Article
Integrative & Complementary Medicine
Rongbo Luo, Chaoxiang Lv, Tiecheng Wang, Xiuwen Deng, Mingwei Sima, Jin Guo, Jing Qi, Weiyang Sun, Beilei Shen, Yuanguo Li, Donghui Yue, Yuwei Gao
Summary: Isoquercitrin shows significant anti-IAV and anti-IBV activity in vitro and in vivo, reducing virus replication and mortality in mouse lethal infection models. It also mitigates lung and multiple organ damage and blocks hyperproduction of cytokines induced by virus infection through inactivating NF-kappa B signaling. Intramuscular injection is a better drug delivery method for isoquercitrin.
Review
Biochemistry & Molecular Biology
Chuyuan Zhang, Xinjie Meng, Hanjun Zhao
Summary: Virus-cell fusion plays a crucial role in viral infection and understanding this process is important for developing antiviral drugs. This review focuses on the fusion of influenza virus and SARS-CoV-2 with host cells, comparing their differences and discussing the development of drugs to prevent respiratory virus infections.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Mei Wang, Jian Zhang, Yutong Dou, Minghui Liang, Yong Xie, Peng Xue, Linyue Liu, Chuanju Li, Yuanze Wang, Feiyan Tao, Xiaohui Zhang, Huili Hu, Kairui Feng, Lei Zhang, Zhuanchang Wu, Yunfu Chen, Peng Zhan, Haiyong Jia
Summary: In this study, benzamide derivatives were designed and synthesized, and compound 17i showed significantly increased anti-HBV activity and inhibited the assembly of HBV capsid protein. It also exhibited good metabolic stability and oral bioavailability, as well as inhibitory effects on HBV replication.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Virology
Pinar Yazici ozkaya, Ese Eda Turanli, Hamdi Metin, Ayca Aydin Uysal, Candan cicek, Bulent Karapinar
Summary: This study aimed to identify the clinical features and mortality associated with severe influenza A and B virus infections in children admitted to the pediatric intensive care unit (PICU) between 2012 and 2019. The study found that although the proportion of influenza A cases admitted to the PICU was higher, the percentage of cases requiring PICU admission was nearly two times higher in influenza B cases. Additionally, there was no statistically significant difference in disease severity and complications in patients with influenza A and influenza B.
JOURNAL OF MEDICAL VIROLOGY
(2022)
Article
Chemistry, Organic
Liselle Atkin, Angus Robertson, Jonathan M. White, Mark A. Rizzacasa
Summary: The total synthesis of viridiofungins A and B via beta-lactone 3 in 13 steps is described, with key steps including an HF-mediated rearrangement, olefin cross metathesis while suppressing isomerization, and a novel beta-lactone ring opening. Deprotection yielded either viridiofungin A or B in high yield.
Article
Chemistry, Physical
Emmanuelle Bignon, Elise Dumont, Antonio Monari
Summary: In this study, we investigated the dynamic behavior of the precursor of tick-borne encephalitis virus membrane fusion protein E at neutral and acidic pH. We found different stabilizations of the E dimer and identified the role of the small fusion-assisting protomer (pr). Understanding the precise regulation of viral maturation at the atomic level is crucial for developing effective strategies against emerging viral threats.
JOURNAL OF PHYSICAL CHEMISTRY LETTERS
(2023)
Article
Microbiology
Nicolas Malausse, Sylvie van der Werf, Nadia Naffakh, Sandie Munier
Summary: Co-infections between influenza A virus (IAV) and influenza B virus (IBV) were studied by infecting A549 cells with recombinant IAV-GFP and IBV-mCherry. Surprisingly, IBV replication was enhanced when co-infected with IAV, particularly when IAV was added 1 hour before IBV. This enhancing effect was dependent on transcription/replication of the IAV genome.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Chemistry, Medicinal
Marta De Angelis, Barbara De Filippis, Marwa Balaha, Letizia Giampietro, Mariya Timotey Miteva, Giovanna De Chiara, Anna Teresa Palamara, Lucia Nencioni, Adriano Mollica
Summary: This study optimized the structure of resveratrol (RSV) by synthesizing new RSV derivatives and evaluated their potential anti-influenza virus activity. The results showed that nitro-containing compounds strongly inhibited viral replication. Furthermore, these derivatives exerted their antiviral effects by interfering with cellular mechanisms such as viral nuclear-cytoplasmic traffic.
