Novel steroid derivatives: synthesis, antileishmanial activity, mechanism of action, and in silico physicochemical and pharmacokinetics studies was written by da Trindade Granato, Juliana;dos Santos, Juliana Alves;Calixto, Stephane Lima;Prado da Silva, Natalia;da Silva Martins, Jefferson;da Silva, Adilson David;Coimbra, Elaine Soares. And the article was included in Biomedicine & Pharmacotherapy in 2018.Related Products of 2387-23-7 This article mentions the following:
We investigated the antileishmanial activity and cytotoxicity of novel steroids against murine macrophages with a focus on the derivatives of cholesterol (CD), cholic acid (CA), and deoxycholic acid (DA). Furthermore, the mechanism of action of the best compound was assessed, and in silico studies to evaluate the physicochem. and pharmacokinetic properties were also conducted. Among the sixteen derivatives, schiffbase2, CD2 and DOCAD were effective against promastigotes of Leishmania species. Despite their low toxicity to macrophages, the majority of DOCADs were active against intracellular amastigotes of L. amazonensis, and DOCAD5 exhibited the best biol. effect against these parasitic stages (IC50 = 15.34 μM). Neither the CA derivatives (CAD) nor DA alone inhibited the intracellular parasites. Thus, the absence of hydroxyl in the C-7 position of the steroid nucleus, as well as the modification of the acid group in DOCADs were considered important for antileishmanial activity. The treatment of L. amazonensis promastigote forms with DOCAD5 induced biochem. changes such as depolarization of the mitochondrial membrane potential, increased ROS production and cell cycle arrest. No alterations in parasite plasma membrane integrity were observed In silico physicochem. and pharmacokinetic studies suggest that DOCAD5 could be a good candidate for an oral drug. The data demonstrate the potential antileishmanial effect of certain steroid derivatives and encourage new in vivo studies. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Related Products of 2387-23-7).
1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. As a result of interactions such as these, the water solubility of amides is greater than that of corresponding hydrocarbons. These hydrogen bonds are also have an important role in the secondary structure of proteins.Related Products of 2387-23-7
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics