In an article, author is Bhat, Saleem Yousuf, once mentioned the application of 97-90-5, HPLC of Formula: C10H14O4, Name is Ethane-1,2-diyl bis(2-methylacrylate), molecular formula is C10H14O4, molecular weight is 198.22, MDL number is MFCD00008590, category is thiazolidines. Now introduce a scientific discovery about this category.
Development of quinoline-based hybrid as inhibitor of methionine aminopeptidase 1 fromLeishmania donovani
Methionine aminopeptidase 1 (MetAP1) is a target for drug discovery against many adversaries and a potential antileishmanial target for its role in N-terminal methionine processing. As an effort towards new inhibitor discovery against methionine aminopeptidase 1 fromLeishmania donovani(LdMetAP1), we have synthesized a series of quinoline-based hybrids, that is (Z)-5-((Z)-benzylidine)-2-(quinolin-3-ylimino)thiazolidin-4-ones (QYT-4a-i) whose in vitro screening led to the discovery of a novel inhibitor molecule (QYT-4h) againstLdMetAP1. The compound QYT-4h showed nearly 20-fold less potency for human MetAP1 and had drug-like features. Time-course kinetic assays suggested QYT-4h acting through a competitive mode by binding to the metal-activated catalytic site. Notably, QYT-4h was most potent against the physiologically relevant Mn(II) and Fe(II) supplemented forms ofLdMetAP1 and less potent against Co(II) supplemented form. Surface plasmon resonance and fluorescence spectroscopy demonstrated high affinity of QYT-4h forLdMetAP1. Through molecular modelling and docking studies, we found QYT-4h binding at theLdMetAP1 catalytic pocket occupying both the catalytic and substrate binding sites mostly with hydrogen bonding and hydrophobic interactions which provide structural basis for its promising potency. These results demonstrate the feasibility of employing small-molecule inhibitors for selective targeting ofLdMetAP1 which may find use to effectively eliminate leishmaniasis.
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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com