6437-06-5

Upstream product

• 13906-09-7 2-thioxo-2,3-dihydro-1H-quinazolin-4-one 
• 80-48-8 methyl p-toluene sulfonate 
• 13906-09-7 2-mercapto-3H-quinazolin-4-one 
• 74-88-4 methyl iodide 
• 118-92-3 anthranilic acid 
• 1705-09-5 3-methyl-4-oxoquinazoline-2-thione 
• 77-78-1 dimethyl sulfate 
• 82018-09-5 2-mercapto-4(3H)-quinazolinone sodium salt 
• 54855-81-1 2-methylthioquinazolin-4(3H)-one 

Downstream Products

• 61507-80-0 2-hydrazino-3-methyl-4a,8a-dihydro-3H-quinazolin-4-one 
• 109791-99-3 3-methyl-2-<3-<3-(1-piperidinylmethyl)phenoxy>propylamino>-4(3H)-quinazolinone 

Relevant academic research and scientific papers

Identification and optimization of a new series of anti-tubercular quinazolinones

A high throughput phenotypic screening against Mycobacterium smegmatis led us to the discovery of a new class of bacteriostatic, highly hydrophobic antitubercular quinazolinones that potently inhibited the in vitro growth of either extracellular or intramacrophagic M. tuberculosis (Mtb), via modulation of an unidentified but yet novel target. Optimization of the initial hit compound culminated in the identification of potent but poorly soluble Mtb growth inhibitors, three of which were progressed to in vivo efficacy studies. Despite nanomolar in vitro potency and attractive PK properties, none of these compounds was convincingly potent in our in vivo mouse tuberculosis models. This lack of efficacy may be linked to the poor drug-likeness of the test molecules and/or to the properties of the target.[Figure presented]

PYRIMIDINE DERIVATIVE

This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X 1 stands for hydrogen, lower alkyl, amino, etc., X 2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0 - 4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT 3 antagonistic agent which concurrently exhibits 5-HT 1A agonistic activity, or administering 5-HT 1A agonistic agent and 5-HT 3 antagonistic agent simultaneously, in sequence or at an interval.

Phase-transfer catalyzed alkylation and cycloalkylation of 2-mercaptoquinazolin-4(3H)-one

Solid/liquid phase-transfer catalyzed alkylation of 2-mercaptoquinazolin- 4(3H)-one at 25°C by different organohalogen compounds in the presence of tetrabutylammonium bromide as a catalyst underwent, exclusively, S-monoalkylation or S- and N-, di-, or cyc

Synthesis of 2-aminoquinazoline-4(3H)-one derivatives as potential potassium channel openers

Starting from 2-thioxoquinazolin-4-one, the synthesis of 2-amino-4(3H)- one derivatives, structurally related to potassium channels openers pinacidil and diazoxide, is described.

SYNTHESIS OF 2-ALKYLTHIOQUINAZOL-4-ONES

Alkylation of 2-thioxoquinazol-4-one by different alkylating agents was studied, and it was found that the reaction proceeds at the exocyclic sulfur atom with the formation of 2-alkylthioquinazol-4-ones.

SYNTHESIS AND SPECTRAL EXAMINATION OF THE POSITION OF TAUTOMERIC EQUILIBRIUM IN 2-THIOXO-4-QUINAZOLONE

2-Thioxo-4-quinazolone and its derivatives mono- and dimethylated at ring atoms N(1) and N(3) and the exocyclic sulfur have been synthesized.Using model compounds, UV spectroscopy has been used to show that 2-thioxo-4-quinazolone exists in the thioketo-form, no appreciable amounts of the thiol or enol isomers being present.

SYNTHESIS AND ALKYLATION OF 2-MERCAPTO-4-QUINAZOLONE AND THE FUNGICIDAL ACTIVITIES OF THE COMPOUNDS OBTAINED

A convenient method of obtaining 2-mercapto-4-quinazolone has been developed and the alkylation of its ambidentate anions has been studied.It has been found that they exhibit a dual reactivity in alkylation reactions.It has been shown that alkylated 2-mercapto-4-quinazolones possess a moderate fungicidal activity.