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Hatzade K.,Rashtrasant Tukadoji Maharaj Nagpur University | Hatzade K.,Dhote Bandhu Science College | Taile V.,Rashtrasant Tukadoji Maharaj Nagpur University | Gaidhane P.,Rashtrasant Tukadoji Maharaj Nagpur University | Ingle V.,Rashtrasant Tukadoji Maharaj Nagpur University
Turkish Journal of Chemistry | Year: 2010

A convenient route to synthesize some new medicinally important 7-hydroxy-3-pyrazolyl chromones (3ai) is described. The interaction of 7-hydroxy-3-formyl chromone (1) with various substituted acetophenones and further cyclization with hydrazine hydrate in an aprotic solvent followed by condensation with 2, 3, 4, 6-tetra-o-acetyl-a-d-glucopyranosyl bromide afforded 2, 3, 4, 6-tetra-o-acetyl-β -d-glucopyranosyloxy- 3-(3-aryl-1H-pyrazol-5- yl)-4H-chromen-4-ones (4a-i). Later deacetylation with anhydrous zinc acetate in methanol gave 7-o-β -d-glucopyranosyloxy-3-(3-aryl-1H -pyrazol-5-yl)-4H- chromen-4-ones (5a-i). These compounds were evaluated for their in vitro antimicrobial and anti-oxidant activity. The structures of these newly synthesized o-glucosides were established by IR, NMR, mass spectra, elemental analysis, and chemical analysis. © TÜBİTAK.


Ghatole A.M.,Dhote Bandhu Science College | Lanjewar K.R.,Mohsinbhai Zawer College | Gaidhane M.K.,Shri Lemdeo Patil Mahavidyalaya | Hatzade K.M.,Dhote Bandhu Science College
Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy | Year: 2015

An library of unresolved racemic Mannich bases incorporating two stereogenic carbon centers was evaluated for antibacterial activity against clinically isolated Gram-positive bacteria i.e. Staphylococcus aureus, Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa and for antifungal activity against Candida albicans strains. Additionally, the susceptibility of microorganisms to Mannich bases prompted us to evaluate the potential for anti-tubercular activity against clinically isolated Mycobacterium tuberculosis and virulent H37Rv strains. All compounds showed potent activity against M. tuberculosis strains at MIC ranging from 50 μg/mL to 6.25 μg/mL of concentration. Facile one pot Mannich type syntheses of rac-(2S)-2-[(R)-[(4-substituted phenyl){[4-(4-substituted phenyl)-1,3-thiazol-2-yl]amino}methyl]cyclohexanone derivatives were achieved by reactions of various 2-amino-4-aryl-thiazoles, appropriately substituted aromatic aldehydes and cyclohexanone in Bronsted acidic quaternary ammonium sulfated ionic liquids serving as dual solvents and catalysts. © 2015 Elsevier B.V. All rights reserved.


Salunkhe M.Y.,Institute of Science | Choudhary D.S.,Dhote Bandhu Science College | Kondawar S.B.,Rashtrasant Tukadoji Maharaj Nagpur University
Der Pharma Chemica | Year: 2013

The substitution of trivalent aluminium in Sr-Y type hexaferrite is considered to be an important for the enhancement of its magnetic and electrical properties. A series of single phase polycrystalline samples with chemical composition Sr2Zn2AlxFe12-xO22 (x = 2-10) were prepared by high temperature solid state reaction technique. The formed samples were analyzed with the help of X-ray diffractometer for single phase without the traces of ambiguous reflections. It is found to have hexagonal Y type structure with space group R3m. the helium Picnometric real density nearly agrees with X ray density. The electrical conductivity and magnetic susceptibility measurement was carried out over the temperature range 400-800K. It shows semiconducting behavior with dual conduction mechanism for higher iron concentration. Magnetic study of the compounds was performed by Gouy's method. The Curie temperature TC and Curie molar constant CM of the compounds was found to be decreasing with increase in aluminium concentration.


Salunkhe M.Y.,Institute of Science | Choudhary D.S.,Dhote Bandhu Science College | Kulkarni D.K.,Institute of Science
Solid State Sciences | Year: 2010

A series of oxides with chemical formula Y1-xNaxCa2Cu3O7-δ (x = 0.1, 0.2, 0.3 & 0.4) have been synthesized by solid-state diffusion method. The influence of substitution of Na with different Y concentrations has been studied using XRD, electrical resistivity and ac magnetic susceptibility measurements. The formation is checked by XRD and all samples found to crystallize in a single phase with orthorhombic structure, isostructural to YCa2Cu3O7. The substitution of Na at Y site has a distinct effect on the superconducting properties of the oxides. With increase in Na content the critical temperature decreases. The resistivity of the compound above Tc is in the range of semiconductors but the behavior is metallic. © 2010 Elsevier Masson SAS. All rights reserved.


Giriya N.,Dhote Bandhu Science College | Timande S.,Dhote Bandhu Science College
Journal of Pure and Applied Microbiology | Year: 2013

The present study was aimed to investigate the efficacy of honey and citric acid against multidrug resistant clinical isolates of Pseudomonas aeruginosa from infected wounds. A total of twenty-four isolates of Pseudomonas aeruginosa were studied for sensitivity to honey and citric acid on the principle of minimum inhibitory concentration (MIC). The antibiogram suggests that all Pseudomonas aeruginosa isolates were resistant to Gentamicin and susceptible to Ciprofloxacin. The order of antibiotic resistance in Pseudomonas aeruginosa noted was Polymyxin-B > Ceftizoxime > Piperacillin > Tobramycin > Carbenicillin > Ceftazidime > Norfioxacin > Cefepime. The majority (80%) of multidrug resistant Pseudomonas aeruginosa isolates were inhibited by 30% v/v and 500 micrograms/milliliter of Honey and Citric acid concentration respectively. The present study showed that Pseudomonas aeruginosa isolates resistant to routinely used antibiotics were sensitive to antibacterial action of honey and citric acid. The findings of the present study demonstrated the role of honey and citric acid as antipseudomonal agents. This suggests that antibacterial honey and citric acid have potential to be an effective alternative antibacterial agent.


Hatzade K.M.,Rashtrasant Tukadoji Maharaj Nagpur University | Hatzade K.M.,Dhote Bandhu Science College | Taile V.S.,Rashtrasant Tukadoji Maharaj Nagpur University | Ingle V.N.,Rashtrasant Tukadoji Maharaj Nagpur University
Macroheterocycles | Year: 2013

A series of 7-o-β-D-glucopyranosyloxy-3-(disubstituted imidazol-2-yl)-4H-chromen-4-ones 5 was synthesized. The 7-hydroxy-3-formyl-4H-chromen-4-one 1 reacted with various 1,2-dicarbonyl compounds 2 in the presence of ammonium acetate to furnish 7-hydroxy-3-(4,5-disubstitutedimidazol-2-yl)-4H-chromen-4-ones 3, which on glucosylation with a-acetobromoglucose affords 2,3,4,6-tetra-o-acetyl-7-o-β-D-glucopyranosyloxy-3-(4,5-disubstituted imidazol-2-yl)-4H-chromen-4-ones 4. 7-o-/3-D-Glucopyranosyloxy-3-(4,5-disubstituted imidazol-2-yl)-4H-chromen-4-ones 5 were prepared by deacetylation with anhydrous zinc acetate in absolute methanol. Elemental analysis, IR,1H NMR, 13C NMR, EI-MS spectral data were obtained to determine the structure of the newly synthesized compounds. © ISUCT Publishing.


Hadda T.B.,University Mohammed Premier | Bendaha H.,University Mohammed Premier | Sheikh J.,Dhote Bandhu Science College | Ahmad M.,Quaid-i-Azam University | And 2 more authors.
Medicinal Chemistry Research | Year: 2014

A computation model has been developed for the rational design of bioactive pharmacophore sites as anti-Mycobacterium tuberculosis and anti-Trypanosoma cruzi (TC) candidates. The 40 compounds 1-40 analyzed have been previously screened for their antitubercular and antitrypanosomal activity. The highest anti-TC activity is obtained for compounds 8 and 18 which exhibited low IC50 values (9.2 and 10.8 μM), almost equal to clinical drug, nifurtimox (7.7 μM; 100% Inhib.). This could be attributed to the existence of two synergic (Oδ--Nδ-) and (Oδ--O δ-) antitrypanosomal pharmacophore sites. In contrast to compounds 8 and 18 which contain electroattractor groups (R1, R 2 = F), analog compounds 1 and 13 with electro-donor or only hydrogen (R1, R2 = CH3, H) show best antibacterial activity (MIC = 0.977 and 1.190 μg/mL) very close to antitubercular activity of Rifampicin (MIC = 0.125 μg/mL). This could be attributed to the existence of (Oδ--NHδ+) antibacterial pharmacophore site. © Springer Science+Business Media 2013.


