Article
Chemistry, Medicinal
Jerome P. L. Ng, Mohit K. Tiwari, Ali Adnan Nasim, Rui Long Zhang, Yuanqing Qu, Richa Sharma, Betty Yuen Kwan Law, Dharmendra K. Yadav, Sandeep Chaudhary, Paolo Coghi, Vincent Kam Wai Wong
Summary: The cytotoxic effects and anticancer mechanisms of 10 selected peroxides were investigated on different cancer cell lines. Peroxides 7 and 8 showed a better P-gp inhibitory effect and induced apoptosis through a ROS- and caspase-3-independent pathway.
Article
Chemistry, Multidisciplinary
Mohammad Hassam, Ajit Shankar Singh, Dinesh Kumar Yadav, Chandan Singh, Sunil K. Puri, Ved Prakash Verma
Summary: The newly synthesized trioxane compounds showed good oral antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis, with the most active compound providing 100% protection to infected mice.
Review
Chemistry, Medicinal
Monika Shukla, Komal Rathi, Mohammad Hassam, Dinesh Kumar Yadav, Manvika Karnatak, Varun Rawat, Ved Prakash Verma
Summary: The demand for novel, fast-acting, and effective antimalarial medications is rapidly increasing due to the spread of multidrug resistant forms of malaria parasites. Various strategies have been employed to address drug resistance, including targeted therapies, the hybrid drug idea, and the development of advanced analogues of existing drugs. The 1,2,4-trioxane ring system in artemisinin (ART) has been identified as a key pharmacophoric moiety for the potential of endoperoxide-based antimalarials.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Chemistry, Medicinal
Monika Shukla, Mohammad Hassam, Dinesh Kumar Yadav, Siddharth Sharma, Chandan Singh, Sunil K. Puri, Rahul Shrivastava, Ved Prakash Verma
Summary: Malaria epidemics pose a threat to low-income countries, and novel 1,2,4-trioxanes have shown promising anti-malarial activity in mice, with some compounds demonstrating twice the efficacy of artemisinin.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Thomas De Dios Miguel, Dan Louvel, Killian Onida, Adeline Lavoignat, Stephane Picot, Nicolas Duguet
Summary: The study involved the peracetalization of a beta-hydroxy hydroperoxide derived from methyl oleate using benzaldehyde as a model substrate to produce fatty 1,2,4-trioxane. Different acid catalysts and solvents were investigated to optimize the reaction conditions, resulting in the formation of a mixture of regioisomers with only one diastereoisomer of each. Although the antimalarial activity of the trioxanes synthesized was not significant against Plasmodium falciparum, the study provided valuable insights into the synthesis and potential biological activity of these compounds.
SYNTHESIS-STUTTGART
(2022)
Article
Chemistry, Multidisciplinary
Akriti Kumari, Manvika Karnatak, Ajit Shankar Singh, Mohammad Hassam, Varun Rawat, Mohammad Shahidul Islam, Abdullah Mohammed Al-Majid, Mandeep Singh, Ved Prakash Verma
Summary: A mechanistic approach was used to study the metabolism of synthetic 1,2,4-trioxanes, potent antimalarial compounds, and evaluate their bioavailability for antimalarial action. The study found that under acidic conditions, the trioxanes degraded into corresponding ketones and glyoxal, and glyoxal polymerized to form a nonisolable condensate product. This indicates that the actual bioavailability of the drug is much lower than the administered dose.
Article
Biochemistry & Molecular Biology
Pavle Stojkovic, Ana Kostic, Ema Lupsic, Natasa Terzic Jovanovic, Miroslav Novakovic, Paraskev Nedialkov, Antoaneta Trendafilova, Milica Pesic, Igor M. Opsenica
Summary: This study describes the synthesis of 24 hybrid molecules consisting of sclareol and 1,2,4-triazolo [1,5-alpha] pyrimidines to improve cytotoxic properties, activity, and selectivity. The compounds were tested on U87 glioblastoma cells and showed significant reduction in cell viability. Several compounds demonstrated selectivity towards glioblastoma cells and evaded multidrug resistance. Hybrid compounds 12l, 12q, and 12r exhibited inhibition of P-glycoprotein activity and modulation of cellular processes in glioblastoma cells. Collateral sensitivity towards multidrug-resistant glioblastoma cells was achieved through modulation of oxidative stress accompanied by inhibition of mitochondria.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Paolo Coghi, Ivan A. Yaremenko, Parichat Prommana, Jia Ning Wu, Rui Long Zhang, Jerome P. L. Ng, Yulia Yu Belyakova, Betty Yuen Kwan Law, Peter S. Radulov, Chairat Uthaipibull, Vincent Kam Wai Wong, Alexander O. Terent'ev
Summary: In this study, the in vitro activities of bridged aminoperoxides against chloroquine-resistant Plasmodium falciparum and human cancer cells were investigated. The results showed that aminoperoxides exhibited good cytotoxicity against lung cancer cells, while synthetic ozonides displayed high activity against chloroquine-resistant P. falciparum. Moreover, the oxidative capacity of the compounds did not directly correlate with their activity, and the ozonides induced apoptosis in liver cancer cells through a ROS-independent dysfunction pathway.