Article
Chemistry, Organic
Tobias Babl, Oliver Reiser
Summary: The first enantioselective synthesis of (S)-meptazinol in 14 steps from a commercially available compound and the formal synthesis of two anti-Alzheimer's agents are reported. A novel ring expansion reaction provides an effective entry to 3,3-disubstituted azepanes that represent the core for a variety of approved drugs.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Jiwei Zhang, Chuanfeng Liu, Ruifang Jia, Xujie Zhang, Jian Zhang, Chiara Bertagnin, Anna Bonomini, Laura Guizzo, Yuanmin Jiang, Huinan Jia, Shuzhen Jia, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan, Xinyong Liu
Summary: Introducing structurally diverse benzyl side chains at the C5-NH2 position of oseltamivir improves its binding affinity with neuraminidase and anti-influenza activity. We designed and synthesized novel oseltamivir derivatives with different N-heterocycle substituents that induce opening of the 150-loop of group-2 neuraminidases. Compound 6k showed broad-spectrum activity against wild-type neuraminidases and enhanced activity against H3N2 compared to oseltamivir carboxylate and zanamivir.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Sook Kwan Brown, Yeu-Yang Tseng, Ammar Aziz, Mariana Baz, Ian G. Barr
Summary: This study tested 3425 influenza B viruses collected from the Asia-Pacific region against four registered neuraminidase inhibitors (NAIs). It identified 45 influenza B viruses with reduced susceptibility to one or more NAIs, including some with newly identified neuraminidase mutations. The study highlights the potential impact of these mutations on the clinical effectiveness of NAIs in treating influenza B infections in humans.
ANTIVIRAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Remigiusz Worch, Anita Dudek, Paulina Borkowska, Piotr Setny
Summary: The fusion of viral and host cell membranes is a critical step in the life cycle of enveloped viruses. Studies have shown that subunit 2 of hemagglutinin glycoprotein mediates fusion, and fusion peptides possess fusogenic activity, but their mechanism of action remains unclear.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Organic
Liang Shao, Fan Yang, Weijia Li, Fei Yu
Summary: Inhibitors targeting the entry stage of influenza viruses are a key focus in anti-influenza drug development. A series of oleanolic acid C3 glycoconjugates were designed and synthesized, with compound 12a demonstrating the strongest anti-influenza activity. The compound may target viral envelope hemagglutinin (HA) to inhibit virus attachment to host cells, without showing cytotoxic effects on MDCK cells.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Huan He, Fanglin Xue, Zhao Hu, Peng Li, Qian Xiao, Maojie Zhang, Fei Xue, Dan Zhang, Hao Song, Xiao-Yu Liu, Zhibing Zheng, Song Li, Wu Zhong, Yong Qin
Summary: Morphine and its related alkaloids are commonly used natural medicines. However, the current industrial manufacturing process of these compounds causes environmental issues. In this study, researchers developed an efficient total synthesis method for opioids such as codeine, oxycodone, naloxone, and naltrexone. The key step in this synthesis is the Pd-catalyzed dearomatization arene coupling reaction using an inexpensive and stable phosphonium ligand.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Pharmacology & Pharmacy
Ruikun Du, Han Cheng, Qinghua Cui, Norton P. Peet, Irina N. Gaisina, Lijun Rong
Summary: A novel antiviral agent, CBS1194, specific to group 2 IAVs was identified through high-throughput screening, showing potential as a lead compound for further development.