Sheikh J.,Dhote Bandhu Science College | Hatzade K.,Dhote Bandhu Science College | Bader A.,University of Umm Al - Qura | Shaheen U.,University of Umm Al - Qura | And 2 more authors.
Medicinal Chemistry Research | Year: 2014

This paper reports the computational evaluation and experimental verification of 7-hydroxy-3-(1-phenyl-3-aryl-1H-pyrazol-5-yl)-4H-chromen-4-ones 3 and their o-β-d-glucopyranosides 5 for their antimicrobial and antioxidant activity. The prepared compounds were tested against various Gram-positive and Gram-negative bacteria species. Some of the synthesized compounds have shown potential antimicrobial and antioxidant activity. This POM bioinformatic study could greatly help to pharmacomodulate the potential antibiotics and antioxidants. Graphical Abstract: This paper describes the computational POM (Petra/Osiris/Molinspiration) evaluation and experimental verification of 7-o-β-d-glucopyranosyloxy-3-(1-phenyl-3-aryl-1H-pyrazol-5- yl)-4H-chromen-4-ones and metabolites for their antimicrobial and antioxidant activity. [Figure not available: see fulltext.] © 2013 Springer Science+Business Media New York.


Taile V.S.,Rashtrasant Tukadoji Maharaj Nagpur University | Ingle V.N.,Rashtrasant Tukadoji Maharaj Nagpur University | Hatzade K.M.,Rashtrasant Tukadoji Maharaj Nagpur University | Hatzade K.M.,Dhote Bandhu Science College
Journal of Carbohydrate Chemistry | Year: 2010

2-Amino-4-(4'-hydroxyphenyl) thiazole 1a was prepared from reaction between p-hydroxyacetophenone, thiourea, and iodine; compound 1a was treated with several (aryl/hetro aryl) aldehydes to form 2-(substituted benzylideneamino)-4- (4'-hydroxyphenyl) thiazoles 2a-j, which were glucosylated by using acetobromoglucose as a glucosyl donor to afford 2-(substituted benzylideneamino)-4-(2, 3, 4, 6-tetera-o-acetyl-4'-o-β-d-glucosidoxyphenyl) thiazoles 3a-j, which further on during deacetylation produced 2-(substituted benzylideneamino)-4-(4'-o-β-d-glucosidoxyphenyl) thiazoles 4a-j. These compounds were evaluated for biological activity, and their structure was confirmed by IR, NMR, mass spectra, elemental, and chemical analysis. Copyright © Taylor & Francis Group, LLC.


Juneja H.,Rashtrasant Tukadoji Maharaj Nagpur University | Panchbhai D.,Rashtrasant Tukadoji Maharaj Nagpur University | Sheikh J.,Rashtrasant Tukadoji Maharaj Nagpur University | Sheikh J.,Dhote Bandhu Science College | And 2 more authors.
Medicinal Chemistry Research | Year: 2014

This research article reports the synthesis of 4,6-bis(5-aryl/heteroaryl-1, 2-oxazol-3-yl)benzene-1,3-diol 4a-4f and 4,6-bis(5-aryl/heteroaryl-1H-pyrazol-3- yl)benzene-1,3-diol 5a-5f from 1,1′-(4,6-dihydroxybenzene-1,3-diyl)bis(3- aryl/heteroarylpropane-1,3-dione) 3a-3f. The compounds were fully characterized using spectroscopic analyses and tested for their antibacterial activity. A correlation of structure and activities relationship of these compounds with respect to molecular modeling, Lipinski rule of five, drug likeness, toxicity profiles, and other physico-chemical properties of drugs are described and verified experimentally. Graphical Abstract: This article reports the synthesis of bis-isoxazoles 4a-4f and bis-pyrazoles 5a-5f. A good correlation of structure and activities relationship of these compounds with respect to molecular modeling, Lipinski rule of five, drug likeness, toxicity profiles and other physico-chemical properties of drugs are described and verified experimentally.[Figure not available: see fulltext.] © 2013 Springer Science+Business Media New York.

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