Thiazolotriazoles As Anti-infectives: Design, Synthesis, Biological Evaluation and Studies.

The rational design of novel thiazolo[2,3-][1,2,4]triazole derivatives was carried out based on previously identified antitubercular hit molecule H127 for discovering potent compounds showing antimicrobial activity. The designed compounds were screened for their binding efficacies against the antibacterial drug target enoyl-[acyl-carrier-protein] reductase, followed by prediction of drug-likeness and ADME properties. The designed analogues were chemically synthesized, characterized by spectroscopic techniques, followed by evaluation of antimicrobial activity against bacterial and fungal strains, as well as antitubercular activity against and strains.

Lipase mediated new chemo-enzymatic synthesis of (RS)-, (R)-, and (S)-bunolol.

The β-adrenergic receptor blocking agents are an important class of drug molecules. The present study reports a new chemo and chemo-enzymatic synthetic process for (RS)-, (R)-, and (S)-bunolol, one of the potent β-adrenergic receptor blocker. In chemo-enzymatic process, CAL L4777 lipase was employed for enantioselective kinetic resolution to synthesize the enantiopure (R)-alcohol and (S)-ester from the corresponding racemic alcohol.

Gd2: A potential and novel isolate for fibrinolytic enzyme production.

The bacterium with an ability to produce extracellular fibrinolytic protease was isolated and identified as Gd2 based on ribotyping. The fibrinolytic profile of this enzyme depicted 73% of fibrin clot dissolution within 4 h. Fibrinolytic enzyme yield influenced by different physiological (incubation time, temperature, agitation and pH), nutritional (macronutrients such as carbon and nitrogen sources) and biological (inoculums age and inoculums concentration) parameters of fermentation which were optimized based on one-factor-at-a-time (OFAT) approach.

Mutanase Enzyme from RSP02: Characterization and Application as a Biocontrol Agent.

Mutanases are enzymes that have the ability to cleave α-1,3 linkages in glucan polymer. In the present investigation, mutanase enzyme purified from the culture filtrate of was evaluated for biofilm degradation and antimicrobial activity against pathogenic fungi along with enzyme kinetics, activation energies, pH and thermal stability. Biochemical and molecular characterization depicted that the enzyme showed optimum activity at pH 5.

Studies on wound healing potential of red pigment isolated from marine Bacterium sp.

Wounds are common clinical entities of life which may be subacute or acute. Wound healing is a complex biochemical process where the cell structures are restored to normalcy, which depend on cell proliferation and migration, basically fibroblast cell. The present investigation was undertaken to evaluate the healing efficacy of red pigment isolated from marine isolate sps on experimental wounds in albino rats.

Complete Genome Sequence of α-1,3-Glucanase-Producing Strain RSP-02.

A mutanase (α-1,3 glucanase)-producing bacterial strain of Paracoccus mutanolyticus was isolated from soil samples rich in cellulosic waste. Here, we report the whole-genome sequencing and annotation of P. mutanolyticus, which has a genome size of around 3.

Total syntheses of surinone B, alatanones A-B, and trineurone A.

The total syntheses of four polyketides, surinone B (1), alatanones A-B (2-3), and trineurone A (4) were accomplished through an efficient and unified strategy via one-pot C-acylation reaction coupling 1,3-cyclohexadiones with EDC-activated acids under mild conditions. Alatanone A (2) was found to be a potent anti-microbial agent against Gram-positive and Gram-negative bacteria with MIC 31.25 μg/ml while alatanone B (3) was found to be a potent anti-fungal agent against Cladosporium cladosporioides with MIC 62.

Synthesis of novel tetrazole containing hybrid ciprofloxacin and pipemidic acid analogues and preliminary biological evaluation of their antibacterial and antiproliferative activity.

A series of 1-substituted-1H-tetrazole-5-thiol building blocks were synthesized and introduced to the N-4 piperazinyl group at C-7 position of the quinolone core, and these novel compounds (5a-g and 8a-g) were screened for their antibacterial and antiproliferative activities. Bioactive assay studies manifested that most of new compounds exhibited significant antibacterial activity against the tested strains, including multi-drug-resistant MRSA in comparison with reference drugs ciprofloxacin, streptomycin B and pipemidic acid. Among the synthesized compounds, only ciprofloxacin (5a-g) derivatives displayed significant activity ([Formula: see text]) compared to reference drugs.

Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents.

A series of novel pyrazolyl alcohols (5a-h), pyrazolyl azides (6a-h), and pyrazolyltriazoles (8a-h, 10a-p and 12a-l) were prepared and evaluated for their bioactivity (anti-bacterial and anti-inflammatory) profile. The compound 5c displayed the potent anti-bacterial activity against Micrococcus luteus (MIC 3.9 and MBC 7.

Modelling of pretreatment and saccharification with different feedstocks and kinetic modeling of sorghum saccharification.

Experiments have been performed for pretreatment of sorghum, wheat straw and bamboo through high temperature alkali pretreatment with different alkaline loading and temperatures, and the data on extent of delignification in terms of the final compositions of cellulose, hemicellulose and lignin have been generated. Further, enzymatic saccharification has been carried out in all the cases to find the extent of conversion possible after 72h. The effect of different operating parameters on the extent of delignification and cellulose conversion are evaluated.

Synthesis, characterization and antimicrobial activity of novel Schiff base tethered boronate esters of 1,2-O-isopropylidene-α-d-xylofuranose.

A series of twenty one Schiff bases based on boronate ester of 1,2-O-isopropylidene-α-d-xylofuranose scaffold were designed and synthesized by condensation of formyl or amino phenyl boronate esters with substituted anilines or 2-hydroxybenzaldehydes, respectively. All the imines are remarkably stable crystalline solids and were obtained in good yields. All the products were fully characterized by FT-IR, multinuclear NMR ((1)H, (13)C and (11)B) spectroscopy, and elemental analysis.

Synthesis and biological evaluation of novel tamoxifen-1,2,4-triazole conjugates.

A new class of compounds, structurally related to the breast cancer drug tamoxifen, was designed and synthesized. The McMurry coupling reaction was used as the key synthetic step in the preparation of these analogs, and the structural assignments were made on the basis of [Formula: see text] NMR, [Formula: see text] NMR, and HRMS studies. The absolute stereochemistry of E and Z isomers was unambiguously confirmed by a single-crystal X-ray diffraction analysis.

High yield expression of novel glutaminase free L-asparaginase II of Pectobacterium carotovorum MTCC 1428 in Bacillus subtilis WB800N.

Gene encoding glutaminase-free L-asparaginase II (ans B2) from Pectobacterium carotovorum MTCC 1428 was cloned into pHT43, transformed in Bacillus subtilis WB800N and optimised the expression levels of recombinant enzyme. A three-fold higher enzyme production was observed with an efficient transformant as compared to native strain. Enzyme localization studies revealed that >90% of recombinant enzyme is secreted extracellularly, a little fraction is attached to the membrane (>6%) and localised intracellularly (3%).

Fermentative Production of Pyranone Derivate I from Marine Vibrio sp. SKMARSP9: Isolation, Characterization and Bioactivity Evaluation.

Pyranone derivative I was isolated from fermented broth of isolated marine bacterial strain Vibrio sp. SKMARSP9. The compound I was characterized, and evaluated for its antimicrobial properties.

Isolation, semi-synthesis and bio-evaluation of spatane derivatives from the brown algae Stoechospermum marginatum.

A comprehensive investigation of chemical constituents from brown algae Stoechospermum marginatum yielded ten known spatane compounds (1-10). To develop the compound libraries on these scaffolds, a series of semi synthetic derivatives was prepared (1a-1d, 2a, 4a, 11 and 12) and investigated for their anti-microbial and anticancer activities. The results indicated that compounds 2a, 4, 1b and 4a exhibited potent cytotoxic activities against B16F10 cancer cell line with IC50 values of 3.

Production and Characterization of Protein Encapsulated Silver Nanoparticles by Marine Isolate Streptomyces parvulus SSNP11.

