共查询到20条相似文献,搜索用时 46 毫秒
1.
2.
3.
G A Bennett G B Mullen S D Allen J T Mitchell V St Georgiev 《Arzneimittel-Forschung》1989,39(10):1206-1208
The synthesis and antifungal activity of a series of novel 5-substituted 3-(2-naphthalenyl)-3-(1H-imidazol-1-ylmethyl)-2- methylisoxazolidine derivatives are described. When tested in vitro in solid agar assays, some of the compounds demonstrated moderate to potent activity against Trichophyton rubrum and Candida albicans. 相似文献
4.
S Misztal J Boksa E Chojnacka-Wójcik E Tatarczyńska S Russeva 《Polish journal of pharmacology and pharmacy》1988,40(4):413-421
Five derivatives of 2-(3-aminopropionyl)-1-(3-pyridyl)-1,2,3,4-tetrahydro-beta-carboline (2a-e) were obtained, which yielded, as a result of reduction with LiAlH4, five respective 2-aminopropyl-derivatives (3a-e). Pharmacological studies revealed that phenylpiperazine-derivatives 2d, 2e, 3d and 3e have sedative and analgesic properties. All compounds are devoided of neuroleptic, antidepressant, anxiolytic and antiparkinsonic activity. 相似文献
5.
6.
7.
目的对2-(2-(3-(2-(7-氯-2-喹啉基)乙烯基)苯基-3-氧代丙基)苯基)丙醇的合成工艺进行研究。方法以间氰基苯甲醛和邻甲基苯乙酮分别作为起始原料,经过缩合、格氏反应、羟基保护、羟甲基反应、卤化反应,缩合得到最终目标产物。结果总收率为质量分数47.5%。结论该工艺原料易得,降低了制备成本、简化了反应操作条件、提高了产率,更适合工业化生产。 相似文献
8.
9.
D E McClure J J Baldwin W C Randall T F Lyon K Mensler G F Lundell A W Raab D Gross E A Risley C S Sweet M Williams 《Journal of medicinal chemistry》1983,26(5):649-657
An interest in dual-acting antihypertensive agents, specifically those related to (S)-2-[3-(tert-butylamino)-2-hydroxypropoxy]-3-cyanopyridine (1), led us to probe the contribution of the side-chain amino substituent in this series. The ability of 1 and its various analogues to displace radiolabeled alpha 1 (WB-4101 and prazosin) and beta (dihydroalprenolol) adrenergic receptor ligands was assessed by receptor-binding techniques. Most of the compounds exhibited high beta-adrenoceptor binding affinities, but only the N-aralkylamino-substituted compounds showed high alpha 1-adrenoceptor affinities. Therefore, the vasodilation shown by 1 was not due to an interaction with the alpha 1 adrenoceptor. The aralkylamino analogues of 1 in spontaneously hypertensive rats and anesthetized dogs exhibited antihypertensive activity and alpha 1-adrenoceptor blocking properties. Unlike the preference shown by beta-adrenoceptors for S enantiomers in this oxymethylene class of beta blockers, the chirality at the secondary hydroxy center made only a minor contribution to the affinity for the alpha 1-adrenoceptor and even less of a contribution to the observed antihypertensive effects. This lack of chiral influence at the hydroxy center confirmed what had been previously observed in more limited studies with the isomers of both labetalol and medroxalol. 相似文献
10.
目的 设计合成3-(2-烷氧基-5-甲基苯基)-3-苯基丙胺类化合物,从中筛选有抗尿失禁作用而无口干等不良反应的活性化合物。方法 以肉桂酸和对甲酚为起始原料,经环合、甲基化、酰胺化、还原或再经脱甲基化得目标产物。结果 共合成10个新化合物,经IR,^1H-NMR等确证其结构。 相似文献
11.
对甲苯酚和肉桂酸经脱水环合、水解甲基化制得3-(2-甲氧基-5-甲基苯基)-3-苯丙酸,用硼氧化钠在三氟化硼乙醚复合物作用下以无水THF为溶剂直接还原制得托特罗定中间体3-(2-甲氧基-5-甲基苯基)-3-苯丙醇,总收率89%. 相似文献
12.
