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Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00555D, Research Article
Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu
The continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants.
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Advances in antibacterial agents for Mycobacterium fortuitum

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00508B, Review Article
Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli
This review presents the recent findings on antibacterial agents against Mycobacterium fortuitum and reveals the most promising and effective chemical frameworks to inspire the development of new drugs.
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Design, synthesis, and biological evaluation of pyrazole–ciprofloxacin hybrids as antibacterial and antibiofilm agents against Staphylococcus aureus

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00623B, Research Article
Ojaswitha Ommi, Priyanka Sudhir Dhopat, Shashikanta Sau, Madhu Rekha Estharla, Srinivas Nanduri, Nitin Pal Kalia, Venkata Madhavi Yaddanapudi
A series of pyrazole–ciprofloxacin hybrids were designed, synthesized, and tested for antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Mycobacterium tuberculosis, aiming to combat antibiotic resistance.
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Novel quinoxaline-derived derivatives: design, synthesis, bioactive evaluation, SARs and preliminary antibacterial mechanism

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00670D, Research Article
Yuting Liu, Pengju Yang, Yunyun Zhou, Zhiwen Zhou
In the current study, we have designed and prepared a series of quinoxaline-based compounds, which were derived from o-phenylenediamine. Among which, compounds 5m-p displayed good to moderate antibacterial activity with...
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Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00373J, Research Article
YongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian Zhang
The mitotic kinase Aurora A, a pivotal regulator of cell cycle, is overexpressed in various cancers and has emerged as one of the most promising targets for anticancer drug discovery....
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Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00663A, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Václav Pflégr, Klára Konečná, Jiřina Stolaříková, Jan Ősterreicher, Ondřej Janďourek, Martin Krátký
Linking pyridine-4-carbohydrazide to other antimicrobial agents via oxocarboxylic acids significantly enhances efficacy against mycobacteria with promising selectivity and safety profiles.
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Synthesis of cationic N-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of N-acylation's role in membrane-disrupting activity

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00626G, Research Article
Aleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan Veerappan
Lipidation modulates the Gram-selective antibacterial activity of QPyNATh.
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meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article
Open Access
Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza Gaina
New meso-substituted AB3-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.
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Generation and capture of naphthoquinonynes: a new frontier in the development of trypanocidal quinones via aryne chemistry

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00558A, Research Article
Laura P. R. Figueroa, Renato L. de Carvalho, Renata G. Almeida, Esther R. S. Paz, Emilay B. T. Diogo, Maria H. Araujo, Warley S. Borges, Victor F. S. Ramos, Rubem F. S. Menna-Barreto, James M. Wood, John F. Bower, Eufrânio N. da Silva Júnior
This article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.
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3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00597J, Research Article
Albert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken Witt
Somatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...
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SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00722K, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice Mangiatordi
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...
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Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00724G, Research Article
Zhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei Mao
A series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.
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Adjuvant strategies to tackle mcr-mediated polymyxin resistance

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00654B, Review Article
Madison R. Nuske, Junlang Zhong, Renjie Huang, Vijayalekshmi Sarojini, Jack L. Y. Chen, Christopher J. Squire, Mark A. T. Blaskovich, Ivanhoe K. H. Leung
The emergence of the mobile colistin resistance (mcr) gene is a significant threat contributing to the worldwide antibiotic resistance crisis. This review discusses adjuvant strategies to restore polymyxin sensitivity in these resistant bacteria.
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U.S. Presidential polls: Thulasendrapuram residents pray for Kamala Harris ‘victory




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Data crucial for building climate resilience, says ISRO scientist




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Tiruchi Corporation embarks on special drive at night to capture and sterilise street dogs

About 125 stray dogs have been caught and sterilised at Tiruchi animal birth control centres in the last 10 days after the Corporation launched the special drive




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EPS’s dream of AIADMK staging a comeback in 2026 election will not materialise: Law Minister Regupathy




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Students and agriculture officials grapple with logistical, technical issues during digital crop survey




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Association holds protest against delay in Anna University’s staff absorption, promotions




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AIADMK ready to join hands with like-minded parties to defeat DMK: Palaniswami




ia

554: Jamstack Thoughts with Brian Rinaldi

Brian Rinaldi joins us to talk about the state of Jamstack in 2023, acronym confusion, SPA confusion, developing common tools of understanding, why Netlify bought Gatsby, and the state of developer conferences.




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559: Fidget Apps, Coding with AI, Dialog Element Navs, Getting Rid of CSS

Is there still any value in specializing in front-of-the-frontend dev? Would you ever use the dialog element for a mobile navigation? Why did CodePen decide to use Go for its GraphQL server?




