New Advances in Chemical Research, May 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis.293298-33-6, Name is 3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanehydrazide hydrochloride, molecular formula is C7H10ClN3O3, belongs to pyrrolines compound, is a common compound. In a patnet, author is Bonatto, Vinicius, once mentioned the new application about 293298-33-6, Recommanded Product: 3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanehydrazide hydrochloride.
On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors having a reactive group (known as warhead) are subject to continuous studies to discover novel antichagasic compounds. Here, we evaluated how different warheads for a set of structurally similar related compounds could inhibit the activity of cruzipain and, ultimately, their trypanocidal effect. We first investigated in silico the intrinsic reactivity of these compounds by applying the Fukui index to correlate it with the enzymatic affinity. Then, we evaluated their potency against T. cruzi (Y and Tulahuen strains), which revealed the reversible cruzain inhibitor Neq0656 as a better trypanocidal agent (ECY50Y.strain = 0.1 mu M; SI = 58.4) than the current drug benznidazole (EC50Y.strain = 5.1 mu M; SI > 19.6). We also measured the half-life time by HPLC analysis of three lead compounds in the presence of glutathione and cysteine to experimentally assess their intrinsic reactivity. Results clearly illustrated the reactivity trend for the warheads (azanitrile > aldehyde > nitrile), where the aldehyde displayed an intermediate intrinsic reactivity. Therefore, the aldehyde bearing peptidomimetic compounds should be subject for in-depth evaluation in the drug discovery process.
The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, their interactions with reaction intermediates. Interested yet? Read on for other articles about 293298-33-6. Recommanded Product: 3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanehydrazide hydrochloride.
Reference:
Pyrroline – Wikipedia,
,1-Pyrroline | C4H7N – PubChem