- New Labdane diterpenes as intestinal alpha-glucosidase inhibitor from antihyperglycemic extract of Hedychium spicatum (Ham. Ex Smith) rhizomes
[作者:Reddy, PP; Tiwari, AK; Rao, RR; Madhusudhana, K; Rao, VRS; Ali, AZ; Babu, KS; Rao, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2562-2565 , 文章类型: Article,,卷期:2009年19-9]
- Phytochemical investigation of antihyperglycemic extract of rhizomes of Hedychium spicatum led to the isolation of two new labdane type diterpenes 2, 3 along with seven known compounds (1, 4-9). Their structures were est...
- Novel synthesis and in vitro drug release of polymeric prodrug: Chitosan-O-isopropyl-5 '-O-d4T monophosphate conjugate
[作者:Yang, L; Zeng, R; Li, C; Li, G; Qiao, RZ; Hu, LM; Li, ZL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2566-2569 , 文章类型: Article,,卷期:2009年19-9]
- A novel approach to synthesize chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate was developed. Chitosan-d4T monophosphate prodrug with a phosphoramidate linkage was efficiently synthesized through Atherton-Todd reac...
- Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials
[作者:Sunduru, N; Srivastava, K; Rajakumar, S; Puri, SK; Saxena, JK; Chauhan, PMS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2570-2573 , 文章类型: Article,,卷期:2009年19-9]
- In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activi...
- Conjugation with alpha-linolenic acid improves cancer cell uptake and cytotoxicity of doxorubicin
[作者:Huan, ML; Zhou, SY; Teng, ZH; Zhang, BL; Liu, XY; Wang, JP; Mei, QB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2579-2584 , 文章类型: Article,,卷期:2009年19-9]
- The synthetic DOX-LNA conjugate was characterized by proton nuclear magnetic resonance and mass spectrometry. In addition, the purity of the conjugate was analyzed by reverse-phase high-performance liquid chromatography....
- Peganine hydrochloride dihydrate an orally active antileishmanial agent
[作者:Khaliq, T; Misra, P; Gupta, S; Reddy, KP; Kant, R; Maulik, PR; Dube, A; Narender, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2585-2586 , 文章类型: Article,,卷期:2009年19-9]
- Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on dru...
- Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
[作者:Debenham, JS; Madsen-Duggan, CB; Wang, JY; Tong, XC; Lao, JL; Fong, TM; Schaeffer, MT; Xiao, JC; Huang, CCRR; Shen, CP; Stribling, DS; Shearman, LP; Strack, AM; MacIntyre, DE; Hale, JJ; Walsh, TF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2591-2594 , 文章类型: Article,,卷期:2009年19-9]
- The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of s...
- Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist
[作者:Feng, S; Yang, MM; Zhang, ZS; Wang, ZG; Hong, D; Richter, H; Benson, GM; Bleicher, K; Grether, U; Martin, RE; Plancher, JM; Kuhn, B; Rudolph, MG; Chen, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2595-2598 , 文章类型: Article,,卷期:2009年19-9]
- According to the docking studies and the analysis of a co-crystal structure of GW4064 with FXR, a series of 3-aryl heterocyclic isoxazole analogs were designed and synthesized. N-Oxide pyridine analog (7b) was identified...
- Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP1 receptor antagonist for the treatment of inflammatory pain
[作者:Hall, A; Billinton, A; Brown, SH; Chowdhury, A; Clayton, NM; Giblin, GMP; Gibson, M; Goldsmith, PA; Hurst, DN; Naylor, A; Peet, CF; Scoccitti, T; Wilson, AW; Winchester, W,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2599-2603 , 文章类型: Article,,卷期:2009年19-9]
- We describe the medicinal chemistry programme that led to the identification of the EP1 receptor antagonist GSK269984A (8h). GSK269984A was designed to overcome development issues encountered with previous EP1 antagonist...
- Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding (vol 19, pg 1694, 2009)
[作者:Emmitte, KA; Adjabeng, GM; Andrews, CW; Alberti, JGB; Bambal, R; Chamberlain, SD; Davis-Ward, RG; Dickson, HD; Hassler, DF; Hornberger, KR; Jackson, JR; Kuntz, KW; Lansing, TJ; Mook, RA; Nailor, KE; Pobanz, MA; Smith, SC; Sung, CM; Cheung, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2604-2604 , 文章类型: Correction,,卷期:2009年19-9]
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- Deconstructing estradiol: Removal of B-ring generates compounds which are potent and subtype-selective estrogen receptor agonists (vol 19, pg 1250, 2009)
[作者:Asim, M; El-Salfiti, M; Qian, YM; Choueiri, C; Salari, S; Cheng, J; Shadnia, H; Bal, M; Pratt, MAC; Carlson, KE; Katzenellenbogen, JA; Wright, JS; Durst, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2605-2605 , 文章类型: Correction,,卷期:2009年19-9]
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- DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity (vol 19, pg 894, 2009)
[作者:East, SP; White, CB; Barker, O; Barker, S; Bennett, J; Brown, D; Boyd, EA; Brennan, C; Chowdhury, C; Collins, I; Convers-Reignier, E; Dymock, BW; Fletcher, R; Haydon, DJ; Gardiner, M; Hatcher, S; Ingram, P; Lancett, P; Mortenson, P; Papadopoulos, K; Smee, C; Thomaides-Brears, HB; Tye, H; Workman, J; Czaplewski, LG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2606-2606 , 文章类型: Correction,,卷期:2009年19-9]
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- The chemoenzymatic synthesis of usnic acid
[作者:Hawranik, DJ; Anderson, KS; Simmonds, R; Sorensen, JL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2383-2385 , 文章类型: Article,,卷期:2009年19-9]
- Usnic acid, a highly functionalized dibenzofuran, is a polyketide secondary metabolite produced by several species of lichens. Synthesis of usnic acid from commercially available starting material was accomplished in two...
- Discovery and characterization of the N-phenyl-N '-naphthylurea class of p38 kinase inhibitors
[作者:Cirillo, PF; Hickey, ER; Moss, N; Breitfelder, S; Betageri, R; Fadra, T; Gaenzler, F; Gilmore, T; Goldberg, DR; Kamhi, V; Kirrane, T; Kroe, RR; Madwed, J; Moriak, M; Netherton, M; Pargellis, CA; Patel, UR; Qian, KC; Sharma, R; Sun, SX; Swinamer, A; Torcellini, C; Takahashi, H; Tsang, M; Xiong, ZM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2386-2391 , 文章类型: Article,,卷期:2009年19-9]
- An effort aimed at exploring structural diversity in the N-pyrazole-N'-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization of N-phenyl-N'-naphthylureas. Examples of these compounds displ...
- Synthesis and inotropic evaluation of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamides
[作者:Liu, JY; Yu, HL; Quan, ZS; Cui, X; Piao, HR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2392-2395 , 文章类型: Article,,卷期:2009年19-9]
- A series of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl) piperidine-4-carboxamides has been synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume i...
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