Article
Chemistry, Organic
Nilakshi Dutta, Bidyutjyoti Dutta, Apurba Dutta, Bipul Sarma, Diganta Sarma
Summary: An efficient and simple copper catalytic system has been developed for the synthesis of medicinally important 2-substituted quinazoline-4(3H)-ones and 2-substituted quinazolines. The protocol utilizes 2-aminobenzonitrile and benzyl alcohol derivatives, as well as 2-aminobenzylamine and benzaldehyde derivatives, and mild oxidant H2O2, resulting in excellent product yields. The versatility of the protocol is demonstrated through gram-scale syntheses.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Organic
Lin Zhang, Qian Chen, Linlin Li, Nana Ma, Jie Tian, Hao Sun, Qian Xu, Yuanyong Yang, Chun Li
Summary: Unprecedented metal-free synthesis of both Nunsubstituted and N3-substituted quinazoline-2,4(1H,3H)-diones from o-aminobenzamides and CO2 under atmospheric pressure at room temperature is developed. This protocol allows for easy variations of functional groups at the N3-position to accommodate the construction of many important drugs and bioactive compounds. The reaction is eco-friendly, versatile, and can be scaled up to gram scale.
Article
Chemistry, Medicinal
Neetu Dayal, Eva Reznickova, Delmis E. Hernandez, Miroslav Perina, Sandra Torregrosa-Allen, Bennett D. Elzey, Jana Skerlova, Haresh Ajani, Stefan Djukic, Veronika Vojackova, Martin Lepsik, Pavlina Rezacova, Vladimir Krystof, Radek Jorda, Herman O. Sintim
Summary: The study synthesized various compounds containing the 3H-pyrazolo[4,3-f]quinoline moiety, which exhibited potent activity against AML cell lines. The most active compounds effectively inhibited FLT3 kinase and its mutant forms, showing anticancer effects in a mouse model of AML.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Zonghui Ma, Ge Gao, Haiying Sun
Summary: This letter presents a simple and efficient method for the synthesis of pyrido[4,3-d]pyrimidine-2,4-diones and pyrido[4,3-d]pyrimidine-2,4,5(1H,3H,6H)-triones through the oxidative aromatization of easily synthesized 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2,4(1H,3H)-dione derivatives.
TETRAHEDRON LETTERS
(2021)
Article
Chemistry, Multidisciplinary
Abdolali Alizadeh, Azar Rostampoor
Summary: In this research, a simple and chemoselective synthesis of highly fluorescent polysubstituted dihydro-6H-chromeno[4,3-d]pyrazolo[1,5-a]pyrimidin-6-ones containing one chiral stereocenter is presented. The desired products were obtained with short reaction times, easy purification, and medium to high yields under relatively mild reaction conditions.
Article
Energy & Fuels
Zahra Ghamati, Mehdi Pordel, Abolghasem Davoodnia, Safar Ali Beyramabadi
Summary: The study synthesized new fluorescent heterocyclic compounds and characterized their properties through optical and cyclic voltammetry methods. These compounds, as organic photosensitizers, showed promising photovoltaic performance in dye-sensitized solar cells.
INTERNATIONAL JOURNAL OF ENERGY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Xiandeng Li, Tao Yang, Mengshi Hu, Yingxue Yang, Minghai Tang, Dexin Deng, Kongjun Liu, Suhong Fu, Yan Tan, Huan Wang, Yong Chen, Chufeng Zhang, Yong Guo, Bin Peng, Wenting Si, Zhuang Yang, Lijuan Chen
Summary: In this study, a series of novel compounds were synthesized that exhibited inhibitory effects on FLT3 and CDK4 kinases. The optimized compound 23k showed low nanomolar range activities and demonstrated antitumor therapeutic effects in both in vitro and in vivo evaluations.
BIOORGANIC CHEMISTRY
(2022)
Article
Crystallography
Zhi-Qiang Song, Ying-Jie Hou, Hai-Yang Sun, Qi-Di Zhong
Summary: This is a study on the crystal structure of C30H32N10O3. The experimental results provide the cell parameters and structural characteristics of the substance.
ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES
(2022)
Article
Chemistry, Multidisciplinary
Yibo Dong, Jinli Zhang, Jinchen Yang, Congcong Yan, Yangjie Wu
Summary: An efficient approach to quinazolin-4(3H)-ones was developed through a one-pot intermolecular annulation reaction, providing good functional group tolerance and high yields up to 98%. The control experiment showed that the thiol substrate can promote the dehydroaromatization step.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Ke Wang, Hao Chen, Xinyan Dai, Xupeng Huang, Zhiqiang Feng
Summary: This study describes the synthesis of 2-substituted quinazolin-4(3H)-ones using palladium catalysis and hydrogen transfer from o-nitrobenzamides and alcohols. The cascade reaction involves alcohol oxidation, nitro reduction, condensation, and dehydrogenation without the need for additional reducing or oxidizing agents, resulting in good to high yields of various quinazolin-4(3H)-ones.
Article
Chemistry, Multidisciplinary
Joydev K. Laha, Upma Gulati, Saima, Anjali Gupta, Harish Kumar Indurthi
Summary: An improved gram-scale synthesis of sildenafil has been developed using arylacetic acid, a cheap oxidant, and water, reducing costs by half and showing broad application in the synthesis of related derivatives.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Chemistry, Organic
Li-Ping Chen, Shu-Lin Cheng, Xin-Yue Fan, Ji-Fa Zhu, Bi-Qin Wang, Chun Feng, Shi-Kai Xiang
Summary: A palladium-catalyzed triple coupling reaction between 2-iodoanisoles and aryl iodides was developed. By using 3-methyl-2-pyridone as a ligand, the cross-coupling reaction was accelerated and the homo-coupling of 2-iodoanisoles was suppressed. Various 6H-dibenzopyran derivatives can be synthesized using this method.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Physical
Qing Tian, Jinli Zhang, Liang Xu, Yu Wei
Summary: An environmentally friendly electrochemical method was disclosed for the synthesis of quinazolin-4(3H)-one derivatives from readily available alpha-keto acids and 2-aminobenzamides. The decarboxylative cyclization process proceeds conveniently without the need for homogeneous metal catalysts, bases, or external oxidants. The protocol also features CO2 by-products, mild reaction conditions, and a wide variety of substrate scope, including an array of 2,3-disubstituted quinazolinone products.
MOLECULAR CATALYSIS
(2021)
Article
Chemistry, Medicinal
Romain Mustiere, Prisca Lagardere, Sebastien Hutter, Viviana Dell'Orco, Nadia Amanzougaghene, Shahin Tajeri, Jean-Francois Franetich, Sophie Corvaisier, Marc Since, Aurelie Malzert-Freon, Nicolas Masurier, Vincent Lisowski, Pierre Verhaeghe, Dominique Mazier, Nadine Azas, Patrice Vanelle, Nicolas Primas
Summary: Gamhepathiopine (M1) is a multi-stage acting antiplasmodial compound with poor stability, insufficient solubility, and low permeability. In this study, we synthesized 20 new derivatives based on a scaffold hopping strategy from M1, and identified a promising candidate, furane bioisostere 3j, with improved solubility and intestinal permeability, as well as good antiplasmodial activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Engineering, Environmental
Hisao Hori, Tomoki Ushio, Takuma Asai, Ryo Honma, Nadim Eid, Bruno Ameduri
Summary: The mineralization of a fluorotelomer surfactant in hot water was studied, and by optimizing conditions such as temperature and the presence of various chemicals, it was found that a combination of KMnO4 and O-2 efficiently decomposed the surfactant into F-, SO42-, and CO2. Minor products of perfluoroalkanes were detected in the gas phase, with majority and minor products accounting for high percentages of initial materials. The in situ formed MnO2 played a dominant role in the oxidation of the surfactant.
CHEMICAL ENGINEERING JOURNAL
(2021)
Article
Mechanics
Suresh S. Kumar, Arjun Shyam Sundar, R. Deepak
Summary: The stress intensity factor (SIF) of opposite surface cracks in an un-notched round bar under tension and combined load conditions was determined using a numerical method. The influence of loading modes on SIF was investigated, considering different crack depth ratios and crack aspect ratios. It was found that the SIF distribution changed as the crack depth ratio increased under pure tensile loading, and nonuniform and asymmetric SIF spread was observed when torque was applied. The effect of mode-II and mode-III fractures was more pronounced under combined loading.
MECHANICS BASED DESIGN OF STRUCTURES AND MACHINES
(2023)
Article
Mechanics
U. Magarajan, S. Suresh Kumar
Summary: This paper investigates the ballistic performance of AA6061-B4C surface composite targets fabricated by the Friction Stir Processing (FSP) technique. The paper is divided into two stages: stage I focuses on identifying suitable process parameters, while stage II conducts ballistic experiments for single and multiple hit conditions. The results show that FSPed AA6061-B4C targets exhibit better ballistic performance compared to BM targets.
