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Sahu P.K.,Jiwaji University | Sahu P.K.,Jagdishprasad Jhabarmal Tibrewala University | Lal J.,Jiwaji University | Thavaselvam D.,Defence Research & Development Establishment | Agarwal D.D.,Jagdishprasad Jhabarmal Tibrewala University
Medicinal Chemistry Research | Year: 2012

Aluminum trichloride acts as readily available, inexpensive, and efficient catalyst for one-pot three-component condensation reaction of aldehydes, dicarbonyl, and 2-Amino benzothiazole under the solvent-free conditions to afford the 4H-pyrimido[2,1-b][1,3]benzothiazole derivatives 4 with good yield. The compounds synthesized in this study were evaluated for their antibacterial activities against gram-positive and gram-negative bacteria, viz., Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus, and Providencia rettegeri. Compounds 4c, 4d, 4f, 4g, and 4h showed their good activities against tested bacterial species. Pyrimidine derivatives 4d, 4f, and 4g have shown good antifungal activities against tested fungal strains, such as Aspergillus niger, Aspergillus fumigates, Aspergillus flavus, etc. © Springer Science+Business Media, LLC 2011.

Sahu P.K.,Jiwaji University | Sahu P.K.,Jagdishprasad Jhabarmal Tibrewala University | Gupta S.K.,Jiwaji University | Thavaselvam D.,Defence Research & Development Establishment | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2012

A novel, one-pot, simple, efficient procedure for 4H-pyrimido[2,1-b] benzothiazole (4a-h), pyrazole (6a-d) and benzylidene (7a-d) derivatives of curcumin under solvent and solvent free conditions in microwave with good yield is have been synthesized. The synthesized compounds were evaluated for their antibacterial activity against gram-positive and gram-negative bacteria viz. Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Bacillus cereus and Providencia rettgeri and antifungal activity against fungi viz Aspergillus niger, Aspergillus fumigates, Aspergillus flavus. Detailed mechanistic study shows reaction proceeds through Knoevenagel type intermediate 3a which has been suggested as key intermediate for reaction (Fig. 3). © 2012 Elsevier Masson SAS. All rights reserved.

Goel A.K.,Defence Research & Development Establishment
Infection, genetics and evolution : journal of molecular epidemiology and evolutionary genetics in infectious diseases | Year: 2010

Cholera diarrhea is still a major health challenge for a large part of globe. Global replacement of Vibrio cholerae classical biotype by El Tor biotype, emergence of O139 serogroup and rapid spread of antibiotic resistant strains indicate the continuous evolution in V. cholerae. In this study, 114 V. cholerae O1 serotype Ogawa isolates, collected from different cholera outbreaks in different regions of India between 2004 and 2007 were subjected to biochemical, immunological and molecular characterization. All the isolates were PCR positive for various toxigenic, pathogenic and regulatory genes, viz. ompW, ctxB, rfbO1, tcp, zot, rtxC, ace, hlyA, ompU and toxR. The antibiogram studies of isolates revealed the resistance towards several antibiotics including nalidixic acid, co-trimoxazole, streptomycin, nitrofurantoin and polymyxin B. However, antibiogram of the strains confirmed susceptibility to tetracycline and chloramphenicol in all the isolates. This study also substantiated the wide spread of class 1 integrons and SXT elements (mobile genetic elements for antibiotic resistance) in clinical isolates in India. Sequencing of cholera toxin (ctxB) gene revealed the replacement of traditional ctxB of El Tor biotype with ctxB of classical biotype in all the O1 El Tor strains collected since 2004. In addition, in 2007, a new variant of O1 El Tor strain with further modifications in ctxB of classical biotype is discovered among the Indian isolates. Copyright 2009 Elsevier B.V. All rights reserved.

Thakur G.S.,Tropilite Foods Pvt. Ltd | Sharma R.,Tropilite Foods Pvt. Ltd | Sanodiya B.S.,Tropilite Foods Pvt. Ltd | Pandey M.,Xcelris Genomics | And 3 more authors.
Journal of Applied Pharmaceutical Science | Year: 2012

Gymnema sylvestre (Asclepiadaceae) also known as 'gurmar' or 'sugar destroyer' is a woody, climbing traditional medicinal herb which has many therapeutic applications in Ayurvedic system of medicine. It is used for lowering serum cholesterol, triglycerides and blood glucose level (hypoglycemic or antihyperglycemic), hypolipidaemic, weight loss, stomach ailments, constipation, water retention and liver diseases, either high or low blood pressure, tachycardia or arrhythmias, and used as aperitive, purgative, in eye troubles, antiinflammatory, smooth muscle relaxant, prevention of dental caries, cataract and as anticancer-cytotoxic agent. Its flowers, leaves, and fruits contains alkaloids, flavones, saponins, sapogenins, anthraquinones, hentri-acontane, pentatriacontane, a and ß-chlorophylls, phytin, resins, d-quercitol, tartaric acid, formic acid, butyric acid, lupeol, ß-amyrin related glycosides and stigmasterol having main principle bioactive compunds viz. gymnemic acids, gymnemasides, gymnemagenin, gurmarin, gymnemosides, gymnemanol, gymnemasins, gypenoside, and conduritol which act as therapeutic agent and play vital role in many therapeutic applications. Gymnemic acids are thought to be responsible for its antidiabetic activity and it is the major component of an extract shown to stimulate insulin release from the pancreas. Another anti-sweet agent gumarin is utilized as a pharmacological tool in the study of sweet-taste transduction. The commercial exploitation of this plant and their secondary metabolites are some of the major prospective of this rare medicinal herb. The focus of the present review is to achieve the potential of therapeutic value of this herb and mechanism and action of their secondary metabolites.

Afley P.,Defence Research & Development Establishment | Dohre S.K.,Defence Research & Development Establishment | Prasad G.B.K.S.,Jiwaji University | Kumar S.,Defence Research & Development Establishment
Applied Microbiology and Biotechnology | Year: 2015

Brucellae are Gram-negative intracellular bacteria that cause an important zoonotic disease called brucellosis. The animal vaccines are available but have disadvantage of causing abortions in a proportion of pregnant animals. The animal vaccines are also pathogenic to humans. Recent trend in vaccine design has shifted to epitope-based vaccines that are safe and specific. In this study, efforts were made to identify MHC-I- and MHC-II-restricted T cell epitopes of Brucella abortus and evaluate their vaccine potential in mice. The peptides were designed using online available immunoinformatics tools, and five MHC-I- and one MHC-II-restricted T cell peptides were selected on the basis of their ability to produce interferon gamma (IFN-γ) in in vivo studies. The selected peptides were co-administered with poly dl-lactide-co-glycolide (PLG) microparticles and evaluated for immunogenicity and protection in BALB/c mice. Mice immunized with peptides either entrapped in PLG microparticles (EPLG-Pep) or adsorbed on PLG particles (APLG-Pep) showed significantly higher splenocyte proliferation and IFN-γ generation to all selected peptides than the mice immunized with corresponding irrelevant peptides formulated PLG microparticles or phosphate-buffered saline (PBS). A significant protection compared to PBS control was also observed in EPLG-Pep and APLG-Pep groups. A plasmid DNA vaccine construct (pVaxPep) for peptides encoding DNA sequences was generated and injected to mice by in vivo electroporation. Significant protection was observed (1.66 protection units) when compared with PBS and empty vector control group animals. Overall, the MHC-I and MHC-II peptides identified in this study are immunogenic and protective in mouse model and support the feasibility of peptide-based vaccine for brucellosis. © 2015, Springer-Verlag Berlin Heidelberg.

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