Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity
CONCLUSION: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized and characterized using 1H NMR and 13C NMR. Moreover, their purity was determined by HPLC. Both compounds A and B exhibited more potent activities against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) than rupestonic acid. Compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Based on these results, more rupestonic acid derivatives will be designed and synthesized in the future for the development of anti-influenza inhibitors.PMID:38623973 | DOI:1...
Source: Current Pharmaceutical Design - April 16, 2024 Category: Drugs & Pharmacology Authors: Jianping Yong Canzhong Lu Source Type: research
Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity
CONCLUSION: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized and characterized using 1H NMR and 13C NMR. Moreover, their purity was determined by HPLC. Both compounds A and B exhibited more potent activities against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) than rupestonic acid. Compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Based on these results, more rupestonic acid derivatives will be designed and synthesized in the future for the development of anti-influenza inhibitors.PMID:38623973 | DOI:1...
Source: Current Pharmaceutical Design - April 16, 2024 Category: Drugs & Pharmacology Authors: Jianping Yong Canzhong Lu Source Type: research
Discovery andsynthesis of novel benzoylhydrazone neuraminidase inhibitors
Bioorg Med Chem Lett. 2024 Apr 10:129743. doi: 10.1016/j.bmcl.2024.129743. Online ahead of print.ABSTRACTNeuraminidase (NA) serves as a promising target for the exploration and development of anti-influenza drugs. In this work, lead compound 5 was discovered through pharmacophore-based virtual screening and molecular dynamics simulation, and 14 new compounds were obtained by modifying the lead compound 5 based on pharmacophore features. The biological activity test shows that 5n (IC50 = 0.13 μM) has a better inhibitory effect on wild-type NA (H5N1), while 5i (IC50 = 0.44 μM) has a prominent inhibitory effect on mutant NA...
Source: Bioorganic and Medicinal Chemistry Letters - April 12, 2024 Category: Chemistry Authors: Shi Kai Fu Li Ping Cheng Source Type: research
Viruses, Vol. 16, Pages 593: Antiviral Chemotherapy in Avian Medicine & mdash;A Review
Viruses, Vol. 16, Pages 593: Antiviral Chemotherapy in Avian Medicine—A Review
Viruses doi: 10.3390/v16040593
Authors:
Ines Szotowska
Aleksandra Ledwoń
This review article describes the current knowledge about the use of antiviral chemotherapeutics in avian species, such as farm poultry and companion birds. Specific therapeutics are described in alphabetical order including classic antiviral drugs, such as acyclovir, abacavir, adefovir, amantadine, didanosine, entecavir, ganciclovir, interferon, lamivudine, penciclovir, famciclovir, oseltamivir, ribavirin, and zidovudine, repurposed drugs, such as iver...
Source: Viruses - April 12, 2024 Category: Virology Authors: Ines Szotowska Aleksandra Ledwo ń Tags: Review Source Type: research
Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone
Eur J Med Chem. 2024 Mar 12;269:116305. doi: 10.1016/j.ejmech.2024.116305. Online ahead of print.ABSTRACTInspired by our earlier findings regarding neuraminidase (NA) inhibitors interacting with 150-cavity or 430-cavity of NA, sixteen novel polyheterocyclic NA inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone were designed and synthesized based on the lead compound ZINC13401480. Of the synthesized compounds, compound N5 targeting 150-cavity exerts the best inhibitory activity against the wild-type H5N1 NA, with IC50 value of 0.14 μM, which is superior to oseltamivir carboxylate (OSC) (IC50 = 0.31 μM). Comp...
Source: European Journal of Medicinal Chemistry - March 22, 2024 Category: Chemistry Authors: Lin Lin Shang Zhi Jian Zhong Li Ping Cheng Source Type: research
Efficacy of Pharmacotherapy for Seasonal Influenza in Young and Middle-aged Adults: A Systematic Review and Network Meta-analysis
Conclusion Several pharmaceutical treatments were able to reduce the recovery time for fever and symptom alleviation and resumption of usual activities in young and middle-aged adults with seasonal influenza without increasing the risk of complications.PMID:38494721 | DOI:10.2169/internalmedicine.2100-23 (Source: Internal Medicine)
Source: Internal Medicine - March 18, 2024 Category: Internal Medicine Authors: Nao Hanaki Ryoto Sakaniwa Takuhiro Moromizato Jun Miyata Keiko Ishimura Midori Noguchi Hiroyasu Iso Source Type: research
Lianhua Qingwen exerts anti-liver cancer effects and synergistic efficacy with sorafenib through PI3K/AKT pathway: Integrating network pharmacology, molecular docking, and experimental validation
This study broadens the potential application of LHQW and provides insights for liver cancer treatment.PMID:38493972 | DOI:10.1016/j.gene.2024.148383 (Source: Gene)
Source: Gene - March 17, 2024 Category: Genetics & Stem Cells Authors: Jinrui Wei Xuqi Zhao Fuli Long Kunpeng Tian Lichuan Wu Source Type: research
Lianhua Qingwen exerts anti-liver cancer effects and synergistic efficacy with sorafenib through PI3K/AKT pathway: Integrating network pharmacology, molecular docking, and experimental validation
This study broadens the potential application of LHQW and provides insights for liver cancer treatment.PMID:38493972 | DOI:10.1016/j.gene.2024.148383 (Source: Gene)
Source: Gene - March 17, 2024 Category: Genetics & Stem Cells Authors: Jinrui Wei Xuqi Zhao Fuli Long Kunpeng Tian Lichuan Wu Source Type: research
Household Influenza Transmission and Healthcare Resource Utilization Among Patients Treated with Baloxavir vs Oseltamivir: A United States Outpatient Prospective Survey
ConclusionsThe findings from this real-world study suggest that antiviral treatment of influenza with baloxavir may decrease household transmission and reduce healthcare resource utilization compared with oseltamivir. (Source: Infectious Diseases and Therapy)
Source: Infectious Diseases and Therapy - March 14, 2024 Category: Infectious Diseases Source Type: research
Oseltamivir enhances 5-FU sensitivity in esophageal squamous carcinoma with high SPNS1
Biomed Pharmacother. 2024 Mar 8;173:116367. doi: 10.1016/j.biopha.2024.116367. Online ahead of print.ABSTRACTSphingolipid transporter 1 (SPNS1) is a significant differentially expressed gene (DEGs) in esophageal squamous cell carcinoma (ESCC). According to 3 pairs clinic cohorts, transcriptomic (155 pairs of ESCC samples and GSE53624, and proteomic data from PXD021701 including 124 ESCC samples) we found that SPNS1 was significantly higher in ESCC tissues compared to adjacent normal esophagus tissues. ESCC patients with high SPNS1 had a significantly poorer clinical prognosis than those with low SPNS1. Knockdown of SPNS1 s...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - March 9, 2024 Category: Drugs & Pharmacology Authors: Xin Yang Ye Jiao Yingying Zhang Meng Sun Yingzhen Gao Yan Zhou Heng Xiao Jing Ren Zhinan Zhou Yuanfang Zhai Bin Song Ling Zhang Pengzhou Kong Source Type: research
