Article
Chemistry, Multidisciplinary
Ashruba B. Danne, Mukund Deshpande, Jaiprakash N. Sangshetti, Vijay M. Khedkar, Bapurao B. Shingate
Summary: This study describes the design of a small library of new 1,2,3-triazole-appended bis-pyrazoles using a molecular hybridization approach, which show broad-spectrum antifungal activity with excellent minimum inhibitory concentration values against various fungal strains. Additionally, the compounds also exhibit promising antioxidant activity.
Article
Chemistry, Organic
Jeremy R. Tuck, Robert J. Tombari, Noah Yardeny, David E. Olson
Summary: In this study, arylazo-1,2,3-triazoles were successfully synthesized using azide-alkyne click chemistry, showcasing high thermal stabilities and near-quantitative bidirectional photoconversion.
Review
Chemistry, Applied
Farid Ahmed, Hai Xiong
Summary: This review summarizes the latest developments in chemosensors based on click generated triazoles for a range of metal cations, anions, and neutral analytes, highlighting the need for continuous research accumulation in this rapidly growing field to meet demand.
Article
Biochemistry & Molecular Biology
Lijie Wei, Haishan Sui, Jingjing Zhang, Zhanyong Guo
Summary: A novel inulin derivative (3) bearing 1,2,3-triazole and diphenyl phosphate was successfully synthesized using CuAAC Click chemistry, showing significantly enhanced antioxidant activity compared with inulin. In vitro evaluation revealed strong radical scavenging abilities of the derivative, particularly against hydroxyl radicals and superoxide radicals. The synthetic strategy may offer an effective approach for preparing new inulin antioxidant biomaterials.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Multidisciplinary
Alka Agarwal, Preeti Singh, Anand Maurya, Upendra Kumar Patel, Alka Singh, Gopal Nath
Summary: A new series of ciprofloxacin conjugates containing 1,2,3-triazole were designed, synthesized, and evaluated for their antimicrobial activity. Some of the conjugates showed superior activity compared to the control drug ciprofloxacin, and exhibited low hemolysis on red blood cells.
Article
Chemistry, Organic
Cong Guan, Jiabin Yin, Jian Ji, Jinhua Liu, Xiang Wu, Tong Zhu, Shunying Liu
Summary: A regioselective electrochemical C-H amination method using easily accessible ethers has been developed to synthesize N (2)-substituted 1,2,3-triazole. Multiple substituents, including heterocycles, were well-tolerated, and 24 examples were obtained in moderate to good yields. Control experiments and DFT calculations revealed that the electrochemical synthesis occurs through a N-tosyl 1,2,3-triazole radical cation process, promoted by single-electron transfer from the lone pair electrons of the aromatic N-heterocycle, and the desulfonation is responsible for the high N (2)-regioselectivity.
Article
Chemistry, Organic
Jose Laxio Arenas, Pascal Retailleau, Jean-Michel Gillet, Nour-Eddine Ghermani, Sandrine Ongeri, Benoit Crousse
Summary: The 5-fluoro triazole amino acid scaffold prepared by halogen exchange was successfully incorporated into peptides. The X-ray diffraction results revealed an important localization of the 5-fluoro triazole motif on one side of the negative potential surface, with the fluorine atom showing a cylindrical shape in its electron density deformation.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Paulo Sergio Goncalves Nunes, Gabriel da Silva, Sofia Nascimento, Susimaire Pedersoli Mantoani, Peterson de Andrade, Emerson Soares Bernardes, Daniel Fabio Kawano, Andreia Machado Leopoldino, Ivone Carvalho
Summary: ERK1/2 inhibitors are being explored for their potential to overcome resistance to RAF and MEK kinase inhibitors. A new 4-aminoquinazoline derivative, compound 25a, showed promising activity in BT-20 cells by inducing cell death through lactate dehydrogenase release and necrosis induction. The compound also led to cell cycle arrest and downregulation of key signaling pathways in breast cancer cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Nada Y. Tashkandi, Zahra M. Al-Amshany, Nasser A. Hassan
Summary: A series of compounds with potential antibacterial and antifungal activities were designed and synthesized, among which derivative 12 showed superior antibacterial activity against G-positive Bacillus cereus, and all compounds exhibited appreciable antifungal activity.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Md Toufiqur Rahman, Ann M. Decker, Lucas Laudermilk, Rangan Maitra, Weiya Ma, Sami Ben Hamida, Emmanuel Darcq, Brigitte L. Kieffer, Chunyang Jin
Summary: This study identified a series of novel GPR88 agonists, with one showing high potency and suitability for studying the function of GPR88 in the brain.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Plant Sciences
Kaveh Rasoolijokari, Peyman Salehi, Atousa Aliahmadi, Bahareh Heidari, Morteza Bararjanian
Summary: A series of 12 novel 1,2,3-triazole penicillin G derivatives were synthesized and evaluated for their antimicrobial activity. Compounds 5a and 5b showed the highest potency in inhibiting the growth of Staphylococcus aureus.
