Synthesis and Antimicrobial Activity of 3-(1,3,4-Oxadiazol-2-yl)quinazolin-4(3H)-ones

In attempt to find new pharmacologically active molecules, we report here the synthesis and in vitro antimicrobial activity of various 3-(1,3,4-oxadiazol-2-yl)-quinazolin-4(3H)-ones. The antimicrobial activity of title compounds were examined against two gram positive bacteria (S. aureus, S. pyogenes), two gram negative bacteria (E. coli, P. aeruginosa) and three fungi (C. albicans, A. niger, A. clavatus) using the broth microdilution method. Some derivatives bearing a bromo or iodo group exhibited very good antimicrobial activity

New 4-Thiazolidinones of Nicotinic Acid with 2-Amino-6-methylbenzothiazole and their Biological Activity

The title compounds 6a–j, 2-[(6-methyl-1,3-benzothiazol-2-yl)amino]-N-[2-(substituted phenyl/furan-2-yl)-4-oxo-1,3-thiazolidin-3-yl]nicotinamides, were prepared from 2-chloropyridine-3-carboxylic acid (1) and 2-amino-6-methyl-benzothiazole (2) by known methods. All the compounds have been established by IR, 1H NMR, 13C NMR and elemental analyses. The in vitro antimicrobial screening of the compounds were carried out against two Gram positive (S. aureus, S. pyogenes), two Gram negative (E. coli, P. aeruginosa) bacteria and three fungal species (C. albicans, A. niger, A. clavatus) using the broth microdilution method. Some of the compounds are comparable with standard drugs

PYRIMIDINE INCORPORATED SCHIFF BASE OF ISONIAZID WITH THEIR SYNTHESIS, CHARACTERIZATION AND IN VITRO BIOLOGICAL EVALUATION

  Objective: Versatile biological activities of nitrogen containing heterocycles in medicinal chemistry, mainly pyrimidine and pyridine ring based heterocyclic moieties are very important. Pharmaceutical important of pyrimidine and isoniazid moiety prompted us to synthesize isoniazid clubbed pyrimidine derivatives and evaluated for antimicrobial and antituberculosis activity.Method: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) have been synthesized by condensation reaction of 2-chloro-N-[4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl] acetamide and N'-[(E)- (3-bromophenyl) methylidene]pyridine-4-carbohydrazide. All newly synthesized compounds were screened for in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus pyogenes, antifungal against Candida albicans, Aspergillus niger, and Aspergillus clavatus, and antituberculosis activity against Mycobacterium tuberculosis H37RV.Results: Majority of the compounds exhibited good antibacterial, antifungal, and antituberculosis activity. All titled compounds were characterized by spectral analyses (infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectroscopy).Conclusion: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) showed good antimicrobial activity and comparatively good antituberculosis activity. Hence, all the compounds of this series considered for future investigation mainly in area of antibacterial, antifungal study

Electrical and Optical Characteristics of Indium Arsenide Junction Lasers

Electrical and light emission characteristics of pulsed InAs junction lasers were studied at various temperatures ranging from liquid helium temperature to room temperature. The junctions were prepared by vapor diffusing Zn into Sn doped n-type wafers of InAs, with a donor concentration of 1018cm-3. Data variation of capacitance with bias showed these to be abrupt junctions. At low injection currents, the current injection mechanism was determined to be photon-assisted tunneling. Gain and loss factors at 20.4°K were determined from the variation of threshold current with diode cavity length. An independent value of the gain factor was determined from the observed variation with current of the superradiantly narrowed line-width from a nonlasing structure. The time-resolved laser spectra shift to longer wavelengths with time during pulsed operation of the laser. The line shift results from joule heating of the diode, and follows the variation of bandgap of InAs with temperature. Mode confinement studies indicate that the mode confinement is due to the optical gain in the active region at the junction and that the active region extends to approximately a diffusion length on both sides of the junction

Editorial: Discovery and Development of Drugs for Neglected Diseases: Chagas Disease, Human African Trypanosomiasis, and Leishmaniasis

