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.

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.

Leishmanicidal Activity of Guanidine Derivatives against .

Leishmaniasis is a neglected tropical infectious disease with thousands of cases annually; it is of great concern to global health, particularly the most severe form, visceral leishmaniasis. Visceral leishmaniasis treatments are minimal and have severe adverse effects. As guanidine-bearing compounds have shown antimicrobial activity, we analyzed the cytotoxic effects of several guanidine-bearing compounds on in their promastigote and amastigote forms in vitro, their cytotoxicity in human cells, and their impact on reactive nitrogen species production.

Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.

Atypical dopamine reuptake inhibitors, such as modafinil, are used for the treatment of sleeping disorders and investigated as potential therapeutics against cocaine addiction and for cognitive enhancement. Our continuous effort to find modafinil analogues with higher inhibitory activity on and selectivity toward the dopamine transporter (DAT) has previously led to the promising thiazole-containing derivatives CE-103, CE-111, CE-123, and CE-125. Here, we describe the synthesis and activity of a series of compounds based on these scaffolds, which resulted in several new selective DAT inhibitors and gave valuable insights into the structure-activity relationships.

N, N', N″-trisubstituted guanidines: Synthesis, characterization and evaluation of their leishmanicidal activity.

Leishmaniasis is a group of diseases caused by protozoan parasites from the genus Leishmania. There are estimated 1.3 million new cases annually with a mortality of 20,000-30,000 per year, when patients are left untreated.

Benzenesulfonamides act as open-channel blockers on K3.1 potassium channel.

K3.1 blockers can serve as modulators of the rate of action potential firing in neurons with high rates of firing such as those of the auditory system. We studied the effects of several bioisosteres of N-alkylbenzenesulfonamides, and molecules derived from sulfanilic acid on K3.

Correction to: 4-Chloro-3-nitro-N-butylbenzenesulfonamide acts on K3.1 channels by an open-channel blocker mechanism.

Unfortunately, grey trace on Figure 2c was missing in the original publication of the article.

4-Chloro-3-nitro-N-butylbenzenesulfonamide acts on K3.1 channels by an open-channel blocker mechanism.

The effects of 4-chloro-3-nitro-N-butylbenzenesulfonamide (SMD2) on K3.1 channels, heterologous expressed in L-929 cells, were studied with the whole cell patch-clamp technique. SMD2 blocks K3.

Molecular architecture of thin films fabricated via physical vapor deposition and containing a poly(azo)urethane.

Organic thin films are widely applied as transducers in devices whose performance is determined by the optical and electrical properties of the films. In this context, the molecular architecture of the thin films plays an important role. In this work we report the fabrication and characterization of a poly(azo)urethane synthesized fixing CO2 in bis-epoxide followed by a copolymerization reaction with an azodiamine without using isocyanate.