PHYTOCHEMISTRY LETTERS
(2023)
Article
Chemistry, Multidisciplinary
Julia Krzywik, Anna Nasulewicz-Goldeman, Witold Mozga, Joanna Wietrzyk, Adam Huczynski
Summary: In this study, a series of 1,4-disubstituted 1,2,3-triazoles were designed and synthesized, with compounds containing an ester or amide moiety in the fourth position of 1,2,3-triazole of 10-N-methylaminocolchicine showing the greatest therapeutic potential.
Article
Chemistry, Multidisciplinary
Menghan Cui, Changhui Su, Rong Wang, Qing Yang, Chunxiang Kuang
Summary: This novel and green route involves the direct synthesis of vinyl triazole derivatives with alkynes and triazoles promoted by an inorganic base under transition metal-free conditions, showing great catalytic activity for the anti-Markovnikov stereoselective hydroamination of alkynes. Good yields with excellent functional group tolerance are successfully achieved for a range of substrates, making it an advanced concept for the synthesis of alkenyl triazole with a versatile and cost-efficient approach.
Article
Chemistry, Medicinal
Ramesh Gondru, Sirisha Kanugala, Sneha Raj, C. Ganesh Kumar, Mukesh Pasupuleti, Janardhan Banothu, Rajitha Bavantula
Summary: A new series of triazole-thiazole hybrids were synthesized and evaluated for their in vitro antimicrobial activity, showing promising inhibitory effects against bacterial and Candida strains. Compounds 8i, 8k, and 8l demonstrated significant biofilm inhibitory activity against Bacillus subtilis and Staphylococcus aureus.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Medicinal
Juana Suarez-Garcia, Ma-Angeles Cano-Herrera, Alejandra Ramirez-Villalva, Aydee Fuentes-Benites, Nieves Zavala-Segovia, Marco A. Garcia-Eleno, M. Basavanag Unnamatla, Erick Cuevas-Yanez
Summary: A series of 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivatives, synthesized via copper catalyzed azide-alkyne cycloaddition, showed potential antimicrobial activity against Candida genus strains and filamentous fungi. One derivative exhibited remarkable selectivity comparable to that of Itraconazole against Rhizopus oryzae.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Reetika Singh, Christophe Hano, Gopal Nath, Bechan Sharma
Summary: The traditional medicinal plant Carissa carandas L. was used to green synthesize silver nanoparticles (AgNPs) with potential antioxidant and antibacterial activities, demonstrated through UV-Vis, FT-IR, XRD analysis, and DPPH assay.
Article
Pharmacology & Pharmacy
Mayank Gangwar, Sonam Rastogi, Digvijay Singh, Alka Shukla, Neeraj Dhameja, Deepak Kumar, Rajesh Kumar, Gopal Nath
Summary: This study administered different doses of bacteriophages orally to rats for acute and sub-acute toxicity studies, with results showing no adverse reactions in experimental animals, and minimal changes in food and water intake and body weight compared to the control group.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Surgery
Ajay K. Khanna, Awaneesh Katiyar, Soumya Khanna, Gopal Nath, Puneet Kumar, Satyendra K. Tiwary
Summary: This study aimed to investigate if infection can be an etiological factor for varicose veins. The results confirmed the association between microbiological etiology and varicose veins through culture studies and DNA analysis.
INDIAN JOURNAL OF SURGERY
(2023)
Article
Biotechnology & Applied Microbiology
K. Bhargava, K. Gururaj, G. K. Aseri, G. Nath, N. P. Singh, R. V. S. Pawaiya, A. Kumar, A. K. Mishra, V. B. Yadav, N. Jain
Summary: Goats are of increasing significance in developing economies, but they are threatened by bacterial pathogens such as enteropathogenic Escherichia coli (EPEC). EPEC causes gastrointestinal disease in goat kids and lambs, leading to economic losses and potential public health risks. Antibiotics are the primary management method, but alternatives are needed due to antimicrobial resistance. This study identifies the prevalence of EPEC using gene analysis and demonstrates the potential of bacteriophages as a therapeutic alternative to antibiotics.
LETTERS IN APPLIED MICROBIOLOGY
(2022)
Article
Dermatology
Satyanam Kumar Bhartiya, Rina Prasad, Sumit Sharma, VijayKumar Shukla, Gopal Nath, Rajesh Kumar
Summary: This study evaluated the efficacy of topical bacteriophage therapy compared to conventional dressing for large traumatic wounds. The results showed that bacteriophage therapy was more effective in clearing infections and promoting wound healing, leading to shorter hospital stays and lower costs.
