Category: CBL Articles

Novel 5-Nitro Isatin derivatives as DNA Gyrase inhibitors: synthesis, anti-microbial evaluation, molecular docking, ADMET predictions and QSAR studies

Novel series of 5-nitroindoline-2-ones was synthesized starting from 5-nitroindoline-2,3-dione 2 and 2-(5-nitro-2-oxoindolin-3-ylidene)hydrazine-1 carbothioamide 3. Compounds were evaluated for their antimicrobial activities. The data showed that compounds 2 and 6b have excellent antimicrobial activities against the two tested strains of G+ve bacteria Staphylococcus aureus and Streptococcus and E. coli when compared with the standards. Furthermore, in-vitro enzyme assay and molecular docking studies were performed for the compounds 2 and 6b against E. coli DNA gyrase B. Prediction of ADMET properties and QSAR study of compounds was carried out respectively.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/131

Phytochemical screening, GC-MS analysis and In-vitro Antioxidant potential of Parthenium hysterophorus Stem sequentially extracted fractions

Oxidative stress (OS) is involved in pathophysiological events of different diseases. Antioxidants mitigate and suppress the adverse effect of OS in the body. Due to lesser side effects and cost effectiveness natural antioxidant is a choice of people nowadays. The present study was designed to characterize/analyze phytochemicals and antioxidant potential in Parthenium hysterophorus (Asteraceae) stem (PHS) sequentially extracted fractions. Chemical characterization of PHS samples was carried out using Gas Chromatography-Mass Spectrometry (GC-MS) and Spectrophotometric techniques. Comparative antioxidant potential in PHS fractions was studied using in vitro antioxidant models. Thin layer chromatography (TLC) was performed to show a differential occurrence of phytochemicals in test fractions and related radical scavenging potential. PHS fractions showed differential presence of compounds. Appreciable radical scavenging, reducing power, and metal ion chelation potential was found in PHS fractions. In conclusion, P. hysterophorus stem may be considered a good source of natural antioxidant compounds.

https://pubs.thesciencein.org/journal/index.php/cbl/article/view/162

Green synthesized Allium cepa nanoparticles with enhanced antiprotozoal activities for E. gingivalis

Allium cepa has phytochemical characteristics well known to be used in our gastronomy. Due to its particle size, low systemic bioavailability is the major disadvantage associated that pose major hurdle for its use for medicinal purpose. These limitations can be overcome by converting the bulk size particles to nanosized particles. The present study was to prepare the nano-particles of Allium cepa with improved aqueous solubility, and to investigate their in-vitro efficacy against Entamoeba gingivalis, a protozoan associated with poor oral hygiene leading to advanced periodontal disease. Allium cepa nanoparticles of the size ranging 85–95 nm with the aqueous solubility of upto 3 mg/mL were prepared, and the anti-amoebic activities were tested in-vitro against Entamoeba gingivalis (ATCC 30927). The trophozoites of Entamoeba gingivalis were cultured in the presence of Allium cepa’s Bulk/nano- particles or metronidazole, the inhibition caused by each particles type at various concentrations was calculated by counting the viable trophozoites under the inverted microscope. Allium cepa nanoparticles showed inhibitory results of more than 80%, which is comparable with that of standard drug Metronidazole against E. gingivalis demonstrating its use as a potential anti-parasitic herbal drug.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/246

1,3,4 Oxadiazole: An emerging scaffold to target different growth factors and kinases

Five member heterocyclic 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. The important mechanism behind tumor suppression by 1,3,4-Oxadiazole is related with the inhibition of different growth factors, enzymes and kinases etc. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti- cancer activity. There are great potential in the development of the simple and small 1,3,4-oxadiazole nucleus which is present in various compounds that possess considerable pharmcological properties such as anticancer and aimed to evaluate new products. The main aim of this review article is to highlight the targeted activity of 1,3,4-Oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/163

Treatment of Type 2 diabetes mellitus (T2DM): Can GLP-1 Receptor Agonists fill in the gaps?

Type 2 diabetes mellitus (T2DM) is a chronic metabolic syndrome, which occurs due to increased glucose levels in the human body. There has been lot of work in developing novel approaches to tackle this disease. GLP-1 receptor (GLP-1R), one of the class-B G-protein-coupled receptors (GPCR), is a budding molecular target to design drugs for treating type 2 diabetes. In this review, authors have summarized the physiological actions of Glucagon-like peptide-1 receptor (GLP-1R) and current available drugs based on GLP-1 RAs. Some of the exemplary studies in this area have been examined in detail. Authors conclude that development of degradation-resistant, long-acting GLP-1 receptor agonists is a promising area of research and lot of work needs to be done to understand its mechanism of action.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/132

Design, synthesis, ADME prediction and anti-hyperglycemic evaluation of new alkoxyimino-substituted phenyl carboxylic acids as potent alpha-glucosidase inhibitors

In an attempt to further explore the role of substituted carboxylic acid derivatives as antidiabetic agent, a series of alkoxyimino-substituted carboxylic acid derivatives (101-206) were designed, synthesized and evaluated for their inhibitory potential against a-amylase and a-glucosidase enzyme. Among all the tested compounds, 102 & 105 has displayed the most potent activity against a-glucosidase with the IC50 of 142.21±1.8 mM and 182.83±2.43 mM respectively, as compared to the standard drug acarbose (136.89±1.67 mM). Based on the inhibition percentage, the inhibition activity of 102 and 105 on a-glucosidase had higher potential than a-amylase. The mode of binding interactions between the a-glucosidase enzyme and the compound 102 was established to be uncompetitive using kinetic analysis. The predicted drug-likeness properties (Lipinski parameters and in silico ADME properties) of the compounds revealed their suitability as potential drug candidate.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/130

Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice

urn:nbn:sciencein.cbl.2019.v6.115

Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice

Published in: Chemical Biology Letters

  • Suman Devi Maharshi Dayanand University
  • Jagjeet Singh Maharshi Dayanand University
  • Vijay Kumar Maharshi Dayanand University
  • Vinay Malik Maharshi Dayanand University

Keywords: histopathology, oxidative stress, kidney, lipid peroxidation, toxicology

Abstract

The present study investigated the effect of monocrotophos, a commonly used organophosphate pesticide exposure in the kidney tissues of the swiss albino mice. Monocrotophos was administered at the sub-lethal doses of 1.25mg/kg, 2.5 mg/kg and 5.0 mg/kg body weight for 24 hr. Monocrotophos toxicity generated oxidative stress in the mice as evidenced by significant decrease in the activities of glutathione, superoxide dismutase and catalase enzymes. The exposure increased the lipid peroxidation and protein oxidation in a dose dependent manner. Oxidative stress generation also elicited cytotoxic effects on the mice kidney which were supported by the histopathological changes like degeneration in glomerulus, bowmen’s capsule and tubules, hemorrhage, mononuclear cell infiltration, tubular cast and congested blood vessels in a dose-dependent manner. In conclusion, the study indicated that monocrotophos exposure at various doses induces significant deleterious health effects in mice kidney tissues via oxidative stress generation.

Cite as: Devi, S., Singh, J., Kumar, V., & Malik, V. (2019). Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice. Chemical Biology Letters, 6(2), 39-45.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/cbl/article/view/2

Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

urn:nbn:sciencein.cbl.2019v6.107

Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

Published in: Chemical Biology Letters

  • Ashish Bhatt Mewar University
  • Krishna Srivastava Shri Ramswaroop Memorial University
  • Ravi Kant Shri Ramswaroop Memorial University
  • Deepa Lakhmani Shri Ramswaroop Memorial University

Keywords: 4-methyl-1H-isochromen-1-one, 1,1-biphenyl-4,4-diamine, Antibacterial activity, anti-microbial activity

Abstract

Selected novel β-lactam and thiazolidinone derivatives have been synthesized by the reaction of 4-methyl-1H-isochromen-1-one with 1,1-biphenyl-4,4-diamine, followed by the reaction with substituted benzaldehyde and further by the reaction with chloroacetyl chloride (for β-lactam type) and with thioglycolic acid (for thiazolidinone type) respectively . All the compounds were characterised by 1H NMR, IR and mass spectroscopy. These compounds were screened for in-vitro antimicrobial activity against Staphylococus aureus, E. coli, Pseudomonas aeruginosa strain. Some compounds have shown very good efficacy against antibacterial strain.

Cite as: Bhatt, A., Srivastava, K., Kant, R., & Lakhmani, D. (2019). Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity. Chemical Biology Letters, 6(2), 46-54.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/cbl/article/view/35

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

urn:nbn:sciencein.cbl.2019v6.113

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

Published in Chemical Biology Letters

  • Pooja FNU University of Delhi
  • Nimisha Sinha University of Delhi
  • Sonu Kumar University of Delhi
  • Atul FNU University of Delhi
  • Sumit Kumar University of Delhi
  • Prashant Kumar SRM University
  • Abhishek Pandey University of Delhi
  • Pragya Sharma University of Delhi
  • Vithika Aggarwal University of Delhi
  • Poonam FNU University of Delhi
  • Poonam Mothsra University of Delhi
  • Brajendra Kumar Singh University of Delhi
  • Rishi Pal Singh University of Delhi
  • Yogesh Kumar University of Delhi

Keywords: Apoptotic inducer activity, anti-cancer, anti-tumor, breast cancer, enzyme inhibition, medicinal chemistry

Abstract

Coumarin, triazoles and thiazolidinones are one of the most preferred and high valued scaffolds frequently used in medicinal chemistry. The synthesis of newly designed coumarin based triazolyl-thiazolidinones was performed and new compounds were obtained in good yields. The listed compounds were evaluated for their apoptotic activity and determined the minimal inhibitory concentrations for each of the compound on SCC-4 cells using MTT viability test. Furthermore, apoptotic inducer activity was assayed by detecting the expression of caspase-3, a key apoptotic enzyme.

Cite as: FNU, P., Sinha, N., Kumar, S., FNU, A., Kumar, S., Kumar, P., Pandey, A., Sharma, P., Aggarwal, V., FNU, P., Mothsra, P., Singh, B., Singh, R., & Kumar, Y. (2019). Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3. Chemical Biology Letters, 6(2), 30-38.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/cbl/article/view/3

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

urn:nbn:sciencein.cbl.2019v6.111

Published in Chemical Biology Letters

  • Deepak Mishra Delhi Technological University
  • Atiya Fatima Delhi Technological University
  • Ram Singh Delhi Technological University
  • Nupur S Munjal Jaypee University of Information Technology
  • Vineet Mehta Jaypee University of Information Technology
  • Udayabanu Malairaman Jaypee University of Information Technology

Keywords: Alzheimer’s Disease, Brain disease, medicinal chemistry, coumarin derivative, AChE, BuChE, Nervous system, Neurological

Abstract

In this paper, we report the design, synthesis, in-silico, and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (7i) exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (8j) exhibited strongest inhibition with an IC50 value of 46.47 μM.  The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.

Cite as: Mishra, D., Fatima, A., Singh, R., Munjal, N., Mehta, V., & Malairaman, U. (2019). Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors. Chemical Biology Letters, 6(2), 23-30.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/cbl/article/view/36