Article
Biochemistry & Molecular Biology
Akshaya Murugesan, Saravanan Konda Mani, Ramesh Thiyagarajan, Suresh Palanivel, Atash V. Gurbanov, Fedor I. Zubkov, Meenakshisundaram Kandhavelu
Summary: This study synthesized several benzenesulfonamide derivatives and evaluated their inhibitory activities on TrkA in GBM cells. The compound AL106 was identified as a potential anti-GBM compound with lower toxicity in non-cancer cells compared to cisplatin. Docking analysis showed that AL106 has good interactions with TrkA.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Jiyu Du, Peipei Liu, Yanan Zhu, Guoxing Wang, Siqi Xing, Tongtong Liu, Jucheng Xia, Shuanghong Dong, Na Lv, Zeng Li
Summary: In this study, two series of tryptanthrin derivatives with benzenesulfonamide substituents were designed and synthesized to discover new anti-inflammatory agents. Among them, compound 8j showed the best inhibitory activity on nitric oxide production, with no toxicity. Further evaluation demonstrated that 8j could reduce the levels of pro-inflammatory cytokines and inhibit the p38 MAPK signaling pathway. In vivo studies showed that 8j could ameliorate the degree of foot swelling and knee joint pathology in adjuvant-induced arthritis rats.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Eman K. A. Abdelall, Lamees S. Aboelnaga, Randa M. Hassan, Phoebe F. Lamie
Summary: Novel chalcone 3a-c, pyrazoline 4a-i and pyridine 5a-c, 6a & b derivatives bearing methanesulfonamide moiety were synthesized and their structures were confirmed. In vitro and in vivo studies showed their COX-1/COX-2 inhibitory and anti-inflammatory activities. Histopathological and histochemical studies revealed the safety of the most active anti-inflammatory derivatives 4f-4i, especially 4h derivative, on gastric mucosa. Docking studies and physicochemical property predictions indicated good oral bio-availability for compounds 4f-i and 6b.
BIOORGANIC CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Rui Pereira, Artur M. S. Silva, Daniela Ribeiro, Vera L. M. Silva, Eduarda Fernandes
Summary: This review article provides an overview of the chemical structure, chemical properties, and synthesis methods of bis-chalcones. It also emphasizes the anti-inflammatory activity of bis-chalcones and their mechanisms of action.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Denisa Leonte, Daniel Ungureanu, Valentin Zaharia
Summary: This review discusses the synthesis and biological activity of flavones and related compounds, such as flavonols and aurones. It highlights the anticancer, antioxidant, and antimicrobial properties of natural and synthetic flavones and aurones, and summarizes the most promising methods for their synthesis. The review also focuses on the development of new effective antimicrobial derivatives and identifies the most promising antimicrobial agents. Overall, the review provides valuable insights into the synthesis and biological potential of flavones and related compounds.
Article
Microbiology
Runzhe Wu, Xunxi Dong, Qiang Wang, Zirui Zhang, Jianhua Wang, Xiao Wang
Summary: The study synthesized D1018M and D1018 peptides with improved activity and found that they exhibited enhanced resistance against proteases; D1018M showed slightly increased antimicrobial activity, and these peptides had low cytotoxicity, strong inhibitory effects on E. coli, and excellent inhibition capacity against LPS-induced proinflammation response.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Nisha Kamra, Suman Rani, Sumit Thakral, Ajeet Singh, Payare L. Sangwan, Shashank K. Singh, Samridhi Thakral, Vikramjeet Singh, Devinder Kumar
Summary: In this study, a series of novel heterocyclic chalcones were synthesized and screened for their cytotoxic and antimicrobial activity. Some of the heterocyclic chalcones showed good cytotoxicity and antimicrobial activity. Molecular docking results revealed multiple interactions between the synthesized heterocyclic chalcones and their respective biochemical targets.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Infectious Diseases
Carmen Maria Ferrer-Luque, Carmen Solana, Beatriz Aguado, Matilde Ruiz-Linares
Summary: Persistent infections in dentistry pose a challenge due to antibiotic resistance. Nonsteroidal anti-inflammatory drugs (NSAIDs) may be a promising alternative for biofilm control. This study evaluates the antimicrobial activity and cytotoxicity of sodium diclofenac (DCS), ibuprofen (IBP), and ibuprofen arginine (IBP-arginine) against endodontic polymicrobial biofilms. Results show that 4% IBP-arginine solution exhibits the highest antibiofilm activity, followed by 4% DCS and 4% IBP. Cytotoxicity results indicate that a mixed 4% IBP-arginine solution has the most promising outcome. NSAID solutions could be recommended for endodontic disinfection procedures.