Article
Microbiology
Kathrin Witmer, Farah A. Dahalan, Michael J. Delves, Sabrina Yahiya, Oliver J. Watson, Ursula Straschil, Darunee Chiwcharoen, Boodtee Sornboon, Sasithon Pukrittayakamee, Richard D. Pearson, Virginia M. Howick, Mara K. N. Lawniczak, Nicholas J. White, Arjen M. Dondorp, Lucy C. Okell, Kesinee Chotivanich, Andrea Ruecker, Jake Baum
Summary: Resistance to artemisinin-based combination therapy (ACT) in the Plasmodium falciparum parasite threatens recent progress in reducing global malaria deaths. Under artemisinin drug pressure, resistant parasites have a selective advantage in transmission, potentially leading to the spread of multidrug-resistant malaria beyond Southeast Asia.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Multidisciplinary Sciences
Nicholas Nyaaba, Nana Efua Andoh, Gordon Amoh, Dominic Selorm Yao Amuzu, Mary Ansong, Jose M. Ordonez-Mena, Jennifer Hirst
Summary: A network meta-analysis was conducted to evaluate the efficacy and safety of artemisinin derivatives and quinine for severe Plasmodium falciparum malaria. The results showed that artesunate reduced mortality in children and adults, including cerebral malaria. However, there was no consistent superiority among the artemisinin drugs in the assessed outcomes.
Article
Microbiology
Welmoed van Loon, Clara Bergmann, Felix Habarugira, Costanza Tacoli, Darius Savelsberg, Rafael Oliveira, Djibril Mbarushimana, Jules Ndoli, Augustin Sendegeya, Claude Bayingana, Frank P. Mockenhaupt
Summary: The study found an association between Plasmodium falciparum multidrug resistance-1 gene (pfmdr1) polymorphisms and altered antimalarial susceptibility, with a significant increase in the prevalence of the wild-type allele N86 and the wild-type combination NYD in recent years. The molecular data suggests a pattern shift in the pfmdr1 gene associated with artemether-lumefantrine resistance.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Chemistry, Physical
Yuan-Yuan Feng, Chang-E Dong, Rui Li, Xiao-Qing Zhang, Wei Wang, Xing-Rui Zhang, Wei -Wei Liu, Da-Hua Shi
Summary: A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized, and evaluated as antimalarial agents. The structures of these hybrids were confirmed, and compound 5c exhibited the best inhibitory activity.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Editorial Material
Microbiology
William L. Musick
Summary: Campylobacter species infections in immunocompromised patients can lead to serious diseases, but there is a lack of reliable data for treatment decisions and intrinsic antimicrobial resistance further limits treatment options. A recent study provides insights into this clinical dilemma through the investigation of a patient with Campylobacter coli bacteremia, including development, treatment, and molecular investigation.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Infectious Diseases
Melissa Mairet-Khedim, Camille Roesch, Nimol Khim, Sreynet Srun, Anthony Bouillon, Saorin Kim, Sopheakvatey Ke, Chhayleang Kauy, Nimol Kloeung, Rotha Eam, Chanra Khean, Chanvong Kul, Sophy Chy, Rithea Leang, Pascal Ringwald, Jean-Christophe Barale, Benoit Witkowski
Summary: The implementation of artesunate/mefloquine countrywide in Cambodia has not caused a significant increase in the prevalence of triple-resistant P. falciparum parasites. However, these parasites still circulate in the population and show clear resistance to piperaquine, mefloquine, and their combination. This study highlights the ability of P. falciparum to adapt to complex drug associations, which should be taken into consideration in future treatment strategies.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Article
Chemistry, Medicinal
Priyanka Yadav, Niraj Krishna Naikade, Mohammad Hassam, Ajit Shankar Singh, Chandan Singh, Sunil K. Puri, Ved Prakash Verma
Summary: Malaria, categorized as a life-threatening epidemic in underdeveloped countries, has been targeted for eradication by a novel series of synthesized compounds. In mouse models, these compounds demonstrated high protection, with compounds 17a1 and 17a2 proving twice as potent as artemisinin.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Organic
Bhanwar Kumar Malviya, Amanpreet Kaur Jassal, Manvika Karnatak, Ved Prakash Verma, Siddharth Sharma
Summary: This study reports a novel electro-oxidative cascade cyclization reaction, using electricity as the primary energy input, to synthesize a series of indolizine derivatives. This method provides a new strategy for generating heterocyclic diversity of indolizines.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Suman Swami, Rahul Shrivastava, Neelam Sharma, Arunava Agarwala, Ved Prakash Verma, Atul Pratap Singh
Summary: In this article, the authors reported the synthesis of a series of medicinally relevant 1,5-disubstituted tetrazoles using ultrasound irradiation via a one-pot 4-C reaction. The synthesized compounds were characterized by various spectroscopic techniques. The ultrasound-assisted green protocol exhibited advantages such as mild reaction conditions, high yield, catalyst and solvent-free reaction, short reaction time, and easy workup.
