54535-61-4Relevant academic research and scientific papers
Synthesis, characterization, in vitro biological and molecular docking evaluation of N,N'-(ethane-1,2-diyl)bis(benzamides)
Aziz, Hamid,Saeed, Aamer,Jabeen, Farukh,Ullah, Nazif,Rehman, Ashfaq Ur
, p. 2425 - 2436 (2021/03/03)
The present research describes the synthesis, characterization, in vitro biological and docking evaluation of N,N'-(ethane-1,2-diyl)bis(benzamides) (3a-3j). Consequently, in in vitro hRBCs hemolysis assay, only the bis-amide (3d) induced 52.4% hemolysis at higher concentration (1000?μg/mL) that decreased drastically with concentration (250?μg/mL) to 27.9% (CC50 = 400.41). Similarly, the tested bis-amide (3j) was found to be the least toxic with 7.8% hemolysis at higher concentration (1000?μg/mL) that gradually decreases to 6.1% (CC50 = 19,347.83) at lower concentration (250?μg/mL). Accordingly, the tested bis-amides were found to be highly biocompatible against hRBCs at higher concentrations with much higher CC50 values (> 1000?μg/mL). The biocompatible bis-amides (3a-3j) were subjected to in vitro DNA ladder assay to analyze their apoptotic potential. The results obtained suggest the tested bis-amides (3a-3j) are highly degradative toward DNA causing the appearance of more than one bands or complete degradation of DNA except (3a), (3c), (3i) and (3?g). Moreover, the synthesized bis-amides (3a-3j) were tested in in vitro antileishmanial assay to unveil their leishmaniacidal potential. The results obtained clearly indicated that some of the tested bis-amides displayed good dose dependent response. The tested bis-amides were highly active at higher concentration (1000?μg/mL) against the leishmanial promastigotes and their % inhibitory potential decreased drastically with concentration (250?μg/mL). Consequently, at higher concentration (1000?μg/mL), the bis-amide (3f) caused 85% inhibition and was ranked as the most effective leishmaniacidal bis-amides followed by the bis-amide (3?g) with 73.54% inhibition of leishmanial promastigotes. However, in terms of their IC50 values, the best leishmaniacidal potential was displayed by the bis-amide (3f) followed by (3b), (3j) and (3?g) with IC50 values increasing in the order of 633.16, 680.22, 680.22 and 712.93?μg/mL, respectively. Molecular docking studies revealed that bis-amides having electron-donating groups showed good binding potential against antileishmanial target. Graphic abstract: [Figure not available: see fulltext.].
Competitive formation of N-diazeniumdiolates and N-nitrosamines via anaerobic reactions of polyamines with nitric oxide
Coneski, Peter N.,Schoenfisch, Mark H.
supporting information; experimental part, p. 5462 - 5465 (2010/02/28)
"Chemical Equation Presented" Reactions of amines with nitric oxide (NO) at high pressures form diverse NO donor species, highly dependent on the precursor structure. While monoamine precursors favor the formation of N-diazeniumdiolates in high yield, pol