Production of protein encapsulated silver nanoparticles (AgNPs) assisted by marine actinomycetes strain has been investigated. The selective isolate was identified as Streptomyces parvulus SSNP11 based on chemotaxonomic and 16S rRNA analysis. Maximum AgNPs production was observed within 24 h incubation time.

Intensification of Fructosyltransferases and Fructo-Oligosaccharides Production in Solid State Fermentation by Aspergillus awamori GHRTS.

The present work was aimed to investigate the impact of the solid substrates mixture on Fructosyltransferases (FTase) and Fructo-oligosaccharides (FOS) production. An augmented simplex lattice design was used to optimize a three component mixture for FTase production. Among selected substrates corn cobs has highest impact on FTase production followed by wheat bran and rice bran.

Biosynthesis of xylobiose: a strategic way to enrich the value of oil palm empty fruit bunch fiber.

Xylooligosaccharides are functional foods mainly produced during the hydrolysis of xylan by physical, chemical, or enzymatic methods. In this study, production of xylobiose was investigated using oil palm empty fruit bunch fiber (OPEFB) as a source material, by chemical and enzymatic methods. Xylanase-specific xylan hydrolysis followed by xylobiose production was observed.

Characterization of silver nanoparticles synthesized by using marine isolate Streptomyces albidoflavus.

Silver nanoparticles production by the green chemistry approach was investigated using an isolated marine actinomycetes strain. The isolated strain was identified as Streptomyces albidoflavus based on chemotaxonomic and ribotyping properties. The strain revealed production of silver nanoparticles both extracellular and intracellularly.

Laccase- and peroxidase-free tyrosinase production by isolated microbial strain.

Laccase- and peroxidase-free tyrosinase has commercial importance in the production of L-3, 4-dihydroxyphenylalanine (L-DOPA), which is mainly used in the treatment of Parkinson's disease. In the present study, isolation of an actinomycetes microbial strain capable of producing only tyrosinase is reported. Among all soil isolates, three individual colonies revealed black color around the colony in the presence of tyrosine.

Biohydrogen production process optimization using anaerobic mixed consortia: a prelude study for use of agro-industrial material hydrolysate as substrate.

Efficient biohydrogen production from lignocellulosic hydrolysate assumes considerable practical and academic importance. The impact of glucose to xylose ratio, medium pH, inoculum size and age on biohydrogen production indicated that glucose to xylose ratio is the critical parameter for effective H(2) production compared to either pure glucose or xylose as carbon source. Inoculum size and its age contributed more than 70% to overall H(2) production and revealed significance at individual as well as interactive level.

Development of balanced medium composition for improved rifamycin B production by isolated Amycolatopsis sp. RSP-3.

Aim: To develop optimum fermentation environment for enhanced rifamycin B production by isolated Amycolatopsis sp. RSP-3.

Methods And Results: The impact of different fermentation parameters on rifamycin B production by isolated Amycolatopsis sp.

Nickel-impregnated silica nanoparticle synthesis and their evaluation for biocatalyst immobilization.

In the present investigation, impact of nickel-impregnated silica paramagnetic particles (NSP) as biocatalyst immobilization matrices was investigated. These nanoparticles were synthesized by sol-gel route using a nonionic surfactant block co polymer [poly (ethylene glycol)-block-poly-(propylene glycol)-block-poly (ethylene glycol)]. Diastase enzyme was immobilized on these particles (enzyme-impregnated NSP) as model enzyme and characterized using Fourier-transform infrared spectroscopy and X-ray crystallography.

Evaluation of antineoplastic activity of extracellular asparaginase produced by isolated Bacillus circulans.

L-Asparaginase is an important component in the treatment of acute lymphoblastic leukemia in children. Its antineoplastic activity toward malignant cells is due to their characteristic nature in slow synthesis of L-asparagine (Asn), which causes starvation for this amino acid, while normal cells are protected from Asn starvation due to their ability to produce this amino acid. The relative selectivity with regard to the metabolism of malignant cells forces to look for novel asparaginase with little glutaminase-producing systems compared to existing enzyme.