Nhiều dẫn xuất của quinoline-2-on đã được các nhà hóa học hữu cơ nghiên cứu để tổng hợp và đánh giá đặc tính sinh do tác dụng khác nhau chúng, bao gồm hoạt động kháng khuẩn, chống oxy hóa, viêm, ung thư. Sự kết 4-hydroxyquinoline-2-one với 2-amino-pyrimidine hoặc 2-pyrazoline có thể hình thành mới. Trong bài báo này, giả trình bày quả một số chất 2-aminopyrimidine mới đi từ ketone α,β-không no ...

A stereoselective practical synthetic route to indolmycin is described. The route is composed of the regioselective coupling of indolyl magnesium halide with a trans-epoxy ester, diastereoselective oxazolone ring formation with guanidine and amine exchange reaction with methylamine. In the coupling step, use of dichloromethane as co-solvent and conversion of the resulting hydroxy ester to the h...

Although the antibiotic streptomycin was isolated and characterized a number of years ago, little knowledge has accumulated concerning its synthesis by Xtreptonzyces griseus. In I954 Numerof, Gordon, Virgona, and O’Brien (1) administered glycine and acetate labeled in either the carboxyl or the (Y carbon to cultures of X. griseus. A low extent of incorporation of 1% into the streptomycin synthe...

The mutant h-lysozyme, W64CC65A, with Trp64 and Cys65 replaced by Cys and Ala, respectively, was secreted by yeast and purified. Peptide mapping confirmed that W64CC65A contained a nonnative Cys64-Cys81 bond and three native disulfide bonds. The mutant had 2% of the lytic activity of the wild-type lysozyme. The midpoint concentration of the guanidine hydrochloride denaturation curve, the [D]1/2...

Folding studies on proteases by the conventional hydrogen exchange experiments are severely hampered because of interference from the autolytic reaction in the interpretation of the exchange data. We report here NMR identification of the hierarchy of early conformational transitions (folding propensities) in HIV-1 protease by systematic monitoring of the changes in the state of the protein as i...

Guanidine hydrochloride has been widely used in the initial recovery steps of active protein from the inclusion bodies in aqueous two-phase system (ATPS). The knowledge of the guanidine hydrochloride effects on the liquid-liquid equilibrium (LLE) phase diagram behavior is still inadequate and no comprehensive theory exists for the prediction of the experimental trends. Therefore the effect the ...

The mol-ecular structure of the title compound, C(18)H(23)N(3)S, shows it to be a derivative of an amino-thio-phenol possessing a tetra-methyl-guanidine group with a localized C=N double bond of 1.304 (2) Å and a protected thiol functional group as an S-benzyl thio-ether. The two aromatic ring planes make a dihedral angle of 67.69 (6)°.

The reaction of aqueous solutions of amino-guanidine hydrogennitrate and acetyl-acetone produces the title pyrazole salt, C(7)H(18)N(8) (2+)·2NO(3) (-). The crystal structure is stabilized by a complex N-H⋯O hydrogen-bonding network. The difference in the engagement of the two nitrate anions in hydrogen bonding is reflected in the variation of the corresponding N-O bond lengths.

Mechanism-based inhibition of influenza neuraminidases by difluorosialic acids (DFSA) is not only rendered highly specific by incorporation of 4-amino or 4-guanidine substituents but also the half-life for reactivation is greatly increased. Measurement of rate constants for spontaneous hydrolysis of a series of such substituted DFSAs reveals, surprisingly, that inherent inductive effects play v...

This report focus on phase behavior of polyethylene glycol (PEG)4000/ phosphate/ guanidine hydrochloride/ water system at different guanidine hydrochloride concentrations and pH. The binodal of the systems was displaced toward higher concentrations of the components with increasing guanidine hydrochloride concentrations. The partition coefficient of guanidine hydrochloride was near unity and in...