81245-24-1Relevant academic research and scientific papers
Compounds with neuroprotective effect, and preparation method and application thereof
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Paragraph 0424-0428, (2021/06/13)
The invention relates to compounds with a neuroprotective effect, and a preparation method and application thereof. Specifically, the compounds disclosed by the invention have a structure as shown in a formula I, and the definitions of all groups and subs
Preparation method and application of 4-hydroxyemodin
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Paragraph 0048; 0050-0051, (2020/04/29)
The invention belongs to the technical field of medicines, and relates to a preparation method and application of 4-hydroxyemodin, in particular to a preparation method of 4-hydroxyemodin and application of 4-hydroxyemodin, optical isomers, pharmaceutical
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-1" PATHWAY AND METHODS OF USE THEREOF
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Paragraph 0237, (2020/03/02)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF
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Page/Page column 93, (2020/03/05)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I" PATHWAY AND METHODS OF USE THEREOF
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Paragraph 0565, (2020/03/01)
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
Synthesis, in-vitro, in-vivo anti-inflammatory activities and molecular docking studies of acyl and salicylic acid hydrazide derivatives
Ali, Gowhar,Ashraf, Zaman,Hussain, Izhar,Khushal, Adil,Mumtaz, Amara,Munir, Abida,Rashid, Umer,Sadiq, Abdul,Saeed Jan, Muhammad,Saeed, Kiran,Ullah Mughal, Ehsan,Ullah, Rahim
, (2020/09/18)
Over the course of time several drugs have been synthesized and are available in market for the treatment of inflammation. However, they were unable to cure effectively and associated with side effects. To effectively deal with such diseases, heterocycles and their derivatives have gained their special position. For this reason 1,3,4-oxadiazole (15–16), 1,2,4-triazole (17–18), Schiff base (19–24) and 3,5-disubstituted pyrazole (25) derivatives were synthesized starting from salicylic acid and acyl acid hydrazides (12–14) as COX-1 and COX-2 inhibitors. In vivo anti-inflammatory activities were also tested by carrageenan-induced mice paw edema against albino mice of any sex. Structures of all the synthesized compounds were confirmed by FT-IR and 1H NMR analysis. Schiff base derivative of 4-amiontirazole (24) with IC50 value of 1.76 ± 0.05 (COX-2) and 117.8 ± 2.59 emerged as potent COX-2 inhibitor. Furthermore, we also performed in-vivo anti-inflammatory investigations by using carrageenan induced paw edema test. From in-vivo anti-inflammatory activities, it was found that after 1 h the maximum percentage inhibition 15.8% was observed by compound 14 which is comparable with that of the standard drug followed by the compound 18 with percentage inhibition of 10.5%. After 3 h, the maximum percentage inhibition was observed by compound 18 with 22.2% and compound 14 with 16.7%. After 5 h the maximum percentage inhibition was observed by compound 18 with 29.4% followed by compound 16 with 23.5%. We further explore the mechanism of the inhibition by using docking simulations. Docking studies revealed that the selective COX-2 inhibitors established interactions with additional COX-2 enzyme pocket residues.
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0665; 0666; 0667; 0668, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
Novel compounds that are inhibitors of YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma
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Paragraph 0459-0461, (2020/02/01)
These compounds are useful as inhibitors of the YAP/TAZ-TEAD interaction.
Synthesis and antibacterial activity of emodin and its derivatives against methicillin-resistant Staphylococcus aureus
Chalothorn, Thidarat,Rukachaisirikul, Vatcharin,Phongpaichit, Souwalak,Pannara, Sakawrat,Tansakul, Chittreeya
supporting information, (2019/08/08)
Synthesis of the antibacterial emodin was improved using Friedel-Crafts acylation as a key step leading to 37% overall yield. In addition, 21 analogues were synthesized by structural modification of the hydroxyl and methyl groups, as well as the aromatic ring of emodin. Antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and cytotoxicity against noncancerous Vero cells were evaluated. A structure-activity relationship (SAR) study indicated that the hydroxyl groups and the methyl group in the emodin skeleton were crucial for anti-MRSA activity. Furthermore, the presence of an iodine atom or ethylamino group on the aromatic ring enhanced the anti-MRSA activity with higher selectivity indices, while derivatives containing bromine, chlorine atoms or quaternary ammonium salt were as active as emodin. The quaternary ammonium group on the aromatic ring also led to non-cytotoxicity against Vero cells.
Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
Deng, Xiangping,Liu, Renbo,Li, Junjian,Li, Zhongli,Liu, Juan,Xiong, Runde,Lei, Xiaoyong,Zheng, Xing,Xie, Zhizhong,Tang, Guotao
, p. 1874 - 1884 (2019/01/28)
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the apoptosis of HCT-116 cells in a concentration-dependent manner, while it had no effect on their cell cycle. The WB analysis suggested that HIF-1α, tubulin, HK-2, and PFK might be the potential pharmacophore targets of compound 10v. Tubulin was a potential drug target for compound 10v, which was explained by analyzing the crystal structure of compound 10v complexed with tubulin. These results indicated that compound 10v might be a promising anti-tumor agent candidate, deserving further optimization and evaluation.
