Bacterial cell leakage potential of newly synthesized quinazoline derivatives of 1,5‐benzodiazepines analogue

2020 ◽  
Vol 57 (4) ◽  
pp. 1545-1558
Author(s):  
Apoorva Misra ◽  
Jaya Dwivedi ◽  
Shruti Shukla ◽  
Dharma Kishore ◽  
Swapnil Sharma
Keyword(s):  
Bacterial Cell ◽  
Quinazoline Derivatives ◽  
Derivatives Of ◽  
Cell Leakage

Quinazolinone Derivatives of Biological Interest V. Novel 4(3H)-Quinazolinones with Sedative-Hypnotic, Anticonvulsant and Antiinflammatory Activities

1993 ◽  
Vol 58 (8) ◽  
pp. 1963-1968 ◽  
Author(s):  
Abdel-Alim M. Abdel-Alim ◽  
Abdel-Nasser A. El-Shorbagi ◽  
Mahmoud A. El-Gendy ◽  
Hosny A. H. El-Shareif
Keyword(s):  
Present Communication ◽  
Biological Interest ◽  
Quinazoline Derivatives ◽  
Quinazolinone Derivatives ◽  
Derivatives Of

2-Methyl-4(3H)-quinazolines carrying alkyl, cycloalkyl, aralkyl or aryl substituents at N-3 of the quinazoline ring exhibit analgetic, antipyretic and antiinflammatory activities comparable to those of aspirin and phenylbutazone. In our previous work, various 4(3H)-quinazoline derivatives were prepared. The present communication is a continuation of our effort in this field.

scholarly journals Derivatives of Ribosome-Inhibiting Antibiotic Chloramphenicol Inhibit the Biosynthesis of Bacterial Cell Wall

2018 ◽  
Vol 4 (7) ◽  
pp. 1121-1129 ◽  
Author(s):  
Sivan Louzoun Zada ◽  
Keith D. Green ◽  
Sanjib K. Shrestha ◽  
Ido M. Herzog ◽  
Sylvie Garneau-Tsodikova ◽  
...  
Keyword(s):  
Cell Wall ◽  
Bacterial Cell ◽  
Bacterial Cell Wall ◽  
Derivatives Of

Novel derivatives of plant monomeric phenolics: act as inhibitors of bacterial cell-to-cell communication

2020 ◽  
Vol 141 ◽  
pp. 103856
Author(s):  
Nishi Srivastava ◽  
Surabhi Tiwari ◽  
Kalpna Bhandari ◽  
Ajaya K Biswal ◽  
A.K.S. Rawat
Keyword(s):  
Bacterial Cell ◽  
Cell Communication ◽  
Derivatives Of

scholarly journals Bacterial cell wall nature and its mode of resistance against antibiotic drugs: An Overview

2021 ◽  
Vol 16 (3) ◽  
Author(s):  
Saif Ali ◽  
Bhavtosh Sharma ◽  
Anita Rawat
Keyword(s):  
Cell Wall ◽  
Bacterial Cell ◽  
Bacterial Cell Wall ◽  
Human Beings ◽  
Inappropriate Use ◽  
Recurrent Uti ◽  
Antibiotic Drugs ◽  
A Cell ◽  
Current Article ◽  
Derivatives Of

Bacterial cell wall is made up of two derivatives of NAG (N- acetylglucosamine) and NAM (Nacetylmuramic) which forms peptidoglycan. On the basis of peptidoglycan bacteria are classified into two main categories: Gram-positive and Gram-negative. But there are some other bacteria which are devoid of cell wall like PPLOs (pleuropneumonia like organism) and some are L-form which do have a cell wall but they can switch to cell wall deficient state and vice-versa. L- form bacteria can change shapes to avoid antibiotics. Bacterial strain ST144 and ST782 were tested on media with or without osmo-protection in the presence and absence of Fosfomycin and showed that bacteria can switched to L-form and revert back to walled state after antibiotic treatment and causing recurrent UTI (Urinary tract infection) in patients. Inappropriate use of antibiotics and immunity effectors favour bacterial L- form. Bacteria have different mechanism of avoiding antibiotics but changing the morphology to L-form make difficult for antibiotics to identify the cell wall which makes bacteria to persist more in human body to causing full blown infection. Mutation caused by disassembly of ribosomal sub-unit can also helps the bacteria to survive in multi-drug environment. The current article highlights the nature of bacterial cell wall and its nature against antibiotic drugs in human beings.

Synthesis of New Quinazoline Derivatives of Expected Potential Bioresponses.