Review
Biochemistry & Molecular Biology
Ying Luo, Yuzhu Song
Summary: Antimicrobial peptides (AMPs) are considered a new generation of antibiotics with not only antimicrobial activity but also antibiofilm, immune-regulatory, and other activities. Research on the mechanism of action of AMPs can aid in their modification and development, with many studies focusing on this area. AMPs exhibit a dual mechanism of action and possess antifibroblast and anti-inflammatory properties, making them a promising therapeutic prospect.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biotechnology & Applied Microbiology
Nansi Lopez-Valverde, Antonio Lopez-Valverde, Javier Montero, Cinthia Rodriguez, Bruno Macedo de Sousa, Juan Manuel Aragoneses
Summary: Periodontal diseases (PD) are chronic inflammatory oral pathologies that are strongly associated with other diseases in the body. The immune response in PD involves the upregulation of proinflammatory molecules and reactive oxygen species, leading to the development of oxidative stress. Natural antioxidants have anti-inflammatory properties and can reduce key PD indicators. This review analyzes the therapeutic potential of various natural products in treating PD.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2023)
Article
Chemistry, Physical
Jayze da Cunha Xavier, Francisco W. Q. de Almeida-Neto, Janaina E. Rocha, Thiago S. Freitas, Priscila R. Freitas, Ana C. J. de Araujo, Priscila T. da Silva, Carlos E. S. Nogueira, Paulo N. Bandeira, Marcia M. Marinho, Emmanuel S. Marinho, Nitin Kumar, Antonio C. H. Barreto, Henrique D. M. Coutinho, Murilo S. S. Juliao, Helcio S. dos Santos, Alexandre M. R. Teixeira
Summary: The six synthesized 2'-hydroxychalcones were tested for their synergistic effects and mechanisms against multiresistant strains of Staphylococcus aureus, showing significant influences on the MIC values of antibiotics, with A1, A4, A5, and A6 affecting ciprofloxacin and norfloxacin, A2 affecting penicillin, and no effect on erythromycin. The structures of the chalcones, such as the introduction of a furanic ring, chlorine atom and methoxy group at specific positions, a second double bond, and a fluorine atom, played a crucial role in the observed effects.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Organic
Mohammad Asad, Muhammad Nadeem Arshad, Abdullah M. Asiri, Salman A. Khan, Mohd Rehan, Mohammad Oves
Summary: The research established a reaction between chalcones and azomethine ylide to synthesize novel spiropyrrolidines, with compound 4c showing the most potent antibacterial activity against various bacterial strains.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Environmental Sciences
Marwa Kamal, Neveen Abdel-Raouf, Hana Sonbol, Heba Abdel-Tawab, Mohamed Sayed Abdelhameed, Ola Hammouda, Khaled N. M. Elsayed
Summary: This study proposed a method for synthesizing gold nanoparticles using ethanolic extracts of macroalgae. The nanoparticles showed strong antibacterial, antifungal, anti-inflammatory, and schistolarvicidal activities.
FRONTIERS IN MARINE SCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Weihong Lai, Jiaxin Chen, Xinjiao Gao, Xiaobao Jin, Gong Chen, Lianbao Ye
Summary: A novel chalcone derivative, A14, was discovered to have excellent antiproliferative activity against breast cancer cells. A14 could inhibit the proliferation and colony formation activity of MCF-7 cells, making it a promising compound for further anti-breast cancer research.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Food Science & Technology
Meghna Shashikant, Aarti Bains, Prince Chawla, Minaxi Sharma, Ravinder Kaushik, Sridhar Kandi, Ramesh Chander Kuhad
Summary: This study evaluated the physicochemical, functional, antimicrobial, and anti-inflammatory activity of Calocybe indica. The mushroom showed good nutritional composition, functional properties, and exhibited antimicrobial and anti-inflammatory effects. Therefore, it can be used as an effective food preservative, anti-inflammatory, and antimicrobial agent at the industrial level.
