The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states. 611-73-4, Name is 2-Oxo-2-phenylacetic acid, molecular formula is C8H6O3, belongs to phthalazine compound. In a document, author is Romero, Angel H., introduce the new discover, Computed Properties of https://www.ambeed.com/products/611-73-4.html.
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.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem