In Vitro Anti-Toxoplasma gondii and Antimicrobial Activity of Amides Derived from Cinnamic Acid

Abstract

Most cinnamic acids, their esters, amides, aldehydes, and alcohols present several therapeutic actions through anti-inflammatory, antitumor, and inhibitory activity against a great variety of microorganisms. In this work, eight amines derived from cinnamic acid were synthesized and tested against host cells infected with Toxoplasma gondii and the bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus epidermidis, and three strains of Staphylococcus aureus. Compounds 3 and 4 showed the best result against intracellular T. gondii, presenting antiparasitic activity at low concentrations (0.38 and 0.77 mM). The antibacterial activity of these compounds was also evaluated by the agar microdilution method, and amides 2 and 5 had a minimum inhibitory concentration of 250 µg mL−1 against two strains of S. aureus (ATCC 25923 and bovine strain LSA 88). These also showed synergistic action along with a variety of antibiotics, demonstrating that amines derived from cinnamic acid have potential as pharmacological agents.

Novozym 40086 as a novel biocatalyst to improve benzyl cinnamate synthesis

“…Cinnamic acid (3-phenylacrylic acid) is one kind of phenolic acid widely present in plants, which can be used in avoring materials and skin care products. [1][2][3] However, the high melting point (133 C) and poor solubility of cinnamic acid limit its application. Benzyl cinnamate (melting point 34.5 C), one of the derivatives of cinnamic acid, was oen used as a avoring agent and antioxidant in the food, cosmetic and medicine industries.…”

Cinnamic Acid Conjugates in the Rescuing and Repurposing of Classical Antimalarial Drugs

“…Therefore, this work conveyed the disclosure of CAD as inhibitors of the new permeability pathways (NPP) induced by Plasmodium in erythrocytes to enable the translocation of carbohydrates and amino acids [46][47][48][49]. Following this pioneering discovery, other authors have proposed different CA-inspired compounds as potential therapeutic agents against malaria [26,28,29], as well as other parasitic diseases [50][51][52]. In view of this, reports have emerged over the past decade where conjugation to CA was proposed as a useful strategy for the rescuing of known antimalarials [53][54][55].…”

“…Molecules 2020, 24, x FOR PEER REVIEW 3 of 15 malaria [26,28,29], as well as other parasitic diseases [50][51][52]. In view of this, reports have emerged over the past decade where conjugation to CA was proposed as a useful strategy for the rescuing of known antimalarials [53][54][55].…”

The Mechanism of Action of Ursolic Acid as a Potential Anti-Toxoplasmosis Agent, and Its Immunomodulatory Effects

“…However, existing drugs are widely vulnerable to drug-resistance in clinics globally. To overcome pharmacological barriers to these challenges, the efforts for treating infectious diseases have been attempted in various fields, and it has been reported that various extracts/compounds derived from medicinal plants and new synthetic compounds have anti- T. gondii effects in the in vitro and pre-clinic stages [10,11,12,13,14,15]. Until recently, various compounds derived from plants have showed a leading role and ability as a source of specialized metabolites with medical effects as well as pharmacological activities.…”