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1.
Y Kawashima M Sato Y Hatada J Goto Y Nakashima K Hatayama S Shibuya 《Chemical & pharmaceutical bulletin》1990,38(2):393-399
Treatment of (E)-3-(2-hydroxypropylidene)-4-methyl-1-phenylazetidin-2-one (11) with 10% Pd/C gave (E)-(12), (Z)-3-(2-oxopropylidene)-4-methyl-1-phenylazetidin-2-one (13), 3,4-cis-(14a) and 3,4-trans-3-(2-oxopropyl)-4-methyl-1-phenylazetidin-2-one (14b). Among them, 12 and 13 were found to show potent inhibitory activities against rabbit platelet-rich plasma aggregation induced by adenosine diphosphate or collagen. Ring-expanded homologous derivatives and an acyclic analogue of 12 were also synthesized and tested for the biological activities. The azetidin-2-one skeleton bearing a 2-oxoalkylidene moiety at the 3 position was found to be essential for the platelet aggregation inhibitory activities of these compounds. 相似文献
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A Iyobe M Uchida K Kamata Y Hotei H Kusama H Harada 《Chemical & pharmaceutical bulletin》2001,49(7):822-829
A series of 6-cyclic aliphatic amino-7-nitro-3,4-dihydroquinoline-2(1H)-ones were prepared and tested for platelet aggregation inhibitory effect, cardiotonic activity and chronotropic activity. These compounds appeared to show selective inhibitory activity against platelet aggregation. Among them, 6-(4-ethoxycarbonylpiperidino)-7-nitro-3,4-dihydroquinoline-2(1H)-one (22f) showed the most potent inhibitory activity and high selectivity. A divergent synthetic route to 6-cyclic aliphatic amino-7-nitro-3,4-dihydroquinoline-2(1H)-one derivatives has also been investigated. 相似文献
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Four stereoisomers of the title compounds based on side chain ring junctions, (+)-7a, (+)-7b, (-)-7c and (-)-24, were synthesized from (-)-myrtenol and (+)-nopinone. The (1R,2R,3S,5S)-isomer (+)-7b had the most potent inhibitory activity against platelet aggregation and did not show partial agonist activity (shape change of platelets). We also synthesized the antipode, (-)-7b, and derivatives of (+)-7b with various kinds of substituents at the sulfonylamino group, 34a-n and p. The one-carbon homologated compound, (+)-58, was also prepared. The inhibitory activities of these compounds against platelet aggregation were measured. 相似文献
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<正>A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent. 相似文献
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4-Aryl derivatives of 7-ethoxycarbonyl-6,8-dimethyl-1(2H)-phthalazinone and related derivatives were newly synthesized in order to test for their inhibitory activities on platelet aggregation. 4-(2-Anisyl) compound and the corresponding 1-chloro derivative demonstrated significant activity. 相似文献
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6-(4-取代苯基)-5-甲基-4,5二氢-3(2H)哒嗪酮化合物的合成及其抑制血小板聚集作用 总被引:3,自引:0,他引:3
血小板聚集在血栓形成中起着先导而关键的作用,而严重威胁人类生命健康的心脑血管疾病多数与血栓形成和血栓栓塞有着密切的联系[1]。二氢哒嗪酮类化合物对抑制血小板聚集有较强的药理活性,对二磷酸腺苷(ADP)、花生四烯酸(AA)、血小板活化因子(PAF)和胶原(Collagen)引起的血小板聚集均有抑制作用。深入研究二氢哒嗪酮类化合物的构效关系,以期寻找活性更强的抗血小板聚集药物,是开发新型心脑血管系统疾病药物的重要研究方向之一。本文设计合成了6-(4-取代苯基)-5-甲基-4,5二氢-3(2H)哒嗪酮类化合物[2,3,4],并进行了体外药理实验。1实验部… 相似文献
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A Tanaka K Ito S Nishino Y Motoyama H Takasugi 《Chemical & pharmaceutical bulletin》1992,40(12):3206-3213
5-Alkyl-2-aryl-4-pyridylimidazoles were synthesized and tested in rat ex vivo platelet aggregation studies. Among these compounds, 2-(2-fluorophenyl)-5-methyl-4-(3-pyridyl)imidazole (25) was most potent, and showed 98% inhibition at a dose of 10 mg/kg (p.o.). 25 had inhibitory activity on cyclooxygenase, thromboxane A2 (TXA2) synthetase, and phosphodiesterase, and also showed inhibited KCl-induced contraction of rat aorta. All compounds have little acute toxicity and appear to be free of adverse effects on the stomach. 相似文献
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Diphenylimidazole and diphenylthiazole derivatives were synthesized and tested as inhibitors of platelet aggregation in in vitro experiments with the rabbit. Diphenylthiazole derivatives (10) were more potent than diphenylimidazole derivatives (4) in inhibiting arachidonic acid-induced platelet aggregation of rabbit platelet-rich plasma. Two diphenylimidazole and eight diphenylthiazole derivatives were evaluated for ex vivo arachidonic acid and collagen-induced platelet aggregation inhibitory activity using guinea pigs. In these compounds, 4,5-bis(4-methoxyphenyl)-2-(1,5-dimethyl-2-pyrrolyl)thiazole (10n) showed strong activity in vitro and ex vivo. The ex vivo activity of 10n was 200 times stronger than that of aspirin. The mechanism of the activity of 10n was the inhibition of cyclo-oxygenase. 相似文献
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T Tsuri N Haga T Matsui S Kamata H Kakushi K Uchida 《Chemical & pharmaceutical bulletin》1992,40(1):75-84
