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The functions and structure of ABC transporters: implications for the design of new inhibitors of Pgp and MRP1 to control multidrug resistance (MDR).
The most recent discoveries on the structures and functions of the ABC super family, in particular Pgp and MRP are reviewed and the medicinal chemistry of MDR reverters is discussed and the molecules that are presently in development are reviewed.
Cholinergic nicotinic receptors: Competitive ligands, allosteric modulators, and their potential applications
This review focuses on the structure of new ligands for nAChRs, agonists, antagonists and allosteric modulators, and on their possible applications.
Central Nicotinic Receptors: Structure, Function, Ligands, and Therapeutic Potential
This review focuses on the structure of the new agonists, antagonists, and allosteric ligands of nicotinic receptors, it highlights the current knowledge on the binding site models as a molecular modeling approach to design new compounds, and it discusses the nAChR modulators which have entered clinical trials.
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
Several compounds with a 4-aminopiperidine scaffold decorated on both nitrogen atoms by alkyl or acyl moieties containing the structural motifs of verapamil and of flunarizine, as well as those that
DM235 (sunifiram): a novel nootropic with potential as a cognitive enhancer
Results indicate that DM235, a compound structurally related to piracetam, is a novel nootropic endowed with the capability to prevent cognitive deficits at very low doses, and its potency is about 1,000 times higher than that of the most active Piracetam-like compounds.
Design and study of piracetam-like nootropics, controversial members of the problematic class of cognition-enhancing drugs.
Reasons for the problems encountered by nootropics, compounds therapeutically available and those in development, their structure activity relationships and mechanisms of action are discussed and the class is examined in more detail.
Design, synthesis, and in vitro activity of catamphiphilic reverters of multidrug resistance: discovery of a selective, highly efficacious chemosensitizer with potency in the nanomolar range.
One of the compounds presented presents a pharmacological profile (unprecedented nanomolar potency, high reversal of MDR, low cardiovascular activity) that makes it a promising drug candidate to treat MDR and a useful tool for studying P-glycoprotein.