ChemInform ◽  
2003 ◽  
Vol 34 (4) ◽  
Author(s):  
Yvette A. Isaac ◽  
Mona H. Arsanious ◽  
HIsham A. Abd. El-Nabi
Keyword(s):  
Quinazoline Derivatives ◽  
Derivatives Of

scholarly journals ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DERIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH β-CYCLODEXTRIN

2018 ◽  
pp. 51-58
Author(s):  
Mossaraf Hossain ◽  
Ashis Kumar Nanda
Keyword(s):  
Inclusion Complexes ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Guest Molecules ◽  
Solubility Study ◽  
Solvent Free Condition ◽  
Potential Applications ◽  
Quinazoline Derivatives ◽  
Complex Chemistry ◽  
Derivatives Of

Objective: To synthesis a novel methodology of bioactive quinazoline derivatives under greener process to an excellent yields and increases their solubility via inclusion with β-cyclodextrin (CD). Methods: Derivatives of quinazoline compounds were prepared by the mixture of 3-amino-2-phenylquinazolin-4(3H)-one, derived from 2-phenyl-4H-benzo[1,3]oxazin-4-one by refluxing with hydrazine, substituted aromatic aldehyde and alumina intimately in an agate mortar and pestle under solvent-free condition. Using various techniques for preparing inclusion complexes, kneaded method is the best method for encapsulation in host-guest complex chemistry. All compounds including inclusion complexes were characterised by spectral methods. Results: Synthesized a series of novel quinazoline compounds under a very easier greener process with a commercially available reagent. However, their low bioavailability, due to low absorption and solubility, can limit their potential applications. CD was used to resolve this solubility problem. CD can easily accommodated the guest molecules to encapsulate inside its cavity due to interior the hydrophobic nature with a hydrophilic exterior part to form thermodynamically more stable molecular microcapsules, commonly name as host-guest complexes or inclusion complexes. In this sense, CD was utilized to enhance not only the solubility and bioavailability of these quinazoline compounds but also their antibacterial capacity. The formation of inclusion complex was thus confirmed by ultraviolet-visible spectroscopy (UV-VIS), Fourier Transform Infrared Spectrometry (FT-IR), differential scanning calorimetry (DSC) and solubility study technique. Conclusion: Here we have successfully unfolded an eco-friendly methodology for the synthesis of derivatives of quinazoline and increased their solubility via host-guest inclusion technique. From the spectral analysis, it was concluded that the quinazoline compound is fully encapsulated inside the cavity of the CD.

scholarly journals Antimicrobial Activity of Quinazolin Derivatives of 1,2-Di(quinazolin-4-yl)diselane against Mycobacteria

2017 ◽  
Vol 2017 ◽  
pp. 1-7
Author(s):  
Bikui Tang ◽  
Meili Wei ◽  
Qun Niu ◽  
Yinjiu Huang ◽  
Shuo Ru ◽  
...  
Keyword(s):  
New Drugs ◽  
Dependent Manner ◽  
Anticancer Activities ◽  
Quinazoline Derivative ◽  
Damage Level ◽  
New Strategy ◽  
Quinazoline Derivatives ◽  
Clinical Drugs ◽  
Dose Dependent ◽  
Derivatives Of

Mycobacterium tuberculosis (M. tuberculosis) is one of the leading causes of morbidity and mortality. Currently, the emergence of drug resistance has an urgent need for new drugs. In previous study, we found that 1,2-di(quinazolin-4-yl)diselane (DQYD), a quinazoline derivative, has anticancer activities against many cancers. However, whether DQYD has the activity of antimycobacterium is still little known. Here our results show that DQYD has a similar value of the minimum inhibitory concentration with clinical drugs against mycobacteria and also has the ability of bacteriostatic activity with dose-dependent and time-dependent manner. Furthermore, the activities of DQYD against M. tuberculosis are associated with intracellular ATP homeostasis. Meanwhile, mycobacterium DNA damage level was increased after DQYD treatment. But there was no correlation between survival of mycobacteria in the presence of DQYD and intercellular reactive oxygen species. This study enlightens the possible benefits of quinazoline derivatives as potential antimycobacterium compounds and furtherly suggests a new strategy to develop new methods for searching antituberculosis drugs.

The synthesis and binding of N-terminal derivatives of vancomycin to a bacterial cell wall analogue

1999 ◽  
pp. 2267-2270 ◽  
Author(s):  
Thomas F. Gale ◽  
Jochen Görlitzer ◽  
Simon W. O’Brien ◽  
Dudley H. Williams
Keyword(s):  
Cell Wall ◽  
Bacterial Cell ◽  
Bacterial Cell Wall ◽  
Derivatives Of

scholarly journals Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

2021 ◽  
Vol 9 ◽  
Author(s):  
Paulina Wdowiak ◽  
Joanna Matysiak ◽  
Piotr Kuszta ◽  
Katarzyna Czarnek ◽  
Ewa Niezabitowska ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Urinary Bladder Cancer ◽  
Biological Properties ◽  
Diagnostic Methods ◽  
Major Health ◽  
Complex Disorder ◽  
Wide Range ◽  
Quinazoline Derivatives ◽  
Cyclic Compounds ◽  
Derivatives Of

Cancer diseases remain major health problems in the world despite significant developments in diagnostic methods and medications. Many of the conventional therapies, however, have limitations due to multidrug resistance or severe side effects. Bladder cancer is a complex disorder, and can be classified according to its diverse genetic backgrounds and clinical features. A very promising direction in bladder cancer treatment is targeted therapy directed at specific molecular pathways. Derivatives of quinazolines constitute a large group of chemicals with a wide range of biological properties, and many quinazoline derivatives are approved for antitumor clinical use, e.g.,: erlotinib, gefitinib, afatinib, lapatinib, and vandetanib. The character of these depends mostly on the properties of the substituents and their presence and position on one of the cyclic compounds. Today, new quinazoline-based compounds are being designed and synthesized as potential drugs of anticancer potency against bladder cancers.

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