New platelet activating factor (PAF) antagonists, 3 were synthesized by replacing the charged phosphate and trimethylammonium moieties with sulfonamide and heterocyclic quaternary ammonium functionalities, respectively (PAF-sulfonamide isosteres). Darmstoff phosphatidic acid analogues of this class (Darmstoff-sulfonamide isosteres), 6 were also synthesized. The activity of these compounds as PAF antagonists was evaluated from their in vitro inhibitory effect on PAF-induced platelet aggregation in rabbit platelet-rich plasma. Among the compounds tested, some of the 2-methoxypropane derivatives with an octadecylcarbamoyloxy or octadecylcarbamoylthio side chain at the 1-position and a propylsulfonamide function bearing a terminal polar substituent such as a quaternary quinolinium or substituted quinolinium group at the 3-position were found to be the most potent (IC50 = 0.3-0.6 microM). 相似文献
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Y Eguchi F Sasaki Y Takashima M Nakajima M Ishikawa 《Chemical & pharmaceutical bulletin》1991,39(3):795-797
Derivatives of 7-ethoxycarbonyl-4-formyl-6,8-dimethyl-1(2H)-phthalazinone and closely related compounds were synthesized using Wittig and epoxidation reactions. Ring opening amination of the epoxides were carried out using dimethylaluminum amide reagents under mild reaction conditions. beta-Keto ester and beta-diketone moieties were introduced through diazo derivatives. These moieties were reacted with hydrazine hydrate to produce 4-pyrazolyl derivatives. The derivatives were tested for their inhibitory effect on platelet aggregation, and their relaxing effect on blood vessels. 相似文献
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Fan Zhang Dang Wu Gao-Lei Wang Shuang Hou Ping Ou-Yang Jin Huang Xiao-Yong Xu 《中国化学快报》2017,28(5):1044-1048
A series of novel 1,2,3-benzotriazin-4-one derivatives were designed,synthesized and their inhibitory activities against leulcotriene A_4 hydrolase aminopeptidase in vitro were evaluated.Many compounds showed moderate to good activities at the concentration of 10 μmol/L.Among them,compound Ⅳ-16 exhibited the highest inhibitory activity up to 80.6% with an IC_(50) of 1.30 ± 0.20 μmol/L The compound Ⅳ-16 was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA_4H enzyme by molecular docking was studied.It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study.The relationship between structure and inhibitory activity was also preliminarily discussed. 相似文献
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To discover new chemotypes of nematicides with proper toxicological profiles, a series of novel 1,2,3- benzotriazin-4-one derivatives were synthesized and further bioevaluated. The bioassay results showed that most of the synthesized compounds were endowed with moderate to good control efficacy against Meloidogyne incognita at 10.0 mg/L in vivo. Among them, compounds 6k and 6p displayed 100% inhibitory activities at this concentration, which implied that they could be used as lead compounds for promising nematicides. 相似文献
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Gülay Akyüz 《Journal of heterocyclic chemistry》2021,58(5):1164-1170
In this study, novel quinazolinones were designed, synthesized, characterized by FT-IR, 1H-NMR, 13C-NMR spectral data, and LC–MS. New compounds inhibitory activities on urease were assessed. All of the compounds exhibited potent urease inhibitory activities. Especially in the synthesized compounds, 2-benzyl-3-({5-[(4-nitrophenyl)amino]-1,3,4-thiadiazol2-yl}methyl)quinazolin-4(3H)-one has the best inhibitory effect against Jack bean urease with IC50 = 3.30 ± 0.09 μg/mL. And also, N-(4-nitrophenyl)-2-[(4-oxoquinazolin-3(4H)-yl)acetyl] hydrazinecarbothioamide, N-(4-fluorophenyl)-2-[(4-oxoquinazolin-3(4H)-yl)acetyl] hydrazinecarbothioamide, and 2-benzyl-3-({5-[(4-fluorophenyl)amino]-1,3,4-thiadiazol-2yl} methyl)quinazolin-4(3H)-one have best activities among the synthesized compounds. 相似文献
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噻吩并[3,2-c]四氢吡啶和噻吩并[2,3-c]四氢吡啶分别与取代苄溴(2a~2g)经取代反应后,用2 mol·L-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(3b~3e, 3g和5a~5g);噻吩并[3,2-c]四氢吡啶酮与取代苄溴经取代反应,再与乙酸酐缩合,最后经2 mol·L-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(7d, 7e, 7g~7i)。 3, 5和7均为新化合物,其结构经1H NMR 和ESI-MS表征。大鼠体内抗血小板聚集活性研究结果表明:3, 5和7均有一定的抗血小板聚集活性,其中7d, 7h和7i的抑制率分别为66.2%, 86.8%和88.3%,活性优于阳性对照药噻氯匹啶。 相似文献
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A series of new 1- and 2-arylmethyl-3,4-dimethylpyrano[2,3-c]pyrazol-6-one derivatives were synthesized and examined for their antiplatelet activities. Some of these compounds showed significant inhibitory activities. Among them, 1-phenylmethyl-3,4-dimethylpyrano[2,3-c]pyrazol-6(1H)-one (4a), 2-(2'-methoxyphenyl)methyl-3,4-dimethylpyrano[2,3-c]pyrazol-6(2H)- one (3e) and 2-(3'-methoxyphenyl)methyl-3,4-dimethylpyrano[2,3-c]pyrazol-6-(2H) - one (3f) were the most effective. These inhibitors acted in a concentration-dependent manner. The antiplatelet effect of compound 3f is due to the inhibition of thromboxane A2 formation and the blockade of thromboxane A2/prostaglandin endoperoxide receptor in washed rabbit platelets. 相似文献