- Ecotoxic effects of loratadine and its metabolic and light-induced derivatives
-
Loratadine and desloratadine are second-generation antihistaminic drugs. Because of human administration, they are continuously released via excreta into wastewater treatment plants and occur in surface waters as residues and transformation products (TPs). Loratadine and desloratadine residues have been found at very low concentrations (ng/L) in the aquatic environment but their toxic effects are still not well known. Both drugs are light-sensitive even under environmentally simulated conditions and some of the photoproducts have been isolated and characterized. The aim of the present study was to investigate the acute and chronic ecotoxicity of loratadine, desloratadine and their light-induced transformation products in organisms of the aquatic trophic chain. Bioassays were performed in the alga Pseudokirchneriella subcapitata, the rotifer Brachionus calyciflorus and in two crustaceans, Thamnocephalus platyurus and Ceriodaphnia dubia. Loratadine exerted its acute and chronic toxicity especially on Ceriodaphnia dubia (LC50: 600 μg/L, EC50: 28.14 μg/L) while desloratadine showed similar acute toxicity among the organisms tested and it was the most chronically effective compound in Ceriodaphnia dubia and Pseudokirchneriella subcapitata. Generally, transformation products were less active in both acute and chronic assays.
- Iesce, Maria Rosaria,Lavorgna, Margherita,Russo, Chiara,Piscitelli, Concetta,Passananti, Monica,Temussi, Fabio,DellaGreca, Marina,Cermola, Flavio,Isidori, Marina
-
p. 664 - 672
(2019/01/03)
-
- Synthesis method of bacterial infection resistant medicine intermediate
-
The invention belongs to the technical field of chemical medicine intermediate synthesis, and particularly relates to a synthesis method of a bacterial infection resistant medicine intermediate. Liquid ammonia and acrylic ester are used as raw materials for preparing a diester type secondary amine compound 1; then, through cyclization, piperidone is prepared; then, scientific reaction catalysts, temperature and time are used; substitution reaction of secondary amine and iso-propyl iodide is used; the target product is synthesized through six-step reaction; the yield of the whole route reachesup to 35 percent.
- -
-
Paragraph 0028
(2018/07/30)
-
- Development of a Robust Process for the Preparation of High-Quality 4-Methylenepiperidine Hydrochloride
-
An efficient route for the preparation of 4-methylenepiperidine hydrochloride 1 was designed, and then a process feasible for large-scale production was developed with a total yield of 83.5% at a purity of 99.9%.
- Zhu, Fuqiang,Aisa, Haji A.,Zhang, Jian,Hu, Tianwen,Sun, Changliang,He, Yang,Xie, Yuanchao,Shen, Jingshan
-
-
- ANTI-BACTERIAL COMPOUNDS
-
A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.
- -
-
Page/Page column 116; 118
(2017/06/28)
-
- Penfluridol preparation method
-
The invention discloses a penfluridol preparation method. The penfluridol preparation method includes the following steps of 1), subjecting succinic anhydride and fluorobenzene to Friedel-Crafts reaction prior to acid decomposition, and collecting a compound from the formula 2) as is shown in the description; 2), putting the compound in a solvent to collect a compound in formula 3) as is shown in the description in a solvent reduced through a reducing agent; 3), putting the compound into the fluorobenzene to perform the Friedel-Crafts reaction to collect a compound in the formula 4) as is shown in the description; subjecting the compound and ethyl chloroformate to action to generate a compound in formula 5) as is shown in the description; 5), subjecting the compound and a compound shown in formula (XVII) to reaction prior to hydrolyzation to collect a compound in formula 6) as is shown in the description; 6), performing reduction with the reducing agent prior to hydrolyzing a reduction product and then collecting penfluridol (I). The penfluridol preparation method is high in yield, low in cost, moderate in reaction condition, short in circuit, proper for industrial production, low in three wastes, easy to treat and suitable for industrial production.