ANTIVIRAL RESEARCH
(2021)
Article
Chemistry, Medicinal
Girish C. Sati, Vikram A. Sarpe, Takayuki Furukawa, Sujit Mondal, Matilde Mantovani, Sven N. Hobbie, Andrea Vasella, Erik C. Bottger, David Crich
ACS INFECTIOUS DISEASES
(2019)
Article
Biochemistry & Molecular Biology
Ruchika Dadhich, Manjari Mishra, Shangbo Ning, Santanu Jana, Vikram A. Sarpe, Jaladhar Mahato, Mojie Duan, Suvarn S. Kulkarni, Shobhna Kapoor
ACS CHEMICAL BIOLOGY
(2020)
Article
Chemistry, Multidisciplinary
Jonathan C. K. Quirke, Parasuraman Rajasekaran, Vikram Sarpe, Amr Sonousi, Ivan Osinnii, Marina Gysin, Klara Haldimann, Qiao-Jun Fang, Dimitri Shcherbakov, Sven N. Hobbie, Su-Hua Sha, Jochen Schacht, Andrea Vasella, Erik C. Boettger, David Crich
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2020)
Article
Biochemistry & Molecular Biology
Riku Ogasahara, Shuay Abdullayev, Vikram A. Sarpe, Appi Reddy Mandhapati, David Crich
CARBOHYDRATE RESEARCH
(2020)
Article
Chemistry, Organic
Santanu Jana, Vikram A. Sarpe, Suvarn S. Kulkarni
Summary: In this study, a total synthesis strategy for the structurally unique fungal glycolipid fusaroside was reported, with a proposed revision in its structure, particularly regarding the position of olefins in the lipid chain.
Article
Chemistry, Medicinal
Dimitrijs Lubriks, Rimants Zogota, Vikram A. Sarpe, Takahiko Matsushita, Girish C. Sati, Klara Haldimann, Marina Gysin, Erik C. Boettger, Andrea Vasella, Edgars Suna, Sven N. Hobbie, David Crich
Summary: Propylamycin is a next generation amino-glycoside antibiotic that has increased antibacterial potency compared to its parent compound and reduced ototoxicity. However, it is inactivated by a specific enzyme, leading researchers to study various derivatives in order to overcome this issue.
ACS INFECTIOUS DISEASES
(2021)
Article
Biochemistry & Molecular Biology
Santanu Jana, David Crich
Summary: This study describes a novel oxidative fragmentation reaction of methyl ester in DMF with sodium nitrite, yielding a new compound with high yield. Furthermore, another new compound is obtained through the reaction of the same ester with sodium carbonate. Reduction and acetylation of the lactone result in a peracetylated aminodeoxyheptitol with a zig zag conformation of its carbon backbone.
CARBOHYDRATE RESEARCH
(2022)
Article
Chemistry, Organic
Santanu Jana, David Crich
Summary: In this study, we report a straightforward synthesis of Gentamicin C1a and the minor isomer C2b from readily available sisomicin. These compounds exhibit favorable properties in terms of antibacterial activity and toxicity compared to the commercial mixture.
Article
Chemistry, Organic
Sudhakar S. Nalpe, Santanu Jana, Suvarn S. Kulkarni
Summary: We recently synthesized and confirmed the proposed revised structure of fungal glycolipid fusaroside. The total synthesis involved fatty acid construction using Julia-Kocienski olefination, coupling with trehalose, and late-stage gem-dimethylation.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Sudhakar S. Nalpe, Santanu Jana, Suvarn S. Kulkarni
Summary: This article introduces a simple method for synthesizing a lipooligosaccharide analogue from Mycobacterium linda isolated from Crohn's disease. The total synthesis of the tetrasaccharide was achieved through a [2+2] glycosylation reaction, with the key features being the selective functionalization of a trehalose core via highly regioselective acylations and regioselective glycosylations. The synthesis was completed in a longest linear sequence of 14 steps with an overall yield of 14.2%.
Article
Chemistry, Medicinal
Santanu Jana, Parasuraman Rajasekaran, Klara Haldimann, Andrea Vasella, Erik C. Bottger, Sven N. Hobbie, David Crich
Summary: In this study, we synthesized gentamicins C1, C2, and C2a with methyl substitution at the 6'-position, providing an alternative method for accessing these compounds compared to previous chromatographic methods. We also explored the antiribosomal activity of the synthetic gentamicin congeners against bacterial ribosomes and different types of ribosomes, establishing structure-activity relationships with the substitution pattern around ring I, antibacterial resistance, and cochlear toxicity data from literature.
ACS INFECTIOUS DISEASES
(2023)
Review
Chemistry, Organic
Santanu Jana, Suvarn S. Kulkarni
ORGANIC & BIOMOLECULAR CHEMISTRY
(2020)
Meeting Abstract
Chemistry, Multidisciplinary
Santanu Jana, Vikram Sarpe, Suvarn Kulkarni
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2019)
