT; Lim, KT; Kabilan, S; Jeong, YT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6542-6548 , 文章类型： Article，,卷期：2008年18-24] The raise in clinical significance of multidrug-resistant bacterial pathogens has directed us to synthesize 2,6-diarylpiperidin-4-one and Delta(3)-tetrahydropyridin-4-ol based benzimidazole and O-arylsulfonyl derivatives...