Article
Chemistry, Multidisciplinary
Chrysoula Mikra, Zoi Melissari, Maroula G. Kokotou, Panagiotis Gritzapis, Konstantina C. Fylaktakidou
Summary: A series of quinazolinone derivatives were synthesized using a microwave-assisted one-pot four-component or two-step reaction protocol. The reaction conditions and yield were evaluated, and the molecules were found to have potential applications in organic, medicinal, and material chemistry.
SUSTAINABLE CHEMISTRY AND PHARMACY
(2022)
Article
Chemistry, Multidisciplinary
Apurba Dutta, Diganta Sarma
Summary: A metal, solvent and oxidant free method has been developed for the synthesis of quinazolin-4(3H)-ones under microwave irradiation. Using the same catalyst, 2,3-dihydroquinazolin-4(1H)-ones were also synthesized in water as a green and sustainable solvent. These protocols offer a simplistic and rapid approach for assembling diverse structural quinazolinones.
SUSTAINABLE CHEMISTRY AND PHARMACY
(2021)
Article
Chemistry, Organic
Natalia B. Kilimciler, Nicolas M. Palavecino, Nadia Gruber, Daniel R. Vega, Liliana R. Orelli, Jimena E. Diaz
Summary: A novel method utilizing trimethylsilyl polyphosphate (PPSE) has been developed to synthesize quinazolin4(3H)-imines (QIs) by reacting 2-aminobenzonitrile with secondary amides. This general reaction allows for the synthesis of N3-aryl and N3-alkyl QIs with varying 2-substituents, resulting in high yields. The procedure can also be applied to derivatives containing additional functional groups. The simplicity of the method, along with readily available starting materials and a mild dehydrating agent, makes it suitable for scalability. Based on literature data and experimental observations, a possible reaction path involving an intermediate nitrilium ion is proposed.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yueling He, Zhongtao Yang, Danyang Luo, Xiai Luo, Xiaodong Chen, Weiguang Yang
Summary: An oxidant-free and highly efficient synthesis of phenolic quinazolin-4(3H)-ones was achieved by stirring a mixture of 2-aminobenzamides, sulfonyl azides, and terminal alkynes. The intermediate N-sulfonylketenimine underwent two nucleophilic additions and the sulfonyl group eliminated through the power of aromatization. The natural product 2-(4-hydroxybenzyl)quinazolin-4(3H)-one can be synthesized on a large scale under mild conditions with this method.
Article
Chemistry, Multidisciplinary
Sumit Kumar, Kishor Padala, Barnali Maiti
Summary: A quinazolin-4(3H)-one ring system is a privileged heterocyclic moiety with distinct biological properties. This study presents an efficient strategy for the synthesis of quinazolin-4(3H)-one using substituted 2-amino benzamide with dimethyl sulfoxide as a carbon source and hydrogen peroxide as an oxidant.
Article
Biochemistry & Molecular Biology
Tebyan O. Mirgany, Ashraf N. Abdalla, Md Arifuzzaman, A. F. M. Motiur Rahman, Huda S. Al-Salem
Summary: A series of quinazolin-4(3H)-one derivatives showed potent cytotoxicity against human breast adenocarcinoma and ovarian carcinoma cell lines, with some compounds exhibiting inhibitory activity against key enzymes like CDK2, HER2, EGFR, and VEGFR2. Docking analysis revealed that compounds 2i and 3i act as inhibitors against specific kinases, showing superior interactions compared to known inhibitors. Additionally, the drug likeness properties of the derivatives demonstrated better ADME values than the positive control lapatinib.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Osamu Sano, Masahiro Ito, Masayo Saito, Akinori Toita, Toshio Tanaka, Hironobu Maezaki, Shinsuke Araki, Hidehisa Iwata
Summary: Phenotypic screening has identified a new modality of compounds called molecular glues, which induce the degradation of target proteins through ternary complexes of E3 ligases. In this study, a novel Cyclin K degrader, T4, was identified using global proteomic analysis, originally discovered through phenotypic screening for alternative poly-adenylation regulation. Further analysis revealed that T4 induces Cyclin K degradation and regulates alternative polyadenylation. Additionally, a more potent Cyclin K degrader, TR-213, was generated through a structure-activity relationship study of T4, providing novel chemical tools for studying Cyclin K degradation and alternative polyadenylation regulation.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Sumit Kumar, Kishor Padala, Barnali Maiti
Summary: The synthesis of quinazolin-4(3H)-one has always been a challenge in synthetic chemistry. In this report, we propose an efficient protocol using substituted 2-amino benzamide with dimethyl sulfoxide (DMSO) as a carbon source and H2O2 as an oxidant.
