28831-38-1Relevant academic research and scientific papers
Synthesis of methyl [3-alkyl-2-(2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl)-acetamido] alkanoate
Ismail, El Fekki,Ali, Ibrahim A.I.,Fathalla, Walid,Alsheikh, Amer A.,Tamney, El Said El
, p. 104 - 120 (2017/06/19)
A series of methyl [3-alkyl-2-(2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl)-acetamido] alkanoate 10-13a-f has been developed on the basis of the N-chemoselective reaction of 3-substituted quinazoline-2,4-diones 3a-d with ethyl chloroacetate and azide coupling method with amino acid ester hydrochloride. The precursor quinazoline diones 3a-d chemoselective reactions were studied using DFT(B3LYP)/6-311G level of theory and were prepared by a new rearrangement method from the corresponding 2-(3-methyl-4-oxo-3,4- dihydroquinazolin-2-ylthio) acetohydrazide 6. {figure presented}.
Small molecule mimetics of an interferon-α receptor interacting domain
Bello, Angelica M.,Wei, Lianhu,Majchrzak-Kita, Beata,Salum, Noruê,Purohit, Meena K.,Fish, Eleanor N.,Kotra, Lakshmi P.
, p. 978 - 985 (2014/02/14)
Small molecules that mimic IFN-α epitopes that interact with the cell surface receptor, IFNAR, would be useful therapeutics One such 8-amino acid region in IFN-α2, designated IRRP-1, was used to derive 11 chemical compounds that belong to 5 distinct chemotypes, containing the molecular features represented by the key residues Leu30, Arg33, and Asp35 in IRRP-1 Three of these compounds exhibited potential mimicry to IRRP-1 and, in cell based assays, as predicted, effectively inhibited IFNAR activation by IFN-α Of these, compound 3 did not display cell toxicity and reduced IFN-α- inducible STAT1 phosphorylation and STAT-DNA binding Based on physicochemical properties' analyses, our data suggest that moieties with acidic pKa on the small molecule may be a necessary element for mimicking the carboxyl group of Asp35 in IRRP-1 Our data confirm the relevance of this strategy of molecular mimicry of ligand-receptor interaction domains of protein partners for small molecule drug discovery
Synthesis and biological activities of 4-oxo thiazolidine derivatives
Sanghani,Sanja,Rajani,Godhani
experimental part, p. 557 - 560 (2009/08/07)
A series of 4-oxo-2-phenyl-thiazolidin-3-yl derivatives 5a-l have been obtained by cyclisation of various Schiff's base 4 with thioglycolic acid. The Schiff's base 4 are obtained by the reaction of appropriate carbonyl compound with (4-oxo-3-p-tolyl-3,4-dihydro-quinazolin-2-yl-sulfanyl)-acetic acid hydrazide 3. The product is characterized by spectral and analytical data. Most of the tested compounds show promising antibacterial and antifungal activity.