INTERNATIONAL JOURNAL OF FOOD MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Vikas Sharma, Rajiv Kumar, Andrea Angeli, Claudiu T. Supuran, Pawan K. Sharma
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Materials Science, Multidisciplinary
Ravi Kumar, Rahul Kaushik, Rajiv Kumar, D. Amilan Jose, Pawan K. Sharma, Annu Sharma
Summary: This study reports the structural, morphological, and optical analysis of Cu core Ag shell nanoparticles and nanocomposite films. The nanoparticles showed good sensitivity and selectivity for detecting CN- ions with a limit of detection of 0.15 μM.UV-visible analysis revealed that nanocomposites containing a specific percentage of nanoparticles effectively blocked the UV region of the electromagnetic spectrum.
MATERIALS CHEMISTRY AND PHYSICS
(2021)
Article
Biochemistry & Molecular Biology
Masaaki Akabane-Nakata, Namrata D. Erande, Pawan Kumar, Rohan Degaonkar, Jason A. Gilbert, June Qin, Martha Mendez, Lauren Blair Woods, Yongfeng Jiang, Maja M. Janas, Derek K. O'Flaherty, Ivan Zlatev, Mark K. Schlegel, Shigeo Matsuda, Martin Egli, Muthiah Manoharan
Summary: The 2'-fluorinated Northern-methanocarbacyclic nucleotides show good tolerance and comparable potency in RNAi-mediated gene silencing in mice. However, their activity may be affected at specific positions within the guide strand, and adding certain chemical groups may reduce their effectiveness.
NUCLEIC ACIDS RESEARCH
(2021)
Article
Chemistry, Organic
Pawan K. Sharma, Rajiv Kumar, Sita Ram, Navneet Chandak
Summary: A one-pot synthesis of beta-ketonitriles from 3-chloropropenals using benign reagents such as iodine, aqueous ammonia, and sodium hydroxide has been described. This approach is convenient, inexpensive, non-toxic, and eco-friendly.
SYNTHETIC COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Hartmut Jahns, Rohan Degaonkar, Peter Podbevsek, Swati Gupta, Anna Bisbe, Krishna Aluri, John Szeto, Pawan Kumar, Sarah LeBlanc, Tim Racie, Christopher R. Brown, Adam Castoreno, Dale C. Guenther, Vasant Jadhav, Martin A. Maier, Janez Plavec, Martin Egli, Muthiah Manoharan, Ivan Zlatev
Summary: In this study, small circular interfering RNAs (sciRNAs) were synthesized and evaluated for their therapeutic potential. Circularization improved metabolic stability of the sense strand and eliminated off-target effects, resulting in potent GaINAc-sciRNAs at therapeutically relevant doses. Physicochemical studies and NMR-based structural analysis shed light on the interactions of this novel class of siRNAs with the RNAi machinery.
NUCLEIC ACIDS RESEARCH
(2021)
Article
Chemistry, Medicinal
Rajiv Kumar, Amit Kumar, Sita Ram, Andrea Angeli, Alessandro Bonardi, Alessio Nocentini, Paola Gratteri, Claudiu T. Supuran, Pawan K. Sharma
Summary: Two series of novel benzenesulfonamides were synthesized and tested as hCA inhibitors, with amino-linked 1,2,4-thiadiazoles showing better inhibition of hCA I compared to thioureido-linked pyrazoles. Most of the newly synthesized sulfonamides exhibited strong inhibition of hCA II, while compound 8e was found to be the most selective inhibitor of hCA II.
ARCHIV DER PHARMAZIE
(2022)
Article
Materials Science, Multidisciplinary
Durgesh, Rajiv Kumar, Pawan K. Sharma, Annu Sharma
Summary: The study presents the structural and optical analysis of PVA embedded with Ni-Ag core-shell structure nanoparticles, including the formation of surface plasmon resonance band, changes in optical parameters, and the characteristics of the transmission spectra.
