Dual inhibition: a novel promising pharmacological approach for different disease conditions

Abstract

To overcome the problems associated with polypharmacy, which include medication non compliance, adverse drug reactions, drug-drug interactions and increased pill-burden, various strategies, such as sustained-release drugs and fixed-dose combination regimens (polypills), have been developed. Out of these, a novel and very much promising approach is the use of dual-action drugs. Amongst the dual-action drugs, there is a class of compounds known as dual inhibitors, which possess the dual inhibitory activity. The most common examples of dual inhibitors are rivastigmine, ladostigil, asenapine, phenserine, amitriptyline, clomipramine, doxepin and desipramine. This review article focuses on the conventional drugs used in different diseases which possess dual inhibition activity as well as those which are still in the preclinical/clinical phase.

Synthesis and X-ray Structural Analysis of the Ruthenium(III) Complex Na[trans-RuCl4(DMSO) (PyrDiaz)], the Diazene Derivative of Antitumor NAMI-Pyr

“…10 A promising alternative to these so-called cocktails are hybrid molecules that are composed of two or more covalently bound drugs; the compounds that can possess combined pharmacological properties of the individual drugs 10,11 yet superior synergistic effects. 12,13 Over the past years, we have investigated redox-active 14 diazenecarboxamides as potential anti-cancer agents. 15 The results of the in vitro experiments suggested that they likely target tumour cell redox mechanism by oxidation of glutathione into glutathione disulphide.…”

Understanding Acetylcholinesterase Inhibitors: Computational Modeling Approaches

“…91 THA analogues are widely investigated and tested for inhibition of AChE. One of AChEIs derived from THA most studied is the Bis(n)-tacrine derivative, as shown in Figure 11, formed from two units of THA connected by a carbon skeleton with (CH2)n units.…”

“…44,57,91 There are several compounds from acridines derivatives proposed as AChEI candidate. The photosensitizer methylene blue (MTB) 93 a strong reversible AChEI, and the edrophonium (EDR) are two of them.…”

“…91 The phenserine (PHS) is a phenyl carbamate analog of physostigmine developed for AD treatment. It is a highly selective and pseudo-irreversible AChEI.…”

“…In addition LAD possesses multiple therapeutic activities as reduces apoptosis and stimulates the processing of APP protein. 91 LAD nowadays is in II phase of clinic test for AD treatment. The high complexity of AD calls for huge effort to develop molecules able to modulate multiple CNS targets to promote a real improvement of AD therapy.…”