- Synthesis and antiviral activity of N-phenylbenzamide derivatives, a novel class of enterovirus 71 inhibitors
-
A series of novel N-phenylbenzamide derivatives were synthesized and their anti-EV 71 activities were assayed in vitro. Among the compounds tested, 3-amino-N-(4- bromophenyl)-4-methoxybenzamide (1e) was active against the EV 71 strains tested at low micromolar concentrations, with IC50 values ranging from 5.7 ± 0.8-12 ± 1.2 μM, and its cytotoxicity to Vero cells (TC50 = 620 ± 0.0 μM) was far lower than that of pirodavir (TC50 = 31 ± 2.2 μM). Based on these results, compound 1e is a promising lead compound for the development of anti-EV 71 drugs.
- Ji, Xing-Yue,Wang, Hui-Qiang,Hao, Lan-Hu,He, Wei-Ying,Gao, Rong-Mei,Li, Yan-Ping,Li, Yu-Huan,Jiang, Jian-Dong,Li, Zhuo-Rong
-
p. 3630 - 3640
(2013/05/09)
-
- ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
-
The present invention relates to compounds of the formula (I) wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibi
- -
-
Page/Page column 181
(2011/05/11)
-
- Compounds and compositons for treating C1s-mediated diseases and conditions
-
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
- -
-
-
- Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
-
The present invention is directed to compounds of Formula I: wherein X is O, S or NR7and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
- -
-
-
- Cobalt(II)-Catalyzed Reaction of Aldehydes with Acetic Anhydride under an Oxygen Atmosphere: Scope and Mechanism
-
The reaction of aldehydes with acetic anhydride in the presence of catalytic cobalt(II) chloride under an oxygen atmosphere at ambient temperature is dependent upon the reaction medium.Aliphatic aldehydes react in acetonitrile to give 1,2-diones whereas the aromatic aldehydes are acylated to yield the corresponding acylals.On the other hand, carboxylic acids are obtained from aliphatic and aromatic aldehydes by conducting the reaction in dichloroethane or benzene.Cobalt(II) chloride in acetonitrile catalyzes the conversion of aliphatic aldehydes to the correspondinganhydrides in the absence of acetic anhydride whereas aromatic aldehydes remain largely unaffected under these conditions.A preliminary mechanistic study in three different solvents (i.e. acetonitrile, dichloroethane, and DMF) has revealed that in acetonitrile and in the presence of acetic anhydride, aliphatic aldehydes behave differently than aromatic aldehydes.Some trapping experiments using methyl acrylate and stilbene have been conducted to demonstrate the occurence of an acyl cobalt and peroxyacyl cobalt intermediate during these reactions.
- Bhatia, Beena,Punniyamurthy, T.,Iqbal, Javed
-
p. 5518 - 5523
(2007/10/02)
-
- Cobalt (II) catalyzed oxidation of aldehydes to carboxylic acid with molecular oxygen
-
A variety of aromatic and some aliphatic aldehydes are efficiently transformed to the corresponding carboxylic acid in presence of catalytic amount of Cobalt (II) chloride, molecular oxygen and acetic anhydride at room temperature. Phenolic aldehydes undergo acylative oxidation to give the corresponding acylated carboxylic acid.
- Bhatia, Beena,Iqbal, Javed
-
p. 7961 - 7964
(2007/10/02)
-
- Studies on Rhubarb (Rhei Rhizoma). VI. Isolation and Characterization of Stilbenes
-
Nineteen stilbene derivatives (I-XIX), of which five are novel cis-stilbenes, have been obtained from a rhubarb of low quality (commercial name:, Imo-Daio).Based on chemical and spectroscopic evidence, these compounds have been characterized as rhapontigenin (I), rhaponticin (II), rhapontigenin 3'-O-β-D-glucopyranoside (III), rhaponticin 6''-O-gallate (IV), rhaponticin 2''-O-gallate (V), rhaponticin 2''-O-p-coumarate (VI), piceatannol (VII), piceatannol 3-O-β-D-glucopyranoside (VIII), piceatannol 3'-O-β-D-glucopyranoside (IX), piceatannol 3'-O-β-D-xylopyranoside (X), piceatannol 3-O-β-D-(6''-O-galloyl) glucopyranoside (XI), desoxyrhaponticin (XII), desoxyrhaponticin 6''-O-gallate (XIII), 3,4',5-trihydroxystilbene 4'-O-β-D-(6''-O-galloyl) glucopyranoside (XIV), cis-3,3',5-trihydroxy-4'-methoxystilbene 3-O-β-D-glucopyranoside (XV), cis-3,3',5-trihydroxy-4'-methoxystilbene 3-O-β-D-(6''-O-galloyl) glucopyranoside (XVI), cis-3,5-dihydroxy-4'-methoxystilbene 3-O-β-D-glucopyranoside (XVII), cis-3,3',5-trihydroxy-4'-methoxystilbene 3-O-β-D-(2''-O-galloyl) glucopyranoside (XVIII) and cis-3,3',5-trihydroxy-4'-methoxystilbene (XIX).Keywords - rhubarb; Polygonaceae; trans-stilbene; cis-stilbene; gallic acid ester; p-coumaric acid ester; rhaponticin; desoxyrhaponticin; piceatannol; 3,4',5-trihydroxystilbene
- Kashiwada, Yoshiki,Nonaka, Gen-ichiro,Nishioka, Itsuo
-
p. 3501 - 3517
(2007/10/02)
-