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Shiroya U.,Lbrao Institute Of Pharmaceutical Education And Research | Patel M.N.,17 Gopi Park Society
International Journal of Pharmacy and Technology | Year: 2011

Coumarins are important class of compounds, isomeric to quinolones. They may become promising candidates for exploiting more useful therapeutically active molecules. DNA-gyrase has drawn much attention as selected target for finding potent anti-bacterial agents against multi-drug resistant strains such as methicillin-resistant Staphyloccus aureus (MRSA), vancomycin-resistant enterococci (VRE), penicillin-resistant Streptococci pneumonia (PRSP). The objective of the present study was, to study the molecular docking simulations on 5,7-dihydroxy-4-methyl coumarin analogues as probable candidates for inhibiting DNA gyrase subunit-B of S.aureus. In the present study, Docking simulations were carried out on the reported inhibitors of DNA-gyrase subunit A and B using docking software. Based on it, Series of 5,7-dihydroxy-4-methylcoumarin analogues (PH-1 to PH-9) were designed, synthesized, characterized and evaluated for its anti-bacterial activity against S.aureus and E.coli. Out of the nine test compounds, compound PH-4 showed good anti-bacterial activity against S.aureus and E.coli than rest of other compounds. The rational approach to lead discovery has prompted a better insight in developing a more specific 5,7-dihydroxy-4-methyl coumarin analogues as potential antibacterial agent. Source


Shiroya U.,17 Gopi Park Society | Shiroya U.,Lbrao Institute Of Pharmaceutical Education And Research | Patel M.,Lbrao Institute Of Pharmaceutical Education And Research
Medicinal Chemistry Research | Year: 2013

2-Quinolones are an important class of compounds, isomeric to 4-quinolones. They may become promising candidates for exploiting more useful therapeutically active molecules. DNA-gyrase has drawn much attention as a selected target for finding potent anti-bacterial agents against multi-drug resistant strains such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and penicillin-resistant Streptococci pneumonia. The objective of the present study was to study the molecular docking simulations on 2-quinolone analogs as probable candidates for inhibiting DNA gyrase subunit-B of S. aureus. In the present study, docking simulations were carried out on the reported inhibitors of DNA-gyrase subunit A and B using docking software. Based on it, series of 2-quinolone analogs (compound 1-8) were designed, synthesized, characterized, and evaluated for their anti-bacterial activity against S. aureus and E. coli. Out of the eight test compounds, compound-2 showed good anti-bacterial activity against S. aureus and E. coli as compared with the rest of the other compounds. The rational approach to lead discovery has prompted a better insight into developing more specific 2-quinolones as potential antibacterial agents. © 2013 Springer Science+Business Media New York. Source


Das S.K.,Lbrao Institute Of Pharmaceutical Education And Research | Dhake A.S.,Lbrao Institute Of Pharmaceutical Education And Research | Nayak A.,RRL IMMT | Das N.B.,RRL IMMT | Pandeya S.N.,KMIPS
Research Journal of Pharmacy and Technology | Year: 2011

Ammannia baccifera Linn, (family Lythraceae), traditionally it is used as cooling appetizer, rubifacient, laxative, stomachic, diuretic, aphrodisiac and lithotriptic also reported as posses antityphoid and antitubercular.The present study was investigated to evaluate in vitro antimicrobial activity of aqueous, methanolic, hexane extracts against bacteria Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus and against the fungi Candida albicans,Kluyuviromyces mamlamus.The pathogens were tested by disc diffusion assay method, and An attempt has been made to compare the activity of extracts with standard antibiotics against selected pathogen and all the extracts exhibited significant activity. © RJPT All right reserved. Source


Patel S.V.,Lbrao Institute Of Pharmaceutical Education And Research | Patel M.N.,Lbrao Institute Of Pharmaceutical Education And Research
International Journal of Pharmacy and Technology | Year: 2011

Heterobicyclic compounds are widely distributed in nature and exhibit variety of biological activities. They may become promising candidates for exploiting more useful therapeutically active molecules. The compounds having oxazolo pyrimidinone moiety are associated with interesting wide spectrum biological activities, such as kinase inhibition, adenosine receptor antagonism, antibacterial, tumour growth inhibition and some show to inhibit the ability of ricin to inactivate the ribosomes etc. The intermediate azlactones are also useful precursors for the synthesis of amino acids, peptides, heterocycles, biosensors and antitumor or antimicrobial compounds. In the present study, it was proposed to synthesize lead molecules of oxazolo pyrimidinone skeleton, apt for binding to the target enzyme, bacterial MurB based on the rational approach and to study their docking simulations using ArgusLab 4.0.1. Based on the above studies, an attempt was made to synthesize heterobicyclic 6,7-dihydrooxazolo[5,4-d]pyrimidin-5(4H)-one, parent molecule from Erlenmeyer-Plochl azlactone synthesis and its derivatives. Based on it, series of parent compound analogues were designed and synthesized. The synthesized test compounds were then characterized by TLC, melting point determination, IR, H-NMR and mass spectral studies and tested for their antibacterial activity against S.aureus and E.coli. Among all synthesized 8 test compounds, compound 7-(4-chlorophenyl)-2-(4-methoxyphenyl)-6,7-dihydrooxazolo[5,4-d]pyrimidin-5(4H)-one showed better activity against E.coli and compound 7-(4-chlorophenyl)-2-methyl-6,7-dihydrooxazolo[5,4-d]pyrimidin-5(4H)-one showed better activity against S.aureous than rest of the other test compounds. The rational approach to lead discovery has prompted a better insight in developing a more specific 6,7-dihydrooxazolo[5,4-d] pyrimidin-5(4H)-one analogues as potential antibacterial agent. Source


Poshiya A.,Shabri Apt | Poshiya A.,Lbrao Institute Of Pharmaceutical Education And Research | Patel M.N.,Shabri Apt | Patel M.N.,Lbrao Institute Of Pharmaceutical Education And Research
International Journal of Pharmacy and Technology | Year: 2011

The aim of the study was to perform the molecular docking simulations with the use of molecular modeling softwares on 7-hydroxy-4-methyl-2H-chromen-2-one analogues for finding probable candidates for inhibiting DNA gyrase subunit-B of S.aureus. Docking interaction of inhibitor candidates were studied by molecular modeling softwares. Using the in-silico approaches, the parent test compound 7-hydroxy-4-methyl-2H-chromen-2-one & its derivatives (CHR 1-8) were synthesized. All the test compounds were characterized by Thin layer chromatography, melting point determination, IR, 1H-NMR and mass spectral data. The biological activity was evaluated by determining antibacterial activity against S.aureus and E.coli strains of bacteria by using agar diffusion method. Source

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