- -
-
Paragraph 0141; 0142; 0143
(2017/02/24)
-
- HETEROARYL COMPOUNDS AS 5-HT4 RECEPTOR LIGANDS
-
The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
- -
-
Paragraph 0195-0198
(2014/07/08)
-
- Novel Carboline Derivatives as Potent Antifungal Lead Compounds: Design, Synthesis, and Biological Evaluation
-
A series of novel antifungal carboline derivatives was designed and synthesized, which showed broad-spectrum antifungal activity. Particularly, compound C38 showed comparable in vitro antifungal activity to fluconazole without toxicity to human embryonic lung cells. It also exhibited good fungicidal activity against both fluconazole-sensitive and -resistant Candida albicans cells and had potent inhibition activity against Candida albicans biofilm formation and hyphal growth. Moreover, C38 showed good synergistic antifungal activity in combination with fluconazole (FLC) against FLC-resistant Candida species. Preliminary mechanism studies revealed that C38 might act by inhibiting the synthesis of fungal cell wall.
- Wang, Shengzheng,Wang, Yan,Liu, Wei,Liu, Na,Zhang, Yongqiang,Dong, Guoqiang,Liu, Yang,Li, Zhengang,He, Xiaomeng,Miao, Zhenyuan,Yao, Jianzhong,Li, Jian,Zhang, Wannian,Sheng, Chunquan
-
p. 506 - 511
(2014/06/09)
-
- HETEROARYL COMPOUNDS AS 5-HT4 RECEPTOR LIGANDS
-
The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
- -
-
Page/Page column 23
(2013/04/10)
-
- Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties
-
This Letter describes the first account of the synthesis and SAR, developed through an iterative analogue library approach, of analogues of the highly selective M1 allosteric agonist TBPB. With slight structural changes, mAChR selectivity was maintained, but the degree of partial M1 agonism varied considerably.
- Bridges, Thomas M.,Brady, Ashley E.,Phillip Kennedy,Nathan Daniels,Miller, Nicole R.,Kim, Kwango,Breininger, Micah L.,Gentry, Patrick R.,Brogan, John T.,Jones, Carrie K.,Jeffrey Conn,Lindsley, Craig W.
-
experimental part
p. 5439 - 5442
(2009/06/02)
-
- Aryl sulfonamide and sulfonyl compounds as modulators of PPAR and methods of treating metabolic disorders
-
Aryl sulfonamide and sulfonyl compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
- -
-
Page/Page column 59
(2010/02/14)
-
- Synthesis of bicyclic aza-enones via a lewis acid catalysed Michael-type addition with silyl enol ethers bearing a nitrogen atom
-
Silyl enol ethers bearing a nitrogen atom protected by an electron-withdrawing group give in high yield a Micheal-type addition with hemiacetal vinylog or a mixture of methyl vinyl ketone and an alcohol in the presence of boron trifluoride etherate as a catalyst. The aza-1,5-diketones so prepared can be cyclised leading to aza-enones precursors of some biologycally active structures.
- Duhamel, Pierre,Deyine, Abdallah,Poirier, Jean-Marie
-
p. 3863 - 3866
(2007/10/02)
-
- THE HOFFMAN-LIKE FRAGMENTATION INDUCED BY N-ACYLATION OF 1-METHYL-1-AZA-4-CYCLANONES AND ITS USE IN THE SYNTHESIS OF 2-AZA-HYDRINDANONES AND 2-AZA-DECALONES
-
The N-methyl-piperidone 4a was fragmented to the vinylketonic acrylamide 9a by successive treatment with acryloyl chloride and Huenig's base.The 2-azahydrindandione 13a resulted from the cyclization of 9a in the form of its enol dimethylterbutyl ether.N-methyl-azepinone 4b was transformed in a similar way to the two epimeric 2-azadecalindiones 13b + 14b in four steps only.
- Levy, Jean,Laronze, Jean-Yves,Sapi, Janos
-
p. 3303 - 3306
(2007/10/02)
-