Article
Chemistry, Medicinal
Ling Lv, Mireguli Maimaitiming, Yan Huang, Jichen Yang, Shuxia Chen, Yanfeng Sun, Xuetao Zhang, Xin Li, Changhu Xue, Pingyuan Wang, Chang-Yun Wang, Zhiqing Liu
Summary: A series of quinazolin-4(3H)-one derivatives with cholinesterase inhibition and anti-inflammatory activities were designed and synthesized. The compound MR2938 showed promising inhibitory activity against acetylcholinesterase and suppressed NO production. It also decreased the levels of pro-inflammatory cytokines and suppressed neuroinflammation through blocking certain signaling pathways. These results suggest that MR2938 could be developed as a potential lead compound for anti-AD drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Divya Rohini Yennamaneni, Vasu Amrutham, Krishna Sai Gajula, Murali Boosa, Ramulamma Madasu, Narender Nama
Summary: Researchers successfully synthesized a wide range of quinazolin-4(3H)-ones using a heterogeneous beta zeolite catalyst through selective cleavage of the C-C bond of 1,3-diketones. This method offers a green and feasible approach by avoiding toxic transition metals, additives, and corrosive oxidants.
SUSTAINABLE CHEMISTRY AND PHARMACY
(2022)
Article
Chemistry, Physical
Priyanka Bhandu, Himanshu Verma, Manmeet Singh, Manoj Kumar, Gera Narendra, Shalki Choudhary, Pankaj Kumar Singh, Om Silakari
Summary: The withdrawal of Zenarestat from clinical trials due to renal toxicity was a setback in the development of ALR2-targeted agents for diabetic complications. However, by making structural modifications and using scaffold hopping, a library of optimized analogues was obtained, and some of them showed potential as ALR2 inhibitors. The synthesized quinazolin-4(3H)-one derivatives, particularly compounds Q2, Q3, and Q10, exhibited potent inhibitory activity against ALR2.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Xiaobin Wang, Jianqi Chai, Xiangyi Kong, Fei Jin, Min Chen, Chunlong Yang, Wei Xue
Summary: The development of novel fungicide candidates is crucial due to the emergence of resistant fungi in agricultural production. A series of 1,3,4-oxadiazole derivatives were constructed to evaluate their inhibition effects against phytopathogenic fungi, leading to the discovery of the promising inhibitor I32 against Rhizoctonia solani with significant preventative effects. Analysis through electron microscopy revealed the mechanisms behind I32's antifungal properties, providing valuable insights for future research in this field.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Agronomy
Mei Zhu, Yan Li, Dan-ping Chen, Cheng-peng Li, Gui-ping Ouyang, Zhen-chao Wang
Summary: In this study, a series of compounds with novel structures were designed and synthesized, and their antibacterial activity against Xanthomonas oryzae pv. oryzae was evaluated. Compound 1 exhibited remarkable antibacterial activity and decreased the pathogenicity of the bacteria. These findings suggest that these compounds have the potential to be used as bacteriostats to control rice bacterial leaf blight.
PEST MANAGEMENT SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Anastasios Panagopoulos, Thomas Balalas, Achilleas Mitrakas, Vassilios Vrazas, Katerina R. Katsani, Alexandros E. Koumbis, Michael I. Koukourakis, Konstantinos E. Litinas, Konstantina C. Fylaktakidou
Summary: Photochemo and photodynamic therapies are minimally invasive approaches for cancer treatment and combating bacterial resistance. Quinazolinone compounds, especially when appropriately substituted, show potential as new lead photosensitizers and DNA photocleaving agents under UV and visible light irradiation.
PHOTOCHEMISTRY AND PHOTOBIOLOGY
(2021)
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
Biotechnology & Applied Microbiology
Swapnil K. Warkhade, Sangesh P. Zodape, Umesh R. Pratap, Atul V. Wankhade
JOURNAL OF CHEMICAL TECHNOLOGY AND BIOTECHNOLOGY
(2018)
Article
Chemistry, Multidisciplinary
Swapnil K. Warkhade, Vayu Chaurasiya, Megha Rawat, Gayatri S. Gaikwad, Sangesh P. Zodape, Umesh R. Pratap, Atul V. Wankhade
Article
Green & Sustainable Science & Technology
Swapnil K. Warkhade, Ranjita S. Das, G. S. Gaikwad, Umesh R. Pratap, Sangesh P. Zodape, Atul V. Wankhade
ENVIRONMENTAL PROGRESS & SUSTAINABLE ENERGY
(2019)
Article
Chemistry, Physical
Swapnil K. Warkhade, Sangesh P. Zodape, Umesh R. Pratap, Atul Wankhade
JOURNAL OF MOLECULAR LIQUIDS
(2019)
Article
Chemistry, Multidisciplinary
Prabhakar Shrivas, Rajat Pandey, Sangesh Zodape, Atul Wankhade, Umesh Pratap
RESEARCH ON CHEMICAL INTERMEDIATES
(2020)
Article
Biotechnology & Applied Microbiology
Prabhakar Shrivas, Sangesh Zodape, Atul Wankhade, Umesh Pratap
ENZYME AND MICROBIAL TECHNOLOGY
(2020)
Article
Chemistry, Inorganic & Nuclear
Swapnil K. Warkhade, Rudra P. Singh, Ranjita S. Das, G. S. Gaikwad, Sangesh P. Zodape, Umesh R. Pratap, Atul Maldhure, Atul V. Wankhade
Summary: An artificial nanoenzyme, CoSe2, with unique flake-like morphology was reported to exhibit excellent intrinsic peroxidase-like activity with enhanced efficiency and stability compared to naturally found enzymes. The nanoenzyme showed a single electron transfer mechanism favoring the formation of products, and its unique morphology provided better accessibility for reactants, resulting in improved catalytic efficiency. Additionally, the synthesized CoSe2 nanoflakes demonstrated high thermal and chemical stability even after 365 days.