MECHANICS BASED DESIGN OF STRUCTURES AND MACHINES
(2023)
Article
Materials Science, Multidisciplinary
Rajendran Praveen, Sajja Rama Koteswara Rao, Saurabh Suresh Kumar, Sundaram Suresh Kumar
Summary: The optimum thickness of aluminium alloy 7075 targets and the influence of heat treatment conditions on their high velocity impact response have been determined. Both experimental and numerical studies show that solution treated targets have higher microhardness and better ballistic performance, making them suitable for armored vehicles.
PROCEEDINGS OF THE INSTITUTION OF MECHANICAL ENGINEERS PART L-JOURNAL OF MATERIALS-DESIGN AND APPLICATIONS
(2023)
Review
Rehabilitation
Yohali Burrola-Mendez, Sureshkumar Kamalakannan, Paula W. Rushton, Selsabil-A. Bouziane, Ed Giesbrecht, R. Lee Kirby, Rosemary J. Gowran, David F. Rusaw, Tomasz Tasiemski, Mary Goldberg, Marco Tofani, Jessica P. Pedersen, Jon Pearlman
Summary: This review summarized the research literature on wheelchair service provision education and found limited information on integrating wheelchair content into professional rehabilitation programs. It suggests prioritizing international partnerships, improving the quality and timeliness of training programs, and providing resources for educators to integrate wheelchair-related content.
DISABILITY AND REHABILITATION-ASSISTIVE TECHNOLOGY
(2023)
Article
Public, Environmental & Occupational Health
Nurfaten Hamzah, Kamarul Imran Musa, Muhammad Hibatullah Romli, Xin Wee Chen, Mohd Zulkifli Abdul Rahim, Jafri Malin Abdullah, Mohd Azmi Suliman, Mohd Ismail Ibrahim, Tengku Alina Tengku Ismail, Iliatha Papachristou Nadal, Suresh Kumar Kamalakannan
Summary: The study aimed to translate and validate the CAFU instrument into Malay and test its validity and reliability among informal stroke caregivers in Malaysia. The results showed that the Malay-CAFU questionnaire had good relevancy, satisfactory item-level CVI, and high internal consistency. Therefore, the Malay-CAFU questionnaire is a valid and reliable instrument to assess the dependence level of stroke survivors and the upset level of informal stroke caregivers in Malaysia.
Review
Crystallography
Madunuri Chandra Sekhar, Eshwarappa Veena, Nagasamudram Suresh Kumar, Kadiyala Chandra Babu Naidu, Allam Mallikarjuna, Dudekula Baba Basha
Summary: This paper provides a review on recent advancements in piezoelectric materials and their applications in various fields such as catalysis, energy harvesting, and sensors. It also discusses the limitations of piezoelectric materials.
CRYSTAL RESEARCH AND TECHNOLOGY
(2023)
Article
Clinical Neurology
Sureshkumar Kamalakannan, Vijay Karunakaran, Ashwin Balaji, Aadi Sai Vijaykaran, Sivakumar Ramachandran, Ramakumar Nagarajan
Summary: ReWin, a digital therapeutics platform for stroke rehabilitation, was found to be feasible and acceptable in an Indian context through two phases of pilot testing. About 76% of participants used ReWin for more than half of the intervention period, and 90% of stroke care providers and 60% of stroke survivors and caregivers found the content of ReWin to be very relevant. Based on overall credibility, usability, and user-friendliness, 40% of stroke survivors and caregivers as well as 90% of stroke care providers rated the ReWin intervention as excellent.
FRONTIERS IN NEUROLOGY
(2023)
Review
Public, Environmental & Occupational Health
Tiago S. Jesus, Sureshkumar Kamalakannan, Sutanuka Bhattacharjya, Janet Prvu Bettger, Karen Jacobs, Helen Hoenig
Summary: This study describes a protocol for a mixed-methods systematic review aimed at identifying the usage and implementation of telerehabilitation in the delivery of rehabilitation services. The review will search six databases for relevant literature and use a framework synthesis approach to analyze the data. The results can inform future implementation efforts.
WORK-A JOURNAL OF PREVENTION ASSESSMENT & REHABILITATION
(2023)
Article
Health Policy & Services
Tiago S. Jesus, Karthik Mani, Sutanuka Bhattacharjya, Sureshkumar Kamalakannan, Claudia von Zweck, Ritchard Ledgerd
Summary: Occupational therapy workforce needs global strategy for strengthening, as there is a lack of research and resources, as well as various challenges and threats that need to be addressed.
INTERNATIONAL JOURNAL OF HEALTH PLANNING AND MANAGEMENT
(2023)
Article
Pediatrics
Manisha Shrestha, Gopal Bhandari, M. Optom, Sureshkumar Kamalakannan, Gudlavalleti Venkata Satyanarayana Murthy, Suresh Kumar Rathi, Anirudh Gaurang Gudlavalleti, Varun Agiwal, Hira Pant, Binod Pandey, Ramesh Ghimire, Daman Ale, Sajani Kayastha, Rakshya Karki, Daya Shankar Chaudhary, Raghunandan Byanju
Summary: This study aimed to evaluate the effectiveness of counseling and SMS/text messaging and phone calls to improve the follow-up rates among pediatric patients. The results showed that these interventions did not have a significant effect on improving the follow-up rate. However, the study provides useful insights for improving the follow-up rate among children with visual disabilities in Nepal and similar contexts.
JMIR PEDIATRICS AND PARENTING
(2023)
Review
Rehabilitation
Tiago S. Jesus, Karthik Mani, Claudia von Zweck, Sutanuka Bhattacharjya, Sureshkumar Kamalakannan, Ritchard Ledgerd
Summary: To fulfill their societal role, occupational therapists need to exist in sufficient supply, be equitably distributed, and meet competency standards. However, worldwide occupational therapy workforce research is scant and inequitably distributed, uses suboptimal methods, and is underfunded. Concerted efforts are needed to strengthen occupational therapy workforce research.
AMERICAN JOURNAL OF OCCUPATIONAL THERAPY
(2023)
Article
Chemistry, Physical
G. Velmurugan, Jasgurpreet Singh Chohan, S. A. Muhammed Abraar, R. Sathish, S. Senthil Murugan, M. Nagaraj, S. Suresh Kumar, V. Siva Shankar, D. Elil Raja
Summary: Natural fibre-based nanocomposite is a revolutionary material with excellent strength-to-weight ratio and lightweight, widely used in construction and dynamic industries. This study investigated the effects of silicon nanoparticles on the moisture absorption, mechanical properties, flammability, and dynamic mechanical behavior of PP/jute fibre composites. The results showed that increasing the weight of SiO2 nanoparticles improved the modulus of elasticity, tension strength, and elongation at breakage of the composites. The addition of SiO2 nanoparticles also enhanced the fire characteristics and dynamic mechanical behavior. However, the dispersion of SiO2 nanoparticles in the composites needs to be improved.
Article
Chemistry, Multidisciplinary
Rajapriya Pandy, Senthuran Suresh Kumar, Perumal Suresh, Jamespandi Annaraj, Mohan Pandi, Shanmugaiah Vellasamy, Suresh Sagadevan
Summary: In this study, seven endophytic fungi from Millingtonia hortensis were screened and five of them were found to produce taxol. The fungal taxol showed significant antibacterial and antifungal activities against human and fungal pathogens. Moreover, it exhibited cytotoxic effects against human liver cancer cells, suggesting its potential as an anticancer agent.
Article
Chemistry, Applied
Jhilmil Swapnalin, Suresh N. Kumar, Kadiyala Chandra Babu Naidu, Prasun Banerjee
Summary: This review investigates the applications of Electron paramagnetic resonance (EPR) in biological systems, discussing its latest developments in areas such as photosynthesis, metalloproteins, radical enzymes, and phospholipid membranes. By utilizing EPR spectroscopy, the dynamics and structure of biological systems can be calculated, providing a better understanding of the radical state of proteins compared to XRD or NMR techniques.
BIOINTERFACE RESEARCH IN APPLIED CHEMISTRY
(2023)
Review
Rehabilitation
Sureshkumar Kamalakannan, Paula W. Rushton, Ed Giesbrecht, David F. Rusaw, Selsabil-A Bouziane, Melodie Nadeau, Jennifer McKee, Rosemary J. Gowran, R. Lee Kirby, Jessica P. Pedersen, Tomasz Tasiemski, Yohali Burrola-Mendez, Marco Tofanin, Mary Goldberg, Jon Pearlman
Summary: This planned scoping review aims to examine and synthesize the global literature on wheelchair service provision education for healthcare professional students, healthcare personnel and educators. The review will provide insights into the organization, content, evaluation, and integration models of wheelchair service provision education on a global scale.
DISABILITY AND REHABILITATION-ASSISTIVE TECHNOLOGY
(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)
