Study of the antileishmanial activity of novel guanidine and hybrid acridine - guanidine compounds.

The inadequacies of the currently available treatment options for leishmaniasis, a highly prevalent but neglected tropical disease caused by protozoan parasites, urge the discovery and development of novel, safe, and efficacious antileishmanial drugs. In continuation of our work on N, N', N″-trisubstituted guanidines, which have shown promising results, we present in this study a series of new derivatives with further improved activity against the species Leishmania (Leishmania) amazonensis, Leishmania (Leishmania) infantum and Leishmania (Viannia) braziliensis. This enhancement was achieved by replacing the benzoyl group as one of the three guanidine substituents of the starting structures with an acridinyl group, which consistently decreased the IC values against the promastigote form of L.

Antifungal activity of guanidine compounds.

Guanidinic compounds are a class of compounds distributed in nature but also synthesized in vitro with a wide variety of applicability. One of the potentials of those molecules is antimicrobial activity. In that sense, although mainly limited to immunocompromised people, fungi pathogens are a cause of concern, even more so after the COVID-19 pandemic.

Guanidines Conjugated with Cell-Penetrating Peptides: A New Approach for the Development of Antileishmanial Molecules.

Leishmaniasis is a neglected tropical disease caused by a protozoan of the genus Leishmania, which has visceral and cutaneous forms. The symptoms of leishmaniasis include high fever and weakness, and the cutaneous infection also causes lesions under the skin. The drugs used to treat leishmaniasis have become less effective due to the resistance mechanisms of the protozoa.

Evidence of Guanidines Potential against : Exploring In Vitro Effectiveness, Toxicities and of Innate Immunity Response Effects.

Leishmaniasis is a complex group of infectious and parasitic diseases that afflict many thousands of individuals across five continents. Leishmaniasis treatment remains a challenge because it relies on drugsknown for their high toxicity and limited efficacy, making itimperative to identify new molecules that offer greater effectiveness and safety. This study sought to explore the impact of seven synthetic guanidine derivatives (LQOF-G1, LQOF-G2, LQOF-G6, LQOF-G7, LQOF-G32, LQOF-G35 and LQOF-G36) onthe parasite and in vitro macrophage infection by this parasite, as well as cytotoxic approaches in vitro models of mammalian host cells and tissues.

Development of New Leishmanicidal Compounds via Bioconjugation of Antimicrobial Peptides and Antileishmanial Guanidines.

Leishmaniasis refers to a collection of diseases caused by protozoa from the genus. These diseases, along with other parasitic afflictions, pose a significant public health issue, particularly given the escalating number of at-risk patients. This group includes immunocompromised individuals and those residing in impoverished conditions.

Novel Selective and Low-Toxic Inhibitor of CPB2.8ΔCTE (CPB) One Important Cysteine Protease for Virulence.

Leishmaniasis is a highly prevalent, yet neglected disease caused by protozoan parasites of the genus . In the search for newer, safer, and more effective antileishmanial compounds, we herein present a study of the mode of action in addition to a detailed structural and biological characterization of [-benzoyl-'-benzyl-″-(4-tertbutylphenyl)guanidine]. X-ray crystallography and extensive NMR experiments revealed that nearly exclusively adopts the conformation stabilized by an intramolecular hydrogen bond.

Synthesis and dopamine receptor binding of dihydrexidine and SKF 38393 catecholamine-based analogues.

Dopamine is an important neurotransmitter that regulates numerous essential functions, including cognition and voluntary movement. As such, it serves as an important scaffold for synthesis of novel analogues as part of drug development effort to obtain drugs for treatment of neurodegenerative diseases, such as Parkinson's disease. To that end, similarity search of the ZINC database based on two known dopamine-1 receptor (D1R) agonists, dihydrexidine (DHX) and SKF 38393, respectively, was used to predict novel chemical entities with potential binding to D1R.