LETTERS IN ORGANIC CHEMISTRY
(2022)
Review
Chemistry, Analytical
Pooja Rawat, Parul Nain, Shaveta Sharma, Parshant Kumar Sharma, Vidhu Malik, Sudip Majumder, Ved Prakash Verma, Varun Rawat, Jong Soo Rhyee
Summary: Carbon quantum dots (CQDs) are promising carbonaceous nanomaterials with unique properties and wide applications. They are known for their excellent solubility and luminescence, and can be efficiently and economically prepared through sustainable chemical strategies. Recent advances have been made in the photoluminescence applications of CQDs in chemical and biological fields.
Article
Chemistry, Multidisciplinary
Akriti Kumari, Manvika Karnatak, Debanjan Sen, Varun Rawat, Shahnawaz Khan, Ved Prakash Verma
Summary: This study reports the evaluation of the binding profile of epoxide derivatives of 1,2,4-trioxanes to the Pf-DHFR receptor using molecular docking and dynamics experiments. The synthesized compounds showed a good binding profile to the protein.
STRUCTURAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Mahesh Meena, Bhanwar K. Malviya, Karandeep Singh, Priyanka Yadav, Pankaj Naharwal, Neetu Kumari, Ved Prakash Verma, Dinesh K. Yadav, Siddharth Sharma
Summary: An efficient methodology for the synthesis of indolizines from readily accessible substrates via I-2/FeCl3 is described. This approach provides a highly efficient and convenient way to obtain indolizine derivatives under relatively mild reaction conditions.
Article
Chemistry, Multidisciplinary
Akriti Kumari, Manvika Karnatak, Ajit Shankar Singh, Mohammad Hassam, Varun Rawat, Mohammad Shahidul Islam, Abdullah Mohammed Al-Majid, Mandeep Singh, Ved Prakash Verma
Summary: A mechanistic approach was used to study the metabolism of synthetic 1,2,4-trioxanes, potent antimalarial compounds, and evaluate their bioavailability for antimalarial action. The study found that under acidic conditions, the trioxanes degraded into corresponding ketones and glyoxal, and glyoxal polymerized to form a nonisolable condensate product. This indicates that the actual bioavailability of the drug is much lower than the administered dose.
Article
Chemistry, Physical
Bhawna Rani, Neelam Sharma, Rahul Shrivastava, Arunava Agarwala, Ved Praksah Verma
Summary: A styryl-BODIPY based receptor (SBT) has been synthesized as a colorimetric chemosensor for selective sensing of CN- and Cu2+ ions. The receptor exhibited notable optical color changes in the presence of aqueous solutions of CN- and Cu2+ ions respectively. It showed a linear shift in absorption peak for sensing CN- ions and selective sensing of Cu2+ ions over other competitive cations with detection limits lower than the recommended concentration of Cu2+ in drinking water.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Review
Chemistry, Medicinal
Monika Shukla, Komal Rathi, Mohammad Hassam, Dinesh Kumar Yadav, Manvika Karnatak, Varun Rawat, Ved Prakash Verma
Summary: The demand for novel, fast-acting, and effective antimalarial medications is rapidly increasing due to the spread of multidrug resistant forms of malaria parasites. Various strategies have been employed to address drug resistance, including targeted therapies, the hybrid drug idea, and the development of advanced analogues of existing drugs. The 1,2,4-trioxane ring system in artemisinin (ART) has been identified as a key pharmacophoric moiety for the potential of endoperoxide-based antimalarials.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Chemistry, Multidisciplinary
Neelam Sharma, Suman Swami, Sakshi Pathak, Ved Prakash Verma, Rahul Shrivastava
Summary: A simple and efficient method for the synthesis of substituted pyrazole-containing tetrazole derivatives has been developed using sulfonic acid decorated graphene oxide (GO-SO3H) as a catalyst. The GO-SO3H catalyst exhibited high catalytic activity, giving yields of over 95% within 15-20 minutes under mild reaction conditions. The catalyst was also found to be reusable for up to five reaction cycles without significant loss of efficiency. Spectroscopic techniques were used to confirm the structures of the synthesized compounds.
