54525-19-8Relevant academic research and scientific papers
NOVEL ADENINE DERIVATIVES
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Page/Page column 54-55, (2010/04/03)
Compounds of formula (I) wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure (II): n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH2)n- moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
HETEROCYCLIC COMPOUNDS AS CCR2B ANTAGONISTS
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Page/Page column 193, (2008/06/13)
Compounds of formula (I) Q-L-W-C(=X)-Z-P wherein Q is an amine of the formula-N (R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6-or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N-CN or S; Z is NR 3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C-C chemokine mediated conditions.
Design, synthesis, and biological evaluation of substituted benzoate analogues of the selective nicotinic acetylcholine receptor antagonist, methyllycaconitine
Doisy, Xavier,Blagbrough, Ian S.,Wonnacott, Susan,Potter, Barry V. L.
, p. 313 - 317 (2007/10/03)
The norditerpenoid alkaloid methyllycaconitine (MLA) acts as a competitive antagonist on the nicotinic acetylcholine receptor (nAChR) with a high preference for the neuronal α-bungarotoxin (αBgt)-sensitive nAChR over the muscle nAChR in mammals. MLA is thus a useful pharmacological tool. Furthermore, its efficient binding to insect nAChR indicates a high insecticidal potency. Within the complex hexacyclic structure of MLA, we envisaged a potential simple pharmacophore. This led to the design and synthesis of acyclic and monocyclic analogues of MLA. The biological activity of these derivatives at both neuronal nicotinic and muscarinic AChR was evaluated. Some of these structurally simple compounds, despite displaying a modest affinity for the nAChR, showed good specificity. We were able to show the importance of the 2-(methylsuccinimido)benzoate ester moiety and the E-ring of MLA. None of the analogues tested displayed any affinity for [3H]nicotine binding sites in brain membranes, indicating that α7-selectivity is already inherent in these simple structures. If higher affinities are to be obtained, however, there is a clear need for more structural information in the design of second generation simple analogues of MLA.
3-arylcarbonyl-1-(C-attached-N-heteryl)-1H-indoles
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, (2008/06/13)
2-R2 -R4 -substituted-3-R3 -CO-1-[(C-attached-N-herteryl)-(Alk)n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
