- Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)(n)NH2
[作者:Vergara, FMF; Henriques, MDMO; Candea, ALP; Wardell, JL; De Souza, MVN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4937-4938 , 文章类型: Article,,卷期:2009年19-17]
- A series of 11 alpha,omega-diaminoalkanes, (H2N(CH2)nNH(2), n = 2-12) have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Compounds, (H2N(CH2)(n)NH2, n = 9-12), exhibit...
- Unsaturated genistein disaccharide glycoside as a novel agent affecting microtubules
[作者:Rusin, A; Gogler, A; Glowala-Kosinska, M; Bochenek, D; Gruca, A; Grynkiewicz, G; Zawisza, J; Szeja, W; Krawczyk, Z,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4939-4943 , 文章类型: Article,,卷期:2009年19-17]
- Genistein, due to its recognized chemopreventive and antitumor potential, is a molecule of interest as a lead compound in drug design. While multiple molecular targets for genistein have been identified, so far neither f...
- The synthesis of 2-and 3-aryl indoles and 1,3,4,5-tetrahydropyrano[4,3-b]indoles and their antibacterial and antifungal activity
[作者:Leboho, TC; Michael, JP; van Otterlo, WAL; van Vuuren, SF; de Koning, CB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4948-4951 , 文章类型: Article,,卷期:2009年19-17]
- A series of 2- and 3-aryl substituted indoles and two 1,3,4,5-tetrahydropyrano[4,3-b] indoles were synthesized from indole and 5-methoxyindole. The 2- aryl indoles were synthesized from the 1-(phenylsulfonyl) indole deri...
- Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors
[作者:Gonzalez, A; Quirante, J; Nieto, J; Almeida, MR; Saraiva, MJ; Planas, A; Arsequell, G; Valencia, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5270-5273 , 文章类型: Article,,卷期:2009年19-17]
- The isatin core structure was found to be a novel chemical scaffold in transthyretin (TTR) brillogenesis inhibitor design. Among the series of isatin analogues prepared and tested, the nitro compound 1,3-dihydro3-[(4-nit...
- Schisanwilsonins A-G and related anti-HBV lignans from the fruits of Schisandra wilsoniana
[作者:Ma, WH; Lu, Y; Huang, H; Zhou, P; Chen, DF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4958-4962 , 文章类型: Article,,卷期:2009年19-17]
- Seven new dibenzocyclooctane lignans, schisanwilsonins A-G (1-7), were isolated from the fruits of Schisandra wilsoniana, together with five known lignans (8-12). The structures of these new compounds were elucidated by ...
- Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH)
[作者:Kummerle, AE; Vieira, MM; Schmitt, M; Miranda, ALP; Fraga, CAM; Bourguignon, JJ; Barreiro, EJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4963-4966 , 文章类型: Article,,卷期:2009年19-17]
- A set of six azaheterocycles were designed as conformationnaly-constrained N-acylhydrazones and tested as analgesics. (C) 2009 Elsevier Ltd. All rights reserved.
- Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)
[作者:Williams, R; Johnson, KA; Gentry, PR; Niswender, CM; Weaver, CD; Conn, PJ; Lindsley, CW; Hopkins, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4967-4970 , 文章类型: Article,,卷期:2009年19-17]
- This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an i...
- 2,4-Diamino-quinazolines as inhibitors of beta-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer
[作者:Chen, ZC; Venkatesan, AM; Dehnhardt, CM; Dos Santos, O; Delos Santos, E; Ayral-Kaloustian, S; Chen, L; Geng, Y; Arndt, KT; Lucas, J; Chaudhary, I; Mansour, TS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4980-4983 , 文章类型: Article,,卷期:2009年19-17]
- The synthesis and SAR of a series of 2,4-diamino-quinazoline derivatives as beta-catenin/Tcf-4 inhibitors are described. This series was developed by modifying the initial lead 1, which was identified by screening of our...
- Development of a novel expression, ZI(MAX)/K-ZI, for determination of the counter-anion effect on the antimicrobial activity of tetrabutylammonium salts
[作者:Ingalsbe, ML; St Denis, JD; McGahan, ME; Steiner, WW; Priefer, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4984-4987 , 文章类型: Article,,卷期:2009年19-17]
- Due to the increasing number of strains of drug-resistant bacteria, the development of new antibiotics has become increasingly important. The antibacterial properties of quaternary amines and their derivatives on both Gr...
- 4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents
[作者:Duan, MS; Aquino, C; Dorsey, GF; Ferris, R; Kazmierski, WM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4988-4992 , 文章类型: Article,,卷期:2009年19-17]
- A series of 4,4-disubstituted cyclohexylamine based CCR5 antagonists has been designed and synthesized. Their antiviral structure-activity relationship has been extensively explored. (C) 2009 Elsevier Ltd. All rights res...
- A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason
[作者:Hills, ID; Holloway, MK; de Leon, P; Nomland, A; Zhu, H; Rajapakse, H; Allison, TJ; Munshi, SK; Colussi, D; Pietrak, BL; Toolan, D; Haugabook, SJ; Graham, SL; Stachel, SJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4993-4995 , 文章类型: Article,,卷期:2009年19-17]
- During our ongoing efforts to develop a small molecule inhibitor targeting the beta-amyloid cleaving enzyme (BACE-1), we discovered a class of compounds bearing an aminoimidazole motif. Initial optimization led to potent...
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