6484-28-2Relevant academic research and scientific papers
2-Alkyl(aryl)-quinazolin-4(3 H)-thiones, 2-R-(quinazolin-4(3 H)-ylthio)carboxylic acids and amides: Synthesis, molecular docking, antimicrobial and anticancer properties
Antypenko, Lyudmyla,Kovalenko, Sergiy,Posylkina, Yulia,Nikitin, Vladyslav,Fedyunina, Natalia,Ivchuk, Vitalii
, p. 253 - 265 (2016/02/03)
In this study, a series of novel 2-alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides were synthesized and evaluated for antimicrobial and anticancer activities. Their structure was confirmed by elemental analys
Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors
Sánchez, Ana I.,Martínez-Barrasa, Valentín,Burgos, Carolina,Vaquero, Juan J.,Alvarez-Builla, Julio,Terricabras, Emma,Segarra, Víctor
, p. 2370 - 2378 (2013/05/09)
The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7.
Syntheses of Some 4-Anilinoquinazoline Derivatives
Rocco, Silvana A.,Barbarini, Jose Eduardo,Rittner, Roberto
, p. 429 - 435 (2007/10/03)
Some 4-N-(3′- or 4′-substituted-phenyl)amino-6,7- dimethoxyquinazolines and the corresponding unsubstituted compounds were synthesized from 2-amino-4,5-dimethoxybenzoic acid and the appropriate substituted anilines. Other related quinazolines or their synthetic intermediates were also obtained. A large number of the described quinazolines are new compounds, while the remaining were prepared by a more efficient procedure. The main goal for the synthesis of these compounds comes from the fact that the 4-anilinoquinazoline pharmacophore is an important unit, which is found among the ATP-competitive inhibitors of several protein kinase enzymes.
Studies on quinazolines. Part I. Annelation to the quinazoline ring utilizing amino acid esters
Wasfy, Ashraf A. F.
, p. 1349 - 1358 (2007/10/03)
The reaction of quinazoline-4(3H)-thiones 2a-d with amino acid ester hydrochlorides in boiling solvents, under the basic catalysis, afforded the corresponding substitution products (3-6)a-e in low yield. The reaction could be improved by carrying it without a solvent yielding imidazo[1,2-c]- and pyrimido[1,2-c]quinazolines (7-10)a-e. The antibacterial and antifungal activities of the prepared compounds were tested.
Behaviour of β-(4-chloro-3-methyl)benzoyl Acrylic Acid Towards 2-Methyl-3H-quinazolin-4-thione
Marzouk, Magda I.,El-Aasar, Nadia
, p. 843 - 854 (2007/10/03)
β-(4-chloro-3-methyl)benzoylacrylic acid has been reacted with 2-methyl-(3H)-quinazolin-4-thione and gave α-thioquinazoline-β-(4-chloro-3-methyl)benzoyl propionic acid the behaviour of propionic acid derivative towards nitrogen nucleophiles, e.g., hydrazine hydrate, semicarbazide; acid anhydrides, acid amide and benzaldehyde has been discussed.
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds
Segarra, Victor,Crespo, M. Isabel,Pujol, Ferran,Beleta, Jorge,Domenech, Teresa,Miralpeix, Montserrat,Palacios, Jose M.,Castro, Ana,Martinez, Ana
, p. 505 - 510 (2007/10/03)
A 4-centre PDE 4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE 4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.
SYNTHESIS OF SOME HETEROCYCLIC COMPOUNDS WITH BRIDGEHEAD NITROGEN ATOMS
Chaurasia, M.R.,Sharma, Surendra K.
, p. 1759 - 1765 (2007/10/02)
3,5-Dimethyltriazoloquinazoline, 5-methyltetrazoloquinazoline, 5-methyl-s-triazoloquinazoline-3(2H)-thione, 2-quinazolin-3yl)-thiol>-N,N-benzyl-phenylacetanilide, hydrochlorides of 3-substituted phenyl-6-di