INORGANIC CHEMISTRY COMMUNICATIONS
(2021)
Article
Chemistry, Physical
Vandana S. Shende, Umesh R. Pratap, Atul Wankhade, Sangesh P. Zodape
Summary: In this study, experimental density and speed of sound data for the antihypertensive drug Hydralazine hydrochloride in water and two amino acid aqueous solutions were reported. Various parameters were calculated to understand the hydration behavior of the drug in different mediums.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Chemistry, Physical
Vandana S. Shende, Umesh R. Pratap, Atul Wankhade, Sangesh P. Zodape
Summary: This study measured the properties of two medicinal compounds in aqueous solutions, and investigated how the volume and compressibility of the solutes change with concentration and temperature, as well as the effect of amino acids on the solution properties.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Chemistry, Multidisciplinary
Prerna Khagar, Umesh R. Pratap, Sangesh P. Zodape, Atul V. Wankhade
Summary: This study presents a new and greener self-assembly method for CoSe2 microspheres, demonstrating their high peroxidase mimicking activity and efficient degradation of organic dyes.
Article
Thermodynamics
Anuja Jain, Vandana S. Shende, Dinesh V. Kawadkar, Umesh R. Pratap, Atul V. Wankhade, Sangesh P. Zodape
Summary: The study investigates the stability and behavior of ionic liquids by examining molecular interactions in water and mixed aqueous L-alanine solutions. Parameters such as density and speed of sound are analyzed at different temperatures, along with derived values like apparent molar volume and apparent molar isentropic compressibility for solutes. Transfer parameters for the movement of ionic liquids between aqueous and L-alanine solutions are also explored.
JOURNAL OF CHEMICAL THERMODYNAMICS
(2021)
Article
Engineering, Electrical & Electronic
Rudra P. Singh, Prerna S. Khagar, Adarsh K. Mourya, Swapnil K. Warkhade, Sangesh P. Zodape, Umesh R. Pratap, Atul Wankhade
Summary: Here, we report a facile hydrothermal synthesis method for the production of silver vanadate nano flakes, which can efficiently degrade various dyes under visible light irradiation. The synthesized material also exhibits excellent antibacterial properties, making it a promising disinfection and antibacterial material.
MATERIALS SCIENCE IN SEMICONDUCTOR PROCESSING
(2022)
Article
Chemistry, Physical
Shilpa H. Dani, Umesh R. Pratap
Summary: The copper-loaded melamine-terephthaldehyde based porous organic framework (MTPOF) is an effective catalyst for the C-S coupling reaction, exhibiting high catalytic activity and recyclability.
Article
Chemistry, Physical
Shivani Bhagat, Shilpa Dani, Ankit Verma, Ravinder Dharavath, Umesh R. Pratap
Summary: Covalent triazine frameworks (CTFs) are synthesized and integrated with copper ions to form a catalyst (Cu@CTF) with excellent performance for click reaction. The catalyst shows fast reaction rate, high yield, and recyclability, indicating its superior applicability in catalysis. This research advances the development and usage of functional CTF materials for catalysis.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Prabhakar Shrivas, Umesh Pratap
Article
Chemistry, Organic
Geeta Devi Yadav, Pooja Chaudhary, Balaram Pani, Surendra Singh
Summary: Chiral transition metal complexes with privileged ligands are efficient catalysts for various asymmetric organic transformations. Transition metal complexes of C1-symmetric pyrrolidine-based ligands have been widely used in asymmetric organic reactions. However, a comprehensive review article on the transition metal complexes of chiral C1-symmetric pyrrolidine-based ligands derived from (L)-proline has not been published.
TETRAHEDRON LETTERS
(2024)
