66299-68-1Relevant academic research and scientific papers
Molecular modeling study and synthesis of quinazolinone-arylpiperazine derivatives as α1-adrenoreceptor antagonists
Abou-Seri, Sahar Mahmoud,Abouzid, Khaled,Abou El Ella, Dalal A.
scheme or table, p. 647 - 658 (2011/03/22)
Three series of new 2-[(4-substituted piperazin-1-yl) methyl]quinazolin- 4(3H)-ones 4a-c, Ethyl 6,7-dimethoxy-4-oxo-3-[2-(4-substituted piperazin-1-yl)acetamido/propanamido]-3,4-dihydroquinazoline-2-carboxylates 9a-f and their 2-methyl analogues 13a-l were designed and synthesized as promising α1-adrenoceptor antagonists. The final compounds were evaluated for their in vivo hypotensive activity in normotensive cats. The most potent hypotensive quinazolinone derivatives 4b, 9e, 13i, 13j were further tested on isolated thoracic aortic rings of male Wister rats. All the tested compounds displayed α1-blocking activity with IC50 ranging from 0.2 to 0.4 mM less than prazosin. Furthermore, in the present work, molecular modeling study using Accelrys Discovery Studio 2.1 software was performed by mapping the synthesized compounds to the α1- adrenoceptor antagonist hypothesis in order to predict their mechanism of action. Compound 13j which has the best-fitting score displayed the highest in vivo and in vitro activity among the tested compounds.
Quinazolin-4-one derivatives
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Page/Page column 29, (2010/11/24)
A medicament having an inhibitory activity against hematopoietic prostaglandin D2 synthase, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein X represents a group represented by the formula —N═C(R5)— or the formula —NH—CH(R5)—, R1, R2, R3, and R4 represent a hydrogen atom, a halogen atom, a C1 to C6 alkyl group, or a hydroxy group, R5 represents a C1 to C6 alkyl group or a C6 to C10 aryl group, and R represents an amino group.
Electron Deficient Heteroaromatic Ammonioamidates. Part 26. N-(Quinazolin-3-io)amidates. Part 13. Phototransformations of an N-(Quinazolin-3-io)thioamidate and of a 10bH-1,3,4-thiadiazoloquinazoline, the Ring Isomer of an N-(Quinazolin-3-io)thioamidate, and the Photochemical Fo
Lempert-Sreter, Magda,Lempert, Karoly,Moeller, Joergen
, p. 1143 - 1152 (2007/10/02)
Irradiation of the N-(quinazolin-3-io)thioamidate (10a) in ethanol and butylamine solution furnished, in addition to several other compounds, the 4,4'-biquinazolinyl (12a), the quinazolinyl alcohol (13a) and the quinazolinyl ketone (13b), respectively, the mesoionic triazoloquinazolinylium thiolate (18a) and the corresponding olate (18b) as novel type photolysis products.In contrast, irradiation of the 10bH-1,3,4-thiadiazoloquinazoline (11b), the ring isomer of the N-(quinazolin-3-io)thioamidate (10b) furnishes, with cleavage of either the quinazoline or the thiadiazole ring , a mixture of the thiadiazoles (21a,b), and the quinazoline derivatives (14a), (22a,b) in addition to 3,4-dimethoxybenzonitrile.Irradiation of various sulphur-containing quinazoline derivatives, including the quinazolinethiones (14a,e), the methylthioquinazoline (13f) and the diquinazolinyl disulphide (24a), leads to the formation of 4,4'-biquinazolinyls (12a) and (12b), respectively.Irradiation of the quinazoline (13c), which carries no sulphur-containing substituent, does not lead to the formation of the biquinazolinyl (12a); irradiation of a mixture of quinazoline (13e) and quinazolinethione (14a) gives rise to the formation of a mixture of biquinazolinyls (12a-c) with incorporation of the ring of the sulphur-free starting quinazoline (13e) into the products (12a) and (12b).
