WordNet
- resulting from or employing derivation; "a derivative process"; "a highly derivative prose style"
- a compound obtained from, or regarded as derived from, another compound
- (linguistics) a word that is derived from another word; "`electricity is a derivative of `electric"
PrepTutorEJDIC
- 派生した,由来した;独創性のない,借り物めいた / 派生語 / 派生した物
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English Journal
- Facile and efficient syntheses of a series of N-benzyl and N-biphenylmethyl substituted imidazole derivatives based on (E)-urocanic acid, as angiotensin II AT1 receptor blockers.
- Agelis G1, Kelaidonis K, Resvani A, Kalavrizioti D, Androutsou ME, Plotas P, Vlahakos D, Koukoulitsa C, Tselios T, Mavromoustakos T, Matsoukas J.Author information 1Department of Chemistry, University of Patras, Patras 26500, Greece. aggelisgeorge@hotmail.comAbstractIn the present work, a facile and efficient route for the synthesis of a series of N-substituted imidazole derivatives is described. Docking studies have revealed that N-substituted imidazole derivatives based on (E)-urocanic acid may be potential antihypertensive leads. Therefore, new AT1 receptor blockers bearing either the benzyl or the biphenylmethyl moiety at the N-1 or N-3 position, either the (E)-acrylate or the propanoate fragment and their related acids at the C-4 position as well as a halogen atom at the C-5 position of the imidazole ring, were synthesized. The newly synthesized analogues were evaluated for binding to human AT1 receptor. The biological results showed that this class of molecules possesses moderate or no activity, thus not always confirming high docking scores. Nonetheless, important conclusions can be derived for their molecular basis of their mode of action and help medicinal chemists to design and synthesize more potent ones. An aliphatic group as in losartan seems to be important for enhancing binding affinity and activity.
- Molecules (Basel, Switzerland).Molecules.2013 Jun 27;18(7):7510-32. doi: 10.3390/molecules18077510.
- In the present work, a facile and efficient route for the synthesis of a series of N-substituted imidazole derivatives is described. Docking studies have revealed that N-substituted imidazole derivatives based on (E)-urocanic acid may be potential antihypertensive leads. Therefore, new AT1 receptor
- PMID 23807577
- CD22-antagonists with nanomolar potency: the synergistic effect of hydrophobic groups at C-2 and C-9 of sialic acid scaffold.
- Abdu-Allah HH1, Watanabe K, Completo GC, Sadagopan M, Hayashizaki K, Takaku C, Tamanaka T, Takematsu H, Kozutsumi Y, Paulson JC, Tsubata T, Ando H, Ishida H, Kiso M.Author information 1Department of Applied Bio-organic Chemistry, Faculty of Applied Biological Sciences, The United Graduate School of Agricultural Sciences, Gifu University, Gifu 501-1193, Japan. moazhajjaj@yahoo.comAbstractIn earlier studies, we identified the C-9 amido derivative 1 (9-(4'-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gcα2-6GalOMP) and the C-9 amino derivative 2 (9-(4'-hydroxy-4-biphenyl)methylamino-9-deoxy-Neu5Gcα2-6GalOMP) have the most promising affinity for mouse CD22 and human CD22, respectively. Replacing the subterminal galactose residue (2-6Gal-OMP) of 1 with benzyl (5) or biphenylmethyl (6) as aglycone led to even higher potency for mCD22. In this study, both compounds showed improved potency and selectivity for CD22 (IC(50) 70 nM) and 712-fold more selective for CD22 than for MAG. The corresponding derivatives of 2, compounds 8 and 9, showed comparable activity to 2 but lower potency and selectivity than 5 and 6. Although compounds 5-9 are simple and small molecular weight antagonists, they showed much high potency and selectivity than the corresponding compounds having α 2-6Gal linkage. Both biological and computational docking simulation studies suggest that the 2-6Gal-OMP residues of 1 and 2 are not critical for binding process and could be replaced with hydrophobic non-carbohydrate moieties. The data presented herein has significant implications for the design and discovery of next-generation CD22-antagonists.
- Bioorganic & medicinal chemistry.Bioorg Med Chem.2011 Mar 15;19(6):1966-71. doi: 10.1016/j.bmc.2011.01.060. Epub 2011 Feb 2.
- In earlier studies, we identified the C-9 amido derivative 1 (9-(4'-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gcα2-6GalOMP) and the C-9 amino derivative 2 (9-(4'-hydroxy-4-biphenyl)methylamino-9-deoxy-Neu5Gcα2-6GalOMP) have the most promising affinity for mouse CD22 and human CD22, respectively. Re
- PMID 21349726
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- 関
- analog、analogue、derivate、relative