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581: DevRel, Musical Mics, Social Sharing, and 100 Years of WordPress

Dave calls a quick Luro branding meeting, some thoughts on DevRel, Chris tries to figure out musical instrument mics, follow up on WordPress from a previous episode, Chris' journey through the social graph options, 100 year hosting with WordPress, and the introduction of a new segment: Happy Project Share Time.




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591: Cascade Layers, CSS Functions, and more CSS with Miriam Suzanne

Miriam Suzanne stops by to talk about CSS updates and news on container queries, rolling out cascade layers, !important things to remember, custom properties, exit animations, CSS functions, state queries, and more.




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595: MedTalk Show, Plagiarism and Code Grifting, and How We’re Testing Code

Blood pressure, stress, and COVID highlight the MedTalk Show portion of this episode, a new "Did You Know" segment about dev tools in Chrome, 4 hour video on plagiarism and code grifters, typography, breaking out of CSS Grid, the oldest things Chris and Dave worked on, and what the testing process is like at Luro or CodePen.




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634: Fabian Kägy on WordPress, Blocks, and Enterprise Dev

Fabian Kägy helps us understand the modern WordPress development process, Gutenberg vs Block editor vs full site editing, building with blocks or pages, what's coming in the Twenty Twenty-Five Theme, and whether the theme authoring process has been made too difficult in 2024?




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637: Approachable Open Source with Brian Muenzenmeyer

Brian Muenzenmeyer joins the show to talk about his book, Approachable Open Source, ways we can make open source easier to get in, important conversations around funding and supporting open source, and whether money helps maintainers deal with burnout or not?




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Are freeways viable?

Barring very few functionally useful ones, many elevated concrete structures with suboptimal utility have ripped the city apart, defiled and marred it.




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It’s all in the material

Materials have a major say in construction, as their manufacture has to be environment-friendly, making them energy-efficient, says green homes builder Chandrashekar Hariharan. By Ranjani Govind




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Green power, officially

The cumulative effects of changing the way government builds can have a lasting impact on the country’s carbon footprint




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F1: Piastri on pole as McLaren in front

McLaren are leading the constructor's championship but are only 29 points ahead of Ferrari, with Leclerc an obvious threat and team mate Carlos Sainz qualifying fifth and Mercedes' George Russell sixth.




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Could Maini be India's next F1 driver?

India could finally have a driver on the F1 grid after 13 long years.




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A sporty knock from India Inc

A growing crop of corporates are making serious investments in sports and beginning to reap the rewards, too




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Unlocking renewable energy from industrial waste: Biogas production from spent wash

It is a sustainable solution for industrial waste management and renewable energy generation




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From agri waste to industrial raw material

altM is developing alternatives to mined materials and petrochemicals 




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As India’s installed solar capacity crosses 90GW, a look at the journey 

Sun-sational growth: In September, India’s installed solar power capacity reached 90,762 MW. Given the current rate of monthly capacity additions, there is little doubt that installed capacity will exceed 100 GW in 2024-25.




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Investing in companies with ‘indicorn’ potential

Titan Capital backs seed-stage companies with potential to reach ₹100 crore revenue within five years




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Diamonds are a UV photodetector’s best friend

How lab-grown rocks from Surat are set to power the development of high-performance electronics



  • Science and Technology

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Catalysing Indian IP creation 

How policy support and monetisation can rev up India’s innovation ecosystem



  • Science and Technology

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‘Our goal is beauty for each,’ says L’Oréal India chief

Aseem Kaushik, who leads the global beauty giant in India, says tech is playing a big part in its personalisation journey




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How Jio is powering Reliance’s media, entertainment biz

Despite a late entry into telecom, digital services, and media, Reliance has raced to the top




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India seeks $70 million from Climate Investment Funds

India looks to accelerate proposed ‘renewable energy integration programme’




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Toxic air chokes urban India 

Residents grapple with respiratory, cardiac, and other ailments as the air thickens




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Why more NRIs are buying health insurance in India

The number of NRIs buying health insurance from India has increased steadily over the past three years




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Corporates look to tread the India Way  

Business leaders are realising that longevity may be a better marker for growth than shareholder value maximisation




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Nvidia: The lynchpin of the AI revolution

The meteoric rise of the Santa Clara-headquartered chipmaker is powered by bold innovation




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IAF Mig-29 fighter crashes near Agra, pilot ejects to safety

An enquiry has been ordered by the IAF, to ascertain the cause of the accident




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Jamiat cautions NDA partners, says ‘crutches’ cannot escape responsibility for Waqf Bill

The Jamiat Ulama-i-Hind urged NDA partners TDP and JD(U) to heed Muslim sentiments on the contentious issue surrounding the Waqf (Amendment) Bill, 2024




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AAP MLA ‘assaults’ MCD official, case registered




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CBSE disaffiliates 21 schools over ‘dummy admissions’