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Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.
The new 1-phenyl-5-(1 H-pyrrol-1-yl)pyrazole-3-carboxamides were compared with the reference compounds AM251 and SR144528 for cannabinoid hCB 1 and hCB 2 receptor affinity and a H-bonding interaction was proposed to account for the high affinity for receptors' inactive state and the inverse agonist activity. Expand
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
The general loss of potency displayed by the compounds toward clinically relevant mutant strains was deeply studied through a molecular modeling approach, leading to the evidence that the dynamic of the entrance in the non-nucleoside binding pocket could represent the basis of the inhibitory activity of the molecules. Expand
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.
Compounds with amidic 'heads' with alkyloxy chains varying in length from 8 to 12 carbon atoms showed nanomolar affinity for both receptors, depending on the type of aromatic backbone, and two of the new compounds exhibit selectivity for CB(1) receptors. Expand
Thiazolothiazepine inhibitors of HIV-1 integrase.
Thiazolothiazepines are potentially important lead compounds for development as inhibitors of IN and HIV replication and suggest that a hydrophobic pocket in the IN active site might accommodate an aromatic system rather than a halogen. Expand
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.
This study planned the synthesis of a series of compounds which retained both a rigid structure, like that of plant cannabinoids, and a flexible portion similar to that of anandamide, and showed that some of the newly developed compounds have high affinity and specificity for cannabinoid CB1 and CB2 receptors. Expand
Synthesis and antitumor activities of a series of novel quinoxalinhydrazides.
A new synthetic route to SC144 is reported and the synthesis of several of its analogues in order to understand required features for activity and modify of the heteroacyl moiety had a dramatic effect on potency. Expand
HIV-reverse transcriptase inhibition: inclusion of ligand-induced fit by cross-docking studies.
The application of the Autodock program is reported assessing its usability through reproduction of 41 NNRTI experimental bound conformations to gain insight on the mode of action of new anti-HIV agents active against both wild-type and resistant strains. Expand
Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABAB and cannabinoid CB1 receptors
Cor659 might exert its behavioral effects via a composite mechanism: (i) positive allosteric modulation of the GABAB receptor, responsible for a large proportion of reduction of alcohol self-administration; (ii) an action at other receptor system(s), including the cannabinoid CB1 receptor, through which COR659 affects seeking and consumption of highly palatable foods. Expand
Regioselective functionalization of quinolin-4(1H)-ones via sequential palladium-catalyzed reactions
Abstract A practical and general synthesis of 1,3,6-trisubstituted quinolin-4(1H)-ones starting from 1-alkyl-6-bromo-3-iodoquinolin-4(1H)-one is described, based on regioselective sequentialExpand
Development and characterization of immobilized cannabinoid receptor (CB1/CB2) open tubular column for on-line screening.
The data from this study confirm that the CB1/CB2-OT column can be used to determine the binding affinities (K(i) values) for a single compound and to screen individual compounds or a mixture of multiple compounds. Expand