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

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

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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

Author Guidelines for International Biomedical Frontiers Journal

Information for Authors for submitting articles to International Biomedical Frontiers Journal

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4. R.S. Buchanod, D.K. Reddy. In Selective Organic Transformations; T.R. Thyagarajan, Ed.; Integrated science: New York, 2002; Vol. 2, pp 1–95.

5. G.L. Loyale, U.S. Patent 5 934 456, 1998; Chem. Abstr. 1998, 65, 2870.

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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 Letters6(2), 23-30.

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

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

urn:nbn:sciencein.jmns.2019v6.109

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

Published in Journal of Materials NanoScience

  • Suman Sheoran M.D. University
  • Sitender Singh M.D. University
  • Ajay Mann M.D. University
  • Anura Samantilleke Universidade of Minho
  • Bernabe Mani Universitat Politecnica de Valencia
  • Devender Singh M.D. University

Keywords: nanophosphors, displays, lanthanide, luminescence, composites, LED

Abstract

A series of Eu3+ doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) was synthesized via sol-gel procedure at 950 oC. The optical characteristics of the materials were studied by Photoluminescence (PL) emission spectra. Upon 395 nm excitation and at 0.03 mole concentration of Eu3+ ion, these nanophosphors display optimum photoluminescence with most intense peak due to 5D07F2 (614-616) of dopant. Powder X-ray diffraction (PXRD) analysis proves that all synthesized materials are of crystalline nature and crystallinity improves on increasing temperature. Transmission electron microscopy (TEM) exhibited the spherical shape of particles in 13-30 nm size. Fourier Transformation infrared (FTIR) spectra showed peaks in 400-1000 cm-1 corresponding to gadolinium-oxygen and silicon-oxygen bond vibrations. In BaGd2Si3O10 material, Gd-O vibration is centered at 492 cm-1 and absorption band at 855 cm-1 is result of asymmetric vibrations of SiO in silicate tetrahedral unit. Due to excellent photoluminescence and suitable CIE coordinates, these materials could have brilliant applications in innovative displays.

Research Highlights

  • Series of trivalent europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+)fluorescent materials were synthesized successfully with sol-gel procedure.
  • The prepared samples were characterized using Photoluminescence analysis, X-ray diffraction study, Transmission Electron Microscopic analysis and Fourier Transform Infrared spectroscopy.
  • The CIE color coordinates values of phosphor confirmed the red color of complex approving the PL results.
  • X-ray diffraction pattern of these materials determined the particle size using Debye Scherrer’s equation.
  • Excellent photoluminescence response and nano size of these materials made them suitable for various innovative display applications.

Cite as: Sheoran, S., Singh, S., Mann, A., Samantilleke, A., Mani, B., & Singh, D. (2019). Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays. Journal of Materials NanoScience, 6(2), 73-81.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/jmns/article/view/109