MATERIALS SCIENCE AND ENGINEERING B-ADVANCED FUNCTIONAL SOLID-STATE MATERIALS
(2022)
Review
Chemistry, Medicinal
Md Abul Barkat, Pawan Kaushik, Harshita Abul Barkat, Mohammad Idreesh Khan, Hazrina Ab Hadi
Summary: The COVID-19 outbreak caused by the coronavirus has resulted in numerous deaths and socio-economic burdens. Efforts are being made by scientific communities worldwide to find a suitable therapeutic drug. Although no promising drug has been discovered yet, plant chemicals are considered the best option due to their minimal side effects.
Article
Biochemistry & Molecular Biology
Amit Kumar, Kiran Siwach, Claudiu T. Supuran, Pawan K. Sharma
Summary: This study reviews the research in the past decade (2010-2020) focusing on the selective and potent inhibitors of tumor-associated isoforms hCA IX and hCA XII. The tail-approach has been identified as a promising method for designing selective inhibitors.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Amit Kumar, Kiran Siwach, Tanmay Rom, Rajiv Kumar, Andrea Angeli, Avijit Kumar Paul, Claudiu T. Supuran, Pawan K. Sharma
Summary: A library of 22 arylthiazolylhydrazono-1,2,3-triazoles was synthesized using a tail-approach method, characterized through various spectroscopic techniques, and screened in-vitro, revealing varying inhibition efficacy against different isoforms of hCA.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Kiran Siwach, Amit Kumar, Harish Panchal, Rajiv Kumar, Jitender Kumar Bhardwaj, Andrea Angeli, Claudiu T. Supuran, Pawan K. Sharma
Summary: In this study, two subsets of novel benzenesulphonamide compounds were designed and synthesized, which showed good inhibition activity against tumour-associated carbonic anhydrase IX. Some of these compounds also demonstrated interesting potential for inducing apoptosis in vitro.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Physics, Multidisciplinary
Ravi Kumar, Rajiv Kumar, Anil Arya, Pawan K. Sharma, Annu Sharma
Summary: Gold core and silver shell nanoparticles fabricated by an efficient synthetic route were used to fabricate polyvinyl alcohol nanocomposite thin films. The core-shell structure of the nanoparticles was confirmed by various characterization techniques. The optical and electrical properties of the nanocomposite films were studied.
BRAZILIAN JOURNAL OF PHYSICS
(2022)
Article
Chemistry, Medicinal
Vikas Sharma, Rajiv Kumar, Andrea Angeli, Claudiu T. Supuran, Pawan K. Sharma
Summary: In this study, a series of novel 1,2,3-triazole benzenesulfonamide compounds were designed and synthesized, and their inhibitory effects on human carbonic anhydrase were tested. The results showed that these compounds displayed variable inhibition constants against different isoforms of carbonic anhydrase, with some compounds exhibiting strong inhibitory potency. Computational simulations revealed the interactions between these compounds and the binding sites of carbonic anhydrase. The study emphasizes the importance of the synthesized 1,2,3-triazole compounds as building blocks for developing carbonic anhydrase inhibitor drugs.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Lalit Vats, Kiran Siwach, Andrea Angeli, Prerna Bikal, Jitender Kumar Bhardwaj, Claudiu T. Supuran, Pawan K. Sharma
Summary: In this study, novel benzenesulfonamide derivatives were synthesized and screened for their inhibitory effects on human carbonic anhydrase (hCA) isoforms. The compounds showed strong inhibition of the tumor-associated isoform hCA IX and moderate inhibition of the glaucoma-associated isoform hCA II. Compound 6Ac exhibited higher inhibitory activity than the standard drug acetazolamide. Selective hCA IX inhibitors also showed better apoptotic efficacy in goat ovarian cells.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Multidisciplinary
Kasper M. Beck, Pawan K. Sharma, Mick Hornum, Nikolaj A. Risgaard, Poul Nielsen
Summary: Research has shown that double-headed nucleotides containing two nucleobases each can form two sets of functional Watson-Crick base pairs when incorporated into dsDNA, behaving as dinucleotides. By preparing three new double-headed nucleic acid monomers, it has been demonstrated that the molecular information of 10 Watson-Crick base pairs can be condensed into highly stable 5-mer DhNA duplexes.
CHEMICAL COMMUNICATIONS
(2021)