Twenty tropical diseases have been listed by the World Health Organization (WHO) as Neglected Tropical Diseases (NTDs). These tropical diseases are called “neglected” for three primary reasons: 1) These diseases are widespread worldwide among the economically weaker (neglected?) section of the society; 2) Although the total number of mortality, morbidity, disability, and health disparity caused annually by the NTDs is more than that attributed by the so-called elite diseases like cancer, diabetes, human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS), cardio- or neurological diseases but NTD patients do not receive comparable attention or treatment opportunities either from the governments or healthcare professionals or non-governmental organizations (NGOs); 3) The scope of drug development research in this field is minimal due to insufficient (negligible) funding, and pharma giants are not interested in developing effective drugs for NTDs on time, due to insignificant profit. It is highly challenging to develop new and novel drugs to combat these tropical diseases to upthrust the lifespan and lifestyle of the socioeconomically deprived people affected by NTDs (Figure 1). The major goal of this research topic is to shed light on the global scenario (current status of the ailments, treatment options, and recent drug development efforts) of three major NTDs, viz. Chagas disease (American trypanosomiasis), Human African trypanosomiasis (HAT), and Leishmaniasis. This research topic contains three reviews and seven research articles

Effect of metabolized polyethylene terephthalate, vacuum packaging and storage temperature on shelf life of papaya pulp Kalakand (Indian cookie)

The dairy plants are looking for newer products for diversification and value addition. There is scope for the dairy industry to introduce newer products as healthy, convenience and ready to eat foods for capacity utilization and value addition, but because of complex biochemical composition and high water content, milk and milk products act as an excellent culture medium for growth and multiplication of varieties of microorganisms. Vacuum packaging reduces product shrinkage, trim losses by eliminating oxidation and freezer burn resulting it can enhance product quality. Now a day metabolized polyethylene terephthalate (MET PET) with vacuum packaging have a promising role in storage of various value added milk product. The developed value added Kalakand product (Indian cookie) could be stored successfully for 5 days in MET PET packaging material at 4±1°C and when the product was packaged under vacuum the shelf life increased up to 10 days at 4±1°C

Study of biophysical properties, synthesis and biological evaluations of newer thiazolidine-2,4-dione conjugates

Thiazolidine-2,4-dione and its derivatives are acting as antimicrobial and antitubercular agents. Computational approach 2D-QSAR is used for prediction of antitubercular activity of the synthetic derivatives. 2D-QSAR generated model using PLSR method which predicted the statistically significant r2 = 0.3333, q2= 0.4000, pred_r2 = -1.9753 and F test = 3.0000. 2D-QSAR generated equation of pMICs is denoted the antitubercular activity correlated with thermodynamic descriptor T_2_2_O. Pharmacokinetic properties absorption, distribution, metabolism, excretion are also predicted which are useful for design the derivatives. A designed derivatives of (Z)-2-(5-substituted-2,4-dioxothiazolidin-3-yl)-N-(4-methoxy-6-methyl-1,3,5-triazin-2-yl)acetamide (C1-C10) are synthesized and spectrally characterized using IR, 1H NMR, 13C NMR and mass spectral data analysis as well as biologically evaluated against antitubercular and antimicrobial activities. From the biologically evaluated derivatives, compounds C1 and C4 were found to be active against the different antimicrobial species. Compounds C7 and C10 are more progressive than others against antitubercular species

Design, synthesis and antimicrobial activity of 4-thiazolidinonyl-quinazolin-4(3H)-ones of diclofenac analogue

A series of 7-chloro-3-(2-substituted phenyl-4-oxo-thiazolidin-3-yl)-2-[2-(2,6-dichlorophenyl) amino]benzyl-quinazolin-4(3H)-ones (5a-j) have been synthesized and characterized by elemental analyses as well as IR and NMR spectra. The Schiff bases 4a-j and 4-thiazolidinones 5a-j have been sceened for in vitro antimicrobial activity by cup-plