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quinazoline as antimicrobials

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https://www.readbyqxmd.com/read/27769618/novel-substituted-hydrazono-indolo-2-1-b-quinazoline-6-12-dione-analogues-as-cytostatic-agents-synthesis-crystal-structure-biological-evaluation-and-molecular-docking-studies
#1
Ramu Guda, Sirassu Narsimha, Ramavath Babu, Srujana Muthadi, Harikiran Lingabathula, Rambabu Palabindela, Narsimha Reddy Yellu, Girijesh Kumar, Mamatha Kasula
A series of novel substituted hydrazono indolo[2,1-b]quinazoline-6,12-dione analogues have been synthesized and screened for their in vitro cytotoxic and antimicrobial activities. Among all the target compounds, 3c exhibited the most potent inhibitory activity against three cancer cell lines MCF-7, A549, HeLa with IC50 values 07.14±1.285μM, 09.18±0.968μM and 10.57±0.581μM respectively, while maintaining low toxicity towards non-cancer originated cell line, HEK-293. The detailed studies about molecular interactions with probable target protein indoleamine 2,3-dioxygenase (IDO1) were done by using docking simulations...
October 5, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27554444/synthesis-biological-evaluation-and-molecular-modeling-study-of-some-new-methoxylated-2-benzylthio-quinazoline-4-3h-ones-as-nonclassical-antifolates
#2
Shahenda M El-Messery, Ghada S Hassan, Mahmoud N Nagi, El-Sayed E Habib, Sarah T Al-Rashood, Hussein I El-Subbagh
A new series of 2,3,6-substituted-quinazolin-4-ones was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 28 and 61 proved to be active DHFR inhibitors with IC50 0.02 and 0.01μM, respectively. Molecular modeling studies concluded that recognition with the key amino acid Phe34 is essential for binding and hence DHFR inhibition. Compounds 34, 56 and 66 showed broad spectrum antimicrobial activity comparable to Gentamicin and Ciprofloxacin...
October 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27306606/antimicrobial-activity-of-new-2-thioxo-benzo-g-quinazolin-4-3h-one-derivatives
#3
Rashad Al-Salahi, Hatem A Abuelizz, Rabab El Dib, Mohamed Marzouk
BACKGROUND: The antimicrobial activity of a synthesized series of 28 2-thioxo-benzo[g]quinazolin-4(3H)-one derivatives was evaluated in vitro against five Gram-positive bacteria, including Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The antibacterial activity was extended to include five Gram-negative bacteria: Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Klebsiella oxytoca and Enterobacter cloacae...
June 9, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27140181/antimicrobial-activity-of-synthesized-2-methylthiobenzo-g-1-2-4-triazolo-1-5-a-quinazoline-derivatives
#4
Rashad Al-Salahi, Hatem A Abuelizz, Mahasin Wadi, Rabab A El Dib, Mohamed Marzouk
BACKGROUND: The present study was carried out to evaluate the antimicrobial activity of a synthesized 2-methylthio-benzo[g][1,2,4]triazolo[1,5-a]quinazoline series. The compounds (1-21) were tested against a variety of Gram-positive bacterial species including Bacillus subtilis (RCMB 01001 69-3), Enterococcus faecalis (RCMB 0100154-2), Staphylococcus aureus (RCMB 0100183-9), Staphylococcus epidermidis (RCMB 0100183-9) and Streptococcus pyogenes (RCMB 0100172-5). In addition, Gram-negative bacteria were also tested including Pseudomonas aeruginosa (RCMB 0100243-5), Escherichia coli (RCMB 010052-6), Proteus mirabilis (RCMB 01002 54-2), Klebsiella oxytoca (RCMB 01002 83-4) and Enterobacter cloacae (RCMB 01002 64-5)...
May 2, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27051427/quinazolinone-and-quinazoline-derivatives-recent-structures-with-potent-antimicrobial-and-cytotoxic-activities
#5
REVIEW
Elham Jafari, Marzieh Rahmani Khajouei, Farshid Hassanzadeh, Gholam Hossein Hakimelahi, Ghadam Ali Khodarahmi
The heterocyclic compounds have a great importance in medicinal chemistry. One of the most important heterocycles in medicinal chemistry are quinazolines possessing wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancer and analgesic activities. This skeleton is an important pharmacophore considered as a privileged structure. This review highlights the recent advances in the synthesis of quinazolines and quinazolinone derivatives with potent antimicrobial and cytotoxic activities...
January 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/26925267/novel-4-thiazolidinone-derivatives-as-anti-infective-agents-synthesis-characterization-and-antimicrobial-evaluation
#6
Amit Gupta, Rajendra Singh, Pankaj K Sonar, Shailendra K Saraf
A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100-400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity...
2016: Biochemistry Research International
https://www.readbyqxmd.com/read/26165131/synthesis-and-in-vitro-antimicrobial-evaluation-of-piperazine-substituted-quinazoline-based-thiourea-thiazolidinone-chalcone-hybrids
#7
D R Shah, H P Lakum, K H Chikhalia
In frames of the search for new biological entities to fight against recent drug-resistant microbial strains, we report a library of quinazoline-based thiourea/4-thiazolidinone/chalcone hybrids. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Klebsiella pneumoniae) and fungi (Candida albicans and Aspergillus clavatus) using the broth dilution technique. From the biological evaluation, (E)-3-(3,4-dimethoxyphenyl)-1-(4-((4-(4-ethylpiperazin-1-yl)quinazolin-2-yl)amino)phenyl)prop-2-en-1-one was found to be the most active analogue (microbial inhibition concentration 3...
March 2015: Bioorganicheskaia Khimiia
https://www.readbyqxmd.com/read/25400411/design-and-synthesis-of-quinazoline-carboxylates-against-gram-positive-gram-negative-fungal-pathogenic-strains-and-mycobacterium-tuberculosis
#8
Theivendren Panneer Selvam, Arumugam Sivakumar, Padmavathi P Prabhu
AIM: A novel series of ethyl 5-(4-substituted phenyl)-3-methyl-6,7,8,9-tetrahydro-5H-thiazolo[2,3-b] quinazoline-2-carboxylate 3a-3j, were synthesized, characterized by spectral, elemental analyses and screened for their in vitro antibacterial and Mycobacterium tuberculosis (MTB) activities. MATERIALS AND METHODS: The in vitro antibacterial and antifungal activities were determined by agar well-diffusion and cup-plate agar diffusion methods and the anti-tuberculosis (TB) screening for test compounds were evaluated against MTB H37Rv strain by Resazurin assay...
October 2014: Journal of Pharmacy & Bioallied Sciences
https://www.readbyqxmd.com/read/25139568/synthesis-biological-evaluation-and-molecular-modeling-study-of-2-1-3-4-thiadiazolyl-thio-and-4-methyl-thiazolyl-thio-quinazolin-4-ones-as-a-new-class-of-dhfr-inhibitors
#9
Sarah T Al-Rashood, Ghada S Hassan, Shahenda M El-Messery, Mahmoud N Nagi, El-Sayed E Habib, Fatmah A M Al-Omary, Hussein I El-Subbagh
A new series of 2-(1,3,4-thiadiazolyl- or 4-methyl-thiazolyl)thio-6-substituted-quinazolin-4-one analogs was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, and antitumor activities. Compounds 29, 34, and 39 proved to be the most active DHFR inhibitors with IC50 values range of 0.1-0.6 μM. Compounds 28, 31 and 33 showed remarkable broad-spectrum antimicrobial activity comparable to the known antibiotic Gentamicin. Compounds 26, 33, 39, 43, 44, 50, 55 and 63 showed broad spectrum antitumor activity with GI values range of 10...
September 15, 2014: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/24901072/the-human-cathelicidin-ll-37-induces-muc5ac-mucin-production-by-airway-epithelial-cells-via-tace-tgf-%C3%AE-egfr-pathway
#10
Yuke Zhang, Maoxiang Zhu, Zhihua Yang, Xiujie Pan, Yuanyuan Jiang, Congcong Sun, Qin Wang, Wei Xiao
AIM: To investigate the mechanism for LL-37 inducing MUC5AC mucin production in airway epithelial cells. MATERIALS AND METHODS: The airway epithelial NCI-H292 cells were stimulated with various concentrations of LL-37 synthetic peptide and scrambled LL-37 (sLL-37) synthetic peptide ranged from 2.5 to 10 μg/mL. The effects of LL-37 and sLL-37 on TNF-α-converting enzyme (TACE) and EGFR activation and MUC5AC mucin production were evaluated by fluorescence resonance energy transfer (FRET) assay, Western blotting and ELISA respectively...
September 2014: Experimental Lung Research
https://www.readbyqxmd.com/read/24678278/spectral-characterization-and-3d-molecular-modeling-studies-of-metal-complexes-involving-the-o-n-donor-environment-of-quinazoline-4-3h-one-schiff-base-and-their-biological-studies
#11
Kuruba Siddappa, Sunilkumar B Mane, Deene Manikprabhu
A simple condensation of 3-amino-2-methylquinazoline-4-one with 2-hydroxy-1-naphthaldehyde produced new tridentate ONO donor Schiff base ligand with efficient yield. The structural characterization of ligand and its Cu(II), Ni(II), Co(II), Mn(II), Zn(II), and Cd(II) complexes were achieved by the aid of elemental analysis, spectral characterization such as (UV-visible, IR, NMR, mass, and ESR), and magnetic data. The analytical and spectroscopic studies suggest the octahedral geometries of Cu(II), Co(II), Ni(II) and Mn(II) complexes and tetrahedral geometry of Zn(II) and Cd(II) complexes with the tridentate ONO Schiff base ligand...
2014: TheScientificWorldJournal
https://www.readbyqxmd.com/read/24374193/antiviral-autophagy-restrictsrift-valley-fever-virus-infection-and-is-conserved-from-flies-to-mammals
#12
Ryan H Moy, Beth Gold, Jerome M Molleston, Veronica Schad, Kilangsungla Yanger, Mary-Virginia Salzano, Yoshimasa Yagi, Katherine A Fitzgerald, Ben Z Stanger, Samantha S Soldan, Sara Cherry
Autophagy has been implicated as a component of host defense, but the significance of antimicrobial autophagy in vivo and the mechanism by which it is regulated during infection are poorly defined. Here we found that antiviral autophagy was conserved in flies and mammals during infection with Rift Valley fever virus (RVFV), a mosquito-borne virus that causes disease in humans and livestock. In Drosophila, Toll-7 limited RVFV replication and mortality through activation of autophagy. RVFV infection also elicited autophagy in mouse and human cells, and viral replication was increased in the absence of autophagy genes...
January 16, 2014: Immunity
https://www.readbyqxmd.com/read/23966300/epidermal-egfr-controls-cutaneous-host-defense-and-prevents-inflammation
#13
Beate M Lichtenberger, Peter A Gerber, Martin Holcmann, Bettina A Buhren, Nicole Amberg, Viktoria Smolle, Holger Schrumpf, Edwin Boelke, Parinaz Ansari, Colin Mackenzie, Andreas Wollenberg, Andreas Kislat, Jens W Fischer, Katharina Röck, Jürgen Harder, Jens M Schröder, Bernhard Homey, Maria Sibilia
The epidermal growth factor receptor (EGFR) plays an important role in tissue homeostasis and tumor progression. However, cancer patients treated with EGFR inhibitors (EGFRIs) frequently develop acneiform skin toxicities, which are a strong predictor of a patient's treatment response. We show that the early inflammatory infiltrate of the skin rash induced by EGFRI is dominated by dendritic cells, macrophages, granulocytes, mast cells, and T cells. EGFRIs induce the expression of chemokines (CCL2, CCL5, CCL27, and CXCL14) in epidermal keratinocytes and impair the production of antimicrobial peptides and skin barrier proteins...
August 21, 2013: Science Translational Medicine
https://www.readbyqxmd.com/read/23895092/synthesis-antimicrobial-anticancer-evaluation-and-qsar-studies-of-thiazolidin-4-ones-clubbed-with-quinazolinone
#14
Aakash Deep, Balasubramanian Narasimhan, Kalavathy Ramasamy, Vasudevan Mani, Rakesh Kumar Mishra, Abu Bakar Abdul Majeed
A series of 3-(5-(arylidene)-2-(aryl)-4-oxothiazolidin-3-yl)-2-phenylquinazolin-4(3H)-one derivatives (1-18) was synthesized in appreciable yield and characterized by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro antimicrobial and anticancer potentials. Antimicrobial properties of the title compounds were investigated against Gram positive and Gram negative bacterial as well fungal strains. 3-(5-(3- Methoxybenzylidene)-2-(4-(dimethylamino)phenyl)-4-oxothiazolidin-3-yl)-2-phenyl quinazolin-4(3H)-one (16, pMICam = 1...
August 2013: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/23675295/volatile-metabolites-of-pathogens-a-systematic-review
#15
REVIEW
Lieuwe D J Bos, Peter J Sterk, Marcus J Schultz
Ideally, invading bacteria are detected as early as possible in critically ill patients: the strain of morbific pathogens is identified rapidly, and antimicrobial sensitivity is known well before the start of new antimicrobial therapy. Bacteria have a distinct metabolism, part of which results in the production of bacteria-specific volatile organic compounds (VOCs), which might be used for diagnostic purposes. Volatile metabolites can be investigated directly in exhaled air, allowing for noninvasive monitoring...
