With the volume and accessibility of scientific research increasing across the world, it has never been more important to continue building the reputation for quality and ethical publishing we’ve spent the past two centuries establishing.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, Category: pyrrolines.
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.
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Reference:
Pyrroline – Wikipedia,
,1-Pyrroline | C4H7N – PubChem