Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 4474-86-6, Name is N-Cbz-D-Asparagine, molecular formula is , belongs to phthalazines compound. In a document, author is Romero, Angel H., Recommanded Product: N-Cbz-D-Asparagine.
Optimization of phthalazin-based aryl/heteroarylhydrazones to design new promising antileishmanicidal agents: synthesis and biological evaluation of 3-aryl-6-piperazin-1,2,4-triazolo[3,4-a]phthalazines
1-Monosubstituted and 1,4-substituted phthalazins based on aryl/heteroarylhydrazinyl have demonstrated attractive antileishmanial profiles against amastigote forms of theLeishmania braziliensisparasite. Further optimization of the mentioned acyclic scaffold motivated us to design a series of 3-aryl-1,2,4-triazolo[3,4-a]phthalazines, cyclic versions of the phthalazins based on aryl/heteroarylhydrazinyl, which have not been evaluated againstLeishmaniaparasites yet. In order to compare to phthalazine-based aryl/heteroarylhydrazones, five essential 3-aryl-6-piperazin-1,2,4-triazolo[3,4-a]phthalazines were efficiently prepared in excellent yields (73-83%) through a facile one-pot procedure from 4-chloro-1-phthalazinyl-arylhydrazonesviaC-H dehydrogenative cyclization using silver(i) salt. Fromin vitroantileismanial evaluation, compound2d, a nitro derivative, was identified as the most promising agent with a good anti-amastigote response (IC50= 9.37 mu M) and low relative toxicity against peritoneal macrophages (LD50= 123.93 mu M). A moderate response was found against clinical amastigote isolates ofL. braziliensis, although superior compared to the reference glucantime. A comparison with their phthalazin analogues based on aryl/heteroarylhydrazinyl gave evidence that the efficacy of each chemical system is determined by the nature of the functionalization next to the aryl moiety, which suggests that different mechanisms of action are involved for each chemical system. The cyclized form led to an enhancement of the antileismanial activity compared to the acyclic form, but the nitroderivatives seemed to be highly more toxic than the parent non-cyclized compounds. From the three compared phthalazine groups, 4-chloro-1-phthalazine-(5-nitrofuryl)hydrazinil with a nanomolar antileishmanial response was identified as a promising lead for further optimization, whereas compound2demerges as a prominent hit platform to prepare a group of derivatives based on phthalazine-1,2,4-triazolo bearing 3-nitro-phenyl at the 3-position.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 4474-86-6, in my other articles. Recommanded Product: N-Cbz-D-Asparagine.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem