- Wake promoting agents: Search for next generation modafinil, lessons learned: Part III
[作者:Dunn, D; Hostetler, G; Iqbal, M; Marcy, VR; Lin, YG; Jones, B; Aimone, LD; Gruner, J; Ator, MA; Bacon, ER; Chatterjee, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3751-3753 , 文章类型: Article,,卷期:2012年22-11]
- In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinet...
- Reexamining hydroxamate inhibitors of botulinum neurotoxin serotype A: Extending towards the beta-exosite
[作者:Smith, GR; Caglic, D; Capek, P; Zhang, Y; Godbole, S; Reitz, AB; Dickerson, TJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3754-3757 , 文章类型: Article,,卷期:2012年22-11]
- Botulinum neurotoxins (BoNTs) are the most toxic proteins known to man, exposure to which results in flaccid paralysis. Given their extreme potency, these proteins have become studied as possible weapons of bioterrorism;...
- Synthesis, reactive oxygen species generation and copper-mediated nuclease activity profiles of 2-aryl-3-amino-1,4-naphthoquinones
[作者:Khodade, VS; Dharmaraja, AT; Chakrapani, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3766-3769 , 文章类型: Article,,卷期:2012年22-11]
- Here we report a series of 2-aryl-3-amino-1,4-naphthoquinones that generated reactive oxygen species (ROS) such as superoxide and hydrogen peroxide upon incubation in pH 7.4 under ambient aerobic conditions. ROS generati...
- Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition
[作者:Mihalic, JT; Fan, PC; Chen, XQ; Chen, X; Fu, Y; Motani, A; Liang, LM; Lindstrom, M; Tang, L; Chen, JL; Jaen, J; Dai, K; Li, LP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3781-3785 , 文章类型: Article,,卷期:2012年22-11]
- An initial SAR study resulted in the identification of the novel, potent MCHR1 antagonist 2. After further profiling, compound 2 was discovered to be a potent inhibitor of the hERG potassium channel, which prevented its ...
- Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11 beta-HSD1 inhibitors
[作者:Rew, Y; DeGraffenreid, M; He, X; Jaen, JC; McMinn, DL; Sun, DQ; Tu, H; Ursu, S; Powers, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3786-3790 , 文章类型: Article,,卷期:2012年22-11]
- A novel series of benzenesulfonanilide derivatives of 11 beta-HSD1 inhibitors were identified via modification of the sulfonamide core of the arylsulfonylpiperazine lead structures. The synthesis, in vitro biological eva...
- The macrocycle of leinamycin imparts hydrolytic stability to the thiol-sensing 1,2-dithiolan-3-one 1-oxide unit of the natural product
[作者:Sivaramakrishnan, S; Breydo, L; Sun, D; Gates, KS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3791-3794 , 文章类型: Article,,卷期:2012年22-11]
- Reaction of cellular thiols with the 1,2-dithiolan-3-one 1-oxide moiety of leinamycin triggers the generation of DNA-damaging reactive intermediates. Studies with small, synthetic analogues of leinamycin reveal that the ...
- Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters
[作者:Trujillo, JI; Kiefer, JR; Huang, W; Day, JE; Moon, J; Jerome, GM; Bono, CP; Kornmeier, CM; Williams, ML; Kuhn, C; Rennie, GR; Wynne, TA; Carron, CP; Thorarensen, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3795-3799 , 文章类型: Article,,卷期:2012年22-11]
- The inhibition of hH-PGDS has been proposed as a potential target for the development of anti-allergic and anti-inflammatory drugs. Herein we describe our investigation of the binding pocket of this important enzyme and ...
- Novel diamide insecticides: Sulfoximines, sulfonimidamides and other new sulfonimidoyl derivatives
[作者:Gnamm, C; Jeanguenat, A; Dutton, AC; Grimm, C; Kloer, DP; Crossthwaite, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3800-3806 , 文章类型: Article,,卷期:2012年22-11]
- Novel insecticidal anthranilamides with elaborated sulfur-containing groups are described. The synthesis of compounds with functional groups such as sulfoximines and scarcely reported groups such as sulfonimidoyl hydrazi...
- Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a] carbazole derivatives
[作者:Akue-Gedu, R; Letribot, B; Saugues, E; Debiton, E; Anizon, F; Moreau, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3807-3809 , 文章类型: Article,,卷期:2012年22-11]
- Development of potent and selective Pim kinase inhibitors has recently emerged as an important field for the design of new anti-cancer drugs. We report the synthesis of new N-10-substituted pyrrolo[2,3-a] carbazole deriv...
- Synthesis and preliminary biological profile of new NO-donor tolbutamide analogues
[作者:Tamboli, Y; Lazzarato, L; Marini, E; Guglielmo, S; Novelli, M; Beffy, P; Masiello, P; Fruttero, R; Gasco, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3810-3815 , 文章类型: Article,,卷期:2012年22-11]
- We describe a new class of NO-donor hypoglycemic products obtained by joining tolbutamide, a typical hypoglycemic sulfonylurea, with a NO-donor moiety through a hard link. As NO-donors we chose either furoxan (1,2,5-oxad...
- An efficient one-pot synthesis, structure, antimicrobial and antioxidant investigations of some novel quinolyldibenzo[b,e][1,4]diazepinones
[作者:Parmar, NJ; Barad, HA; Pansuriya, BR; Teraiya, SB; Gupta, VK; Kant, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3816-3821 , 文章类型: Article,,卷期:2012年22-11]
- A highly improved one-pot procedure for the synthesis of diazepinones, which incorporate a bioactive quinoline nucleus, under catalyst-, and solvent-free environment has been developed. The method allowed us to achieve t...
- A new series of N-5 derivatives of the 1,1,5-trimethyl furo[3,4-c]pyridine-3,4-dione (cerpegin) selectively inhibits the post-acid activity of mammalian 20S proteasomes
[作者:Pham, TH; Hovhannisyan, A; Bouvier, D; Tian, L; Reboud-Ravaux, M; Melikyan, G; Bouvier-Durand, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3822-3827 , 文章类型: Article,,卷期:2012年22-11]
- A large set of N-5-derivatives of cerpegin (1,1,5-trimethyl furo[3,4-c]pyridine-3,4-dione) was designed and synthesized in high yields by a simple and handy method using various primary amines for a pyridine cycle synthe...
- Trigoxyphins H and I: Two new daphnane diterpenoids from Trigonostemon xyphophylloides
[作者:Yang, B; Chen, GY; Song, XP; Yang, LQ; Han, CR; Wu, XY; Li, XM; Zou, BY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3828-3830 , 文章类型: Article,,卷期:2012年22-11]
- Two new daphnane diterpenoids (1 and 2), together with four known analogues (3-6) were isolated from Trigonostemon xyphophylloides. Their structures were elucidated by spectroscopic analysis. Compounds 1 and 2 were evalu...
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