May 2013: PLoS Pathogens
https://www.readbyqxmd.com/read/23647672/antimicrobial-activity-of-newly-synthesized-methylsulfanyl-triazoloquinazoline-derivatives
#16
Rashad Al-Salahi, Mohamed Marzouk, Ghada Awad, Mohamed Al-Omar, Essam Ezzeldin
OBJECTIVE: The aim of this research was to study and evaluate the antimicrobial activity of a novel 2-methylsulfanyl-[1,2,4]triazolo[1,5-a]quinazoline and its derivatives. Antibacterial activity of the target compounds was tested against a variety of species of Gram-positive bacteria such as Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC6633, and Gram-negative bacteria such as Pseudomonas aeruginosa ATCC27953 and Escherichia coli ATCC 25922. In addition some yeast and fungi, Candida albicans NRRL Y-477 and Aspergillus niger, respectively, were screened...
June 2013: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/23641327/design-and-evaluation-of-novel-antimicrobial-and-anticancer-agents-among-tetrazolo-1-5-c-quinazoline-5-thione-s-derivatives
#17
Lyudmyla M Antypenko, Sergey I Kovalenko, Olexii M Antypenko, Andrey M Katsev, Olena M Achkasova
The novel heterocyclization of 5-(2-aminophenyl)-1H-tetrazole with potassium ethylxanthogenate or carbon disulfide was proposed. The potassium salt of the tetrazolo[1,5-c]quinazoline-5-thione was subsequently modified by alkylation with proper halogen derivatives to (tetrazolo[1,5-c]quinazolin-5-ylthio)alkyls, N,N-dialkylethylamines, 1-aryl-2-ethanones, 1-(alkyl)aryl-2-ethanols, carboxylic acids, and esters. The structures of all newly synthesized compounds were confirmed by FT-IR, UV-vis, LC-MS, (1)H, (13)C NMR, and elemental analysis data...
January 2013: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/23529860/synthesis-antimicrobial-evaluation-and-molecular-modelling-of-novel-sulfonamides-carrying-a-biologically-active-quinazoline-nucleus
#18
Mostafa M Ghorab, Zienab H Ismail, Mohamad Abdalla, Awwad A Radwan
A novel series of quinazolines 5-10, triazoloquinazolines 11-17 and triazinoquinazoline 19 bearing a biologically active sulfonamide moiety were synthesized, utilizing methyl 2-isothiocyanato benzoate 2. Some of the newly synthesized compounds revealed promising bacterial growth inhibition, compared with the ampicillin, as the reference drug. A LigandScout approach-generated pharmacophore model for the Staph aureus bacteria growth inhibition was done. The degree of fitting of the test set compounds (3, 4, 6, 8, 11, 17) to the generated hypothetical model revealed a qualitative measure of the more or less microbial inhibition of Staphylococcus aureus...
June 2013: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/23482309/synthesis-and-pharmacophore-modeling-of-novel-quinazolines-bearing-a-biologically-active-sulfonamide-moiety
#19
Mostafa M Ghorab, Zienab H Ismail, Awwad A Radwan, Mohamad Abdalla
In the present work, interaction of the strategic starting material, methyl 2-isothiocyanatobenzoate (1), with sulfa drugs resulted in the formation of methyl 2-[3-(4-(N-substituted sulfamoyl)phenyl)thioureido] benzoates 2-5, which upon reaction with hydrazine hydrate afforded N-amino derivatives 6-9. Triazoloquinazoline derivatives 10-18 were obtained via reaction of compounds 6-8 with aromatic aldehydes. Also, the reaction of compound 8 with formic acid gave the corresponding triazoloquinazoline derivative 19...
March 2013: Acta Pharmaceutica
https://www.readbyqxmd.com/read/23359525/novel-cationic-quinazolin-4-3h-one-conjugated-fullerene-nanoparticles-as-antimycobacterial-and-antimicrobial-agents
#20
Manishkumar B Patel, Uma Harikrishnan, Nikunj N Valand, Nishith R Modi, Shobhana K Menon
A series of novel cationic fullerene derivatives bearing a substituted-quinazolin-4(3H)-one moiety as a side arm were synthesized using the 1,3-dipolar cycloaddition reaction of C60 with azomethine ylides generated from the corresponding Schiff bases of substituted quinazolinones. The synthesized compounds 5a-f were characterized by elemental analysis, FT-IR, 1H NMR, 13C NMR, and ESI-MS and screened for their antibacterial activity against Mycobacterium tuberculosis (H37RV) and antimicrobial activity against selected Gram-positive (Staphylococcus aureus and S...
March 2013: Archiv der Pharmazie
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