- 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
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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
- Antypenko, Lyudmyla,Kovalenko, Sergiy,Posylkina, Yulia,Nikitin, Vladyslav,Fedyunina, Natalia,Ivchuk, Vitalii
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p. 253 - 265
(2016/02/03)
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- Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors
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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.
- Sánchez, Ana I.,Martínez-Barrasa, Valentín,Burgos, Carolina,Vaquero, Juan J.,Alvarez-Builla, Julio,Terricabras, Emma,Segarra, Víctor
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p. 2370 - 2378
(2013/05/09)
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- Syntheses of Some 4-Anilinoquinazoline Derivatives
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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.
- Rocco, Silvana A.,Barbarini, Jose Eduardo,Rittner, Roberto
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p. 429 - 435
(2007/10/03)
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- Behaviour of β-(4-chloro-3-methyl)benzoyl Acrylic Acid Towards 2-Methyl-3H-quinazolin-4-thione
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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.
- Marzouk, Magda I.,El-Aasar, Nadia
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p. 843 - 854
(2007/10/03)
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- Studies on quinazolines. Part I. Annelation to the quinazoline ring utilizing amino acid esters
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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.
- Wasfy, Ashraf A. F.
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p. 1349 - 1358
(2007/10/03)
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- Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds
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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.
- Segarra, Victor,Crespo, M. Isabel,Pujol, Ferran,Beleta, Jorge,Domenech, Teresa,Miralpeix, Montserrat,Palacios, Jose M.,Castro, Ana,Martinez, Ana
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p. 505 - 510
(2007/10/03)
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- SYNTHESIS OF SOME HETEROCYCLIC COMPOUNDS WITH BRIDGEHEAD NITROGEN ATOMS
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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
- Chaurasia, M.R.,Sharma, Surendra K.
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p. 1759 - 1765
(2007/10/02)
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