Novel approaches to screening guanidine derivatives

Abstract

Guanidines, as they are both organically based and also hydrophilic in nature, have undergone a mammoth amount of screening and testing to discover promising lead structures with a CN3 core, appropriate for potential future drug development. The compounds have the potential to be neurodegenerative therapeutic options, as well as: anti-inflammatory, anti-protozoal, anti-HIV, chemotherapeutic, anti-diabetic agents and so on. It is true that guanidine-based compounds of natural sources also, like synthetic and virtually designed drugs, have been of significant interest and have the potential to be useful therapeutic options in the future. As for now, however, there is not sufficient data to support their use in a number of the suggested areas, and further studies are required.

<p>In vitro Antibacterial Activity of Isopropoxy Benzene Guanidine Against Multidrug-Resistant <em>Enterococci</em></p>

“…vancomycin-resistant Enterococci. According to the structure-activity relationship in robenidine analogues, the methylation saw a modest activity improvement, but only with the methoxy group (3-OCH3) (16). However, our compound with the isopropoxy group (3-OCH(CH3) 2 ) displayed a significant reduction in the MIC values against Enterococci.…”

“…14 Substituted benzene guanidine compounds belonging to amino-guanidine compound class have been used in the treatment of a broad range of diseases and emerged as candidates for further structural modification for new promising drugs. [15][16][17] For example, robenidine was synthesized as an anticoccidial agent widely used to prevent coccidian infections since the early 1970s. 18 Recently, robenidine analogues have been shown as Gram-positive antibacterial agents, including Staphylococcus aureus and vancomycin-resistant Enterococci.…”

Cyanobiphenyl versus Alkoxybiphenyl: Which Mesogenic Unit Governs the Mesomorphic Properties of Guanidinium Ionic Liquid Crystals?

“…[1][2][3][4][5] With high thermal stability, the ease of charge delocalization and coordination properties as well as the possibility to attach up to six different substituents on the guanidine moiety has driven research activities in diverse directions, resulting in their use as superbases, [6,7] ligands for coordination complexes, [8][9][10][11] organocatalysts, [12][13][14][15][16] stimuli-responsive materials, [17] hydrogels, [18] anion exchange polymer electrolytes for fuel cells, [19] and biologically active compounds [20][21][22][23][24][25][26][27][28][29] for drug development. Furthermore, guanidinium salts have also entered the field of ionic liquid crystals (ILCs) [30][31][32][33][34][35][36][37][38][39][40][41][42][43][44][45] as an alternative cationic head group to the imidazolium-derived ILCs, which have dominated this research area so far.…”

Synthesis of Polyalkylguanidine Hydrochloride Copolymers and Their Antibacterial Activity Against Conditionally Pathogenic Microorganisms Bacillus Cereus and Escherichia Coli

“…Therefore, their properties need to be constantly improved [10 -12]. The most critical directions for discovering new antimicrobial agents involve not only increasing their antimicrobial activity but also overcoming microorganism drug resistance [8], increasing their service life after the surface treatment, and reducing the toxicity, allergic reactions, and ecological hazard [13]. The biocidal activity and toxicity of polyguanidines can be broadly regulated by chemical modification of the macromolecular structure.…”