- Substituted benzoyl piperazine compound and application thereof in preparation of anti-chikungunya virus drug
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The invention discloses an application of a substituted benzoyl piperazine compound in preparation of an anti-chikungunya virus drug. The substituted benzoyl piperazine compound has a structural general formula shown in the description, wherein R1, R2, R3
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Paragraph 0056-0059
(2021/02/10)
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- Substituted benzoyl piperazine compound and application thereof
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The invention discloses a substituted benzoyl piperazine compound or a medicinal salt thereof. The substituted benzoyl piperazine compound has the following structural general formula, wherein definitions of substituent groups are shown in the specificati
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Paragraph 0054-0055; 0057
(2021/03/03)
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- Synthesis and biological evaluation of cinnamido linked pyrrolo[2,1-c][1,4]benzodiazepines as antimitotic agents
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A series of new cinnamido-pyrrolo[2,1-c][1,4]benzodiazepine conjugates (4a-d and 5a-d) and their dimers (6a-d) have been designed, synthesized and evaluated for their biological activity. The anticancer screening of compound 4a by the NCI exhibited signif
- Kamal, Ahmed,Balakishan,Ramakrishna,Basha Shaik,Sreekanth,Balakrishna,Rajender,Dastagiri,Kalivendi, Shasi V.
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experimental part
p. 3870 - 3884
(2010/09/14)
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- Selective reduction of secondary amides to amines in the presence of tertiary amides
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Secondary amides activated with a Cbz group can be reduced to their corresponding hemiaminals using lithium borohydride. Hydrogenation then removes the Cbz and hydroxyl groups to produce the related amine. Tertiary amides are not affected.
- Lee, Byung H.,Clothier, Michael F.
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p. 643 - 644
(2007/10/03)
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- (Pyridylcyanomethyl)piperazines as orally active PAF antagonists
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A series of (pyridylcyanomethyl)piperazines was prepared and evaluated for PAF-antagonist activity. Compounds were tested in vitro in a PAF-induced platelet aggregation assay and in vivo in a PAF-induced hypotension test in normotensive rats. Oral activity was ascertained through a PAF-induced mortality test in mice. The main structure-activity trends of the series were established. Activity was mainly found in four skeletons: 1-acyl-4-(3- pyridylcyanomethyl)-piperazine, 1-acyl-4-(4-pyridylcyanomethyl)piperazine, 1- acyl-4-(3-pyridylcyanomethyl)piperidine, and 1-acyl-4-cyano-4-(3- pyridylamino)piperidine. The acyl substituents, diphenylacetyl and 3,3- diphenylpropionyl, provided the most active compounds, and the introduction of an amine or hydroxy group in the 3,3-diphenylpropionyl substituent led to further improvement in oral activity. As a result, three of the most active compounds (100, 114, and 115) have been selected for further pharmacological development.
- Carceller,Almansa,Merlos,Giral,Bartroli,Garcia-Rafanell,Forn
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p. 4118 - 4134
(2007/10/02)
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- Synthesis and CNS-depressant profile of 3,4,5-trimethoxybenzoyl analogues
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A series of 3,4,5-trimethoxybenzoyl analogues with varying electronic and stereochemical characteristics has been synthesized. Many of these compounds (4, 5, 9, 12, 15) showed appreciable potentiation of pentobarbitone-induced hypnosis. Several analogues (1, 5, 6, 11, 12, 15) exhibited marked reduction of spontaneous motor activity (SMA).
- Kar
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p. 313 - 315
(2007/10/02)
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