Molecular Consortia—Various Structural and Synthetic Concepts for More Effective Therapeutics Synthesis

Abstract

The design and discovery of novel drug candidates are the initial and most probably the crucial steps in the drug development process. One of the tasks of medicinal chemistry is to produce new molecules that have a desired biological effect. However, even today the search for new pharmaceuticals is a very complicated process that is hard to rationalize. Literature provides many scientific reports on future prospects of design of potentially useful drugs. Many trends have been proposed for the design of new drugs containing different structures (dimers, heterodimers, heteromers, adducts, associates, complexes, biooligomers, dendrimers, dual-, bivalent-, multifunction drugs and codrugs, identical or non-identical twin drugs, mixed or combo drugs, supramolecular particles and various nanoindividuals. Recently much attention has been paid to different strategies of molecular hybridization. In this paper, various molecular combinations were described e.g., drug–drug or drug-non-drug combinations which are expressed in a schematic multi-factor form called a molecular matrix, consisting of four factors: association mode, connection method, and the number of elements and linkers. One of the most popular trends is to create small–small molecule combinations such as different hybrids, codrugs, drug–drug conjugates (DDCs) and small-large molecule combinations such as antibody-drug conjugates (ADCs), polymer-drug conjugates (PDCs) or different prodrugs and macromolecular therapeutics. A review of the structural possibilities of active framework combinations indicates that a wide range of potentially effective novel-type compounds can be formed. What is particularly important is that new therapeutics can be obtained in fast, efficient, and selective methods using current trends in chemical synthesis and the design of drugs such as the “Lego” concept or rational green approach.

In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine

“…However, the idea of its combining with other active compounds, pharmacophores, or moieties can lead to more profound results. The concept of creating molecular conjugates, hybrids, dimers, and other consortia brought drug discovery science to an entirely new unexplored dimension, which has been lately reviewed by Pawełczyk et al [29]. Therefore, we present different azulene derivatives and conjugates, including selected molecular consortia, which exhibite attractive potential for medicine and pharmacy.…”

Synthesis of Paeonol-Ozagrel Conjugate: Structure Characterization and In Vivo Anti-Ischemic Stroke potential

“…Through a logical combination of already known drugs and synthetic methods to produce new drugs that exhibit the desired effect, it could lead to a unique strengthening of activity along with minimizing the side effects (Bansal and Silakari, 2014;Shaveta et al, 2016). In the development of promising drug candidates in the field of medicinal chemistry, hybridization of drugs with complementary pharmacological action represents one of the most effective ways to design new leading candidates (Pawelczyk et al, 2018).…”

Microwave assisted synthesis, characterization and investigation of antibacterial activity of 3-(5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-2H-chromen-2-one derivatives

“…In view of the occurrence of microorganisms' resistance, increase in severe opportunistic microbial infections (Aslam et al, 2018) and the emergence of new diseases, there is a continuous need for the fast synthesis of new bioactive heterocyclic compounds as potential therapeutic agents. The combination of two different and independently linked hybrid compounds can display synergy and result in a pharmacological potency greater than the sum of each individual moiety's potency (PawelÁczyk et al, 2018). Hence, we have herein investigated the microwave assisted synthesis of pyrazoline-linked coumarin as a green synthetic approach to access biologically active coumarin scaffolds.…”