RESEARCH ON CHEMICAL INTERMEDIATES
(2023)
Article
Multidisciplinary Sciences
Mohammad Shahidul Islam, Abdullah Mohammed Al-Majid, Essam Nageh Sholkamy, Assem Barakat, Maurizio Viale, Paola Menichini, Andrea Speciale, Fabrizio Loiacono, Mohammad Azam, Ved Prakash Verma, Sammer Yousuf, Mohamed Teleb
Summary: Recently, clinical-stage spirooxindole-based MDM2 inhibitors have been introduced in cancer research protocols, but tumor resistance to the treatment has been reported. Therefore, researchers have focused on designing various combinatorial libraries of spirooxindoles. In this study, a new series of spirooxindoles were created through the hybridization of a chemically stable core and a pyrazole motif, inspired by lead pyrazole-based p53 activators and promising molecules previously reported. The derivatives were tested for cytotoxic activities on cancer cell lines and some showed potentiation of doxorubicin activity.
SCIENTIFIC REPORTS
(2023)
Review
Chemistry, Multidisciplinary
Garima Sachdeva, Yogita Bamal, Ankit Ladan, Om Shanker Tiwari, Varun Rawat, Priyanka Yadav, Ved Prakash Verma
Summary: The synthesis of polylactide has attracted attention recently due to its biocompatibility and environmental issues associated with fossil-fuel-based polymers. Polylactide can be obtained from natural sources or synthesized in a laboratory using various methods. Lewis acid catalyzed ring-opening polymerization is an effective pathway, and metal-calixarene complexes have been explored as suitable molecular scaffolds for lactide polymerization. This review summarizes the progress in using metal-calixarene complexes for the ring-opening polymerization of lactide.
Article
Chemistry, Organic
Riya Nagar, Dinesh Suwalka, Bhanwar Kumar Malviya, Ved Prakash Verma, Amanpreet Kaur Jassal, Siddharth Sharma
Summary: The combination of the Ugi reaction and electro-organic synthesis has been used to develop a new strategy for the synthesis of novel heterocycles with diverse functional groups. This approach offers high selectivity and is applicable for large-scale synthesis.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Dinesh Suwalka, Bhanwar Kumar Malviya, Ved Prakash Verma, Amanpreet Kaur Jassal, Siddharth Sharma
Summary: In this study, post-Ugi cyclization reactions were explored using N-centered radical-mediated intramolecular ipso cyclization to synthesize diverse spirocyclic variants of 4-imidazolidinones through the use of electrochemically generated amidyl radicals from the bis-amides of the Ugi adducts. This method features metal- and reagent-free reactions that are scalable and have broad substrate scope.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Kuldeep Singh Bhati, Dinesh Suwalka, Ved Prakash Verma, Amanpreet Kaur Jassal, Neetu Kumari, Siddharth Sharma
Summary: This paper presents a simple and efficient electrochemical method to induce structural alterations in 2H-indazole by modulating the cell voltage. The method allows for C-3 acyloxylation of 2H-indazole and facilitates the transfer of the acyl group from C-3 to N-1 for N-acylation of 2H-indazoles. Additionally, the use of the & mu;-electroflow reactor is demonstrated for gram-scale production of 3x in a short residence time.
Article
Chemistry, Medicinal
Priyanka Yadav, Niraj Krishna Naikade, Mohammad Hassam, Ajit Shankar Singh, Chandan Singh, Sunil K. Puri, Ved Prakash Verma
Summary: Malaria, categorized as a life-threatening epidemic in underdeveloped countries, has been targeted for eradication by a novel series of synthesized compounds. In mouse models, these compounds demonstrated high protection, with compounds 17a1 and 17a2 proving twice as potent as artemisinin.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