INTERNATIONAL JOURNAL OF LOWER EXTREMITY WOUNDS
(2022)
Article
Chemistry, Multidisciplinary
Alka Agarwal, Preeti Singh, Anand Maurya, Upendra Kumar Patel, Alka Singh, Gopal Nath
Summary: A new series of ciprofloxacin conjugates containing 1,2,3-triazole were designed, synthesized, and evaluated for their antimicrobial activity. Some of the conjugates showed superior activity compared to the control drug ciprofloxacin, and exhibited low hemolysis on red blood cells.
Article
Biotechnology & Applied Microbiology
V. B. Yadav, G. Nath
Summary: The study found that bacteriophage therapy could effectively treat Salmonella Typhimurium infection and eradicate the pathogen from mice in both acute and chronic infections.
LETTERS IN APPLIED MICROBIOLOGY
(2022)
Article
Computer Science, Information Systems
Aditya Pradhan, Srikanth Prabhu, Krishnaraj Chadaga, Saptarshi Sengupta, Gopal Nath
Summary: The COVID-19 pandemic has had catastrophic consequences on the global economy and well-being of people. Using supervised machine learning models, researchers have proposed an innovative method to predict COVID-19 and identify high-risk patients with a high accuracy rate. However, more research is needed to determine if this method can replace clinical diagnosis.
Article
Computer Science, Information Systems
Gopal Nath, Yawei Wang, Austin Coursey, Krishna K. Saha, Srikanth Prabhu, Saptarshi Sengupta
Summary: This paper introduces how to use predictive analytics and machine learning algorithms to reduce the impact of absenteeism on productivity and proposes optimization methods in classifying absenteeism models. By preprocessing and analyzing data from a Brazilian courier company, and utilizing various machine learning classification methods, the best model is selected. A web-based decision tool supported by cognitive analytics management theory is also provided for managers to make informed decisions without prior knowledge of machine learning.
Article
Pharmacology & Pharmacy
Manish Nath Tripathi, Kirti Singh, Umakant Yadav, Rohit Ranjan Srivastava, Mayank Gangwar, Gopal Nath, Preeti S. Saxena, Anchal Srivastava
Summary: In this study, a biosensor based on surface-enhanced Raman spectroscopy (SERS) was developed for rapid, sensitive, and early-stage detection of Japanese encephalitis (JE) antigen. By depositing silver nanoparticles on a glass coverslip as the substrate for the sensing platform, a suitable surface for SERS was provided. The fabricated sensor showed a linear response in cases of low viral load and could be used for specific diagnosis at the nanogram level.
ANTIVIRAL RESEARCH
(2022)
Review
Biochemistry & Molecular Biology
Bhawana Sharma, Alka Agarwal, Satish Kumar Awasthi
Summary: Despite prevention methods, malaria remains a devastating infection caused by protozoal parasites, resulting in nearly 500,000 fatalities annually. The expansion of drug-resistant malaria parasites poses a threat to the progress made in eradicating the disease. To overcome this obstacle, the development of newly synthesized drugs with multiple modes of action, made possible by hybridization, is necessary. This review outlines the most potent hybrid drugs against Plasmodium species.
RSC MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Prateek Kumar, Taniya Bhardwaj, Ankur Kumar, Bhuvaneshwari R. Gehi, Shivani K. Kapuganti, Neha Garg, Gopal Nath, Rajanish Giri
Summary: This study investigates drug repurposing for the proteases of SARS-CoV-2, identifying potential inhibitors such as hyaluronic acid and acarbose. Molecular dynamics simulation confirms the stable binding of these drugs with the proteases, suggesting their potential for structure-based drug discovery against SARS-CoV-2.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Review
Pharmacology & Pharmacy
Kanika Bhargava, G. Nath, G. K. Aseri, Neelam Jain
Summary: The COVID-19 pandemic has caused massive destruction and high mortality rate primarily due to multi drug resistant microbial infections, unrestrained inflammatory response and delayed antibody production.
INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Primary Health Care
Prerna Srivastava, C. P. Mishra, Gopal Nath
Summary: The study found that the period prevalence of diarrhea in rural under-five children in India was 35.9%, with the highest prevalence in the 0-12 month age group and the lowest in the 49-59 month age group. The study also revealed that a high proportion of cases were treated by unlicensed healthcare providers and a significant number received no treatment at all. While there has been a National Program for Control of Diarrheal Diseases in place for decades, the management of diarrhea in under-five children in rural India still faces challenges.
JOURNAL OF FAMILY MEDICINE AND PRIMARY CARE
(2021)
Article
Plant Sciences
Archana Singh, Paras Nath Singh, Gopal Nath, Nawal Kishore Dubey
Summary: A new species of Pseudocercospora causing leaf spot disease on Crotalaria assamica in India has been identified based on morphological and genetic analyses. The species shows similarities to allied species in the genus Pseudocercospora but is distinguished by its catenate and branched conidia. Phylogenetic analysis using LSU and ITS supports its classification as a new species in the Pseudocercospora genus.
TURKISH JOURNAL OF BOTANY
(2021)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