Ring-Opened Analogues of Serotonine, II: Synthesis of 3-(2-Aminophenyl)propanamine and 1-(Piperidin-1-yl)-3-(2-aminophenyl)propan-3-one and Their Derivatives The synthesis of the title compounds was achieved by Mannich reaction of suitably substituted acetophenones. The preparation of 3-(2-aminophenyl)propanamine and its derivatives requires complete hydrogenation of the carbonyl group of the Mannich bases. 相似文献
13.
14.
The complete reduction of the carbonyl group of the 5-HT agonist 3-(2-amino-5-hydroxy-phenyl)-3-oxo-propanamine results in a drastic loss of activity: as investigations on the isolated gastric fundus of the rat showed, the affinity to the D receptor of serotonin is reduced by a factor of 100 whereas the relative intrinsic activity also decreases from 0.83 to values less than 0.3. The additional suppression of the phenolic hydroxyl group causes only a relatively unimportant decrease of the affinity while the relative intrinsic activity increases again up to 0.65. These results support the postulate according to which the active conformation of serotonin shows a stretched side chain, as its logical interpretation is only possible under this assumption. Inside the 1-(N-piperidino)-3-(2-amino-phenyl)-3-oxo-propanes the derivative methoxylated at C-5 of the benzene nucleus with a pA2 value of 7.39 proved to be the most effective 5-HT antagonist the mechanism being a purely competitive one. 相似文献
15.
16.
Orlandini E Rapposelli S Nencetti S Giannaccini G Betti L Balsamo A 《Archiv der Pharmazie》2007,340(3):135-139
Some oxime ether-substituted aryloxypropanolamines 3-5, structurally related to the active metabolite 2 of sarpogrelate 1, were synthesized and tested for their affinities at 5-HT2A and 5-HT1A serotoninergic receptors as well as at the alpha1-adrenoceptor. The results show that the compounds possess, at least partially, the ability of the model compounds 1 and 2 to interact with the 5-HT2A-receptors; they have the same selectivity towards 5-HT2A receptors vs alpha1-adrenoceptors. 相似文献
17.
18.
B A Mico J E Swagzdis D A Federowicz K Straub 《Journal of pharmaceutical sciences》1986,75(10):929-933
In the previous report, we reported the results of absorption, protein binding, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone, N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide, and 4-(di-n-propylaminoethyl)-2-(3H)-indolone. Both phenolic compounds, 1 and 2, were subject to more rapid metabolism than the nonphenol 3. In the present study, we investigated the metabolic basis of the differences in the pharmacokinetics of these compounds. In both rats and dogs, the principal urinary metabolite of 1 and 2 was the corresponding glucuronide. In contrast, 3 was first converted to 1 which then was converted to a glucuronide. On the basis of the urinary excretion of 1 and its glucuronide after intravenous administration of 1 and 3, approximately 78% of the dose of 3 in rats and 58% in dogs was converted to 1. The depropyl analogue of 3 was identified as a minor urinary metabolite. 4-(2-Di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone was found in the plasma of rats, dogs, and cynomolgus monkeys treated with 3. The concentration of 1 declined in parallel with that of 3 in dogs and monkeys, indicating that the true half-life of 1 is shorter than or equal to that of 3. On the basis of plasma concentrations of 1 in dogs, the apparent conversion of 3 to 1 was 9%.(ABSTRACT TRUNCATED AT 250 WORDS) 相似文献
19.
Servet Büyüktimkin Sigurd Elz Martin Drger Walter Schunack 《Archiv der Pharmazie》1984,317(9):797-802
Quinazolinones, I: Preparation, Crystal Structure, and Activity of 2-Methyl-3-(4-oxo-3-phenylthiazolidine-2-ylidenamino)-4(3H)-quinazolinone The cyclisation of 1-(3,4-dihydro-2-methyl-4-oxo-3H-quinazoline-3-yl)-3-phenylthiourea (2) with chloroacetic acid leads to 2-methyl-3-(4-oxo-3-phenyl-thiazolidine-2-ylidenamino)-4(3H)-quinazolinone (3) and not to the isomer 4 . The crystal structure of 3 has been determined and refined until R = 0.0715. Compound 3 possesses good hypnotic and anticonvulsant activities. 相似文献
20.
N1-[1-[3-aryl-1-(pyridin-2,3-, and 4-yl)-3-oxo[propyl]-2- pyridinecarboxamidrazone derivatives were synthesized and tested for their in vitro antimycobacterial activity. Some compounds showed interesting activity against a strain of Mycobacterium tuberculosis and a strain of Mycobacterium avium. 相似文献