green synthesis and urease inhibitory activity of spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives
نویسندگان
چکیده
sulfonic acid functionalized sba-15 (sba-pr-so3h) with pore size 6 nm as an efficient heterogeneous nanoporous solid acid catalyst exhibited good catalytic activity in the biginelli-like reaction in the synthesis of spiroheterobicyclic rings with good yield and good recyclability. spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives were synthesized in a simple and efficient method using the one-pot three-component reaction of a cyclic 1,3- dicarbonyl compounds (barbituric acid), an aromatic aldehyde and urea or thiourea in the presence of nanoporous silica sba-pr-so3h under solvent free conditions. urease inhibitory activity of spiro compounds were tested against jack bean urease using berthelot alkaline phenol–hypochlorite method. five of 13 compounds were inhibitor and two of them were enzyme activators. analysis of the docking results showed that, in most of the spiro molecules, one of the carbonyl groups is coordinated with both nickel atoms, while the other one is involved in the formation of hydrogen bonds with important active-site residues. the effect of inserting two methyl groups on n atoms of barbiturate ring, s substituted, ortho, meta and para substituted compounds were investigated too.
منابع مشابه
Green Synthesis and Urease Inhibitory Activity of Spiro-pyrimidinethiones/spiro-Pyrimidinones-barbituric Acid Derivatives
Sulfonic acid functionalized SBA-15 (SBA-Pr-SO3H) with pore size 6 nm as an efficient heterogeneous nanoporous solid acid catalyst exhibited good catalytic activity in the Biginelli-like reaction in the synthesis of spiroheterobicyclic rings with good yield and good recyclability. Spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives were synthesized in a simple and efficient ...
متن کاملGreen Synthesis and Urease Inhibitory Activity of Spiro-pyrimidinethiones/spiro-Pyrimidinones-barbituric Acid Derivatives
Sulfonic acid functionalized SBA-15 (SBA-Pr-SO3H) with pore size 6 nm as an efficient heterogeneous nanoporous solid acid catalyst exhibited good catalytic activity in the Biginelli-like reaction in the synthesis of spiroheterobicyclic rings with good yield and good recyclability. Spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives were synthesized in a simple and efficient ...
متن کاملGreen Synthesis and Urease Inhibitory Activity of Spiro-Pyrimidinethiones/Spiro-Pyrimidinones-Barbituric Acid Derivatives.
Sulfonic acid functionalized SBA-15 (SBA-Pr-SO3H) with pore size 6 nm as an efficient heterogeneous nanoporous solid acid catalyst exhibited good catalytic activity in the Biginelli-like reaction in the synthesis of spiroheterobicyclic rings with good yield and good recyclability. Spiro-pyrimidinethiones/spiro-pyrimidinones-barbituric acid derivatives were synthesized in a simple and efficient ...
متن کاملSynthesis and dynamics studies of barbituric acid derivatives as urease inhibitors
BACKGROUND Discovery of potent inhibitors of urease (jack bean) enzyme is the first step in the development of drugs against diseases caused by ureolytic enzyme. RESULTS Thirty-two derivatives of barbituric acid as zwitterionic adducts of diethyl ammonium salts were synthesized. All synthesized compounds (4a-z and 5a-s) were screened for their in vitro inhibition potential against urease enzy...
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عنوان ژورنال:
iranian journal of pharmaceutical researchجلد ۱۴، شماره ۴، صفحات ۱۱۰۵-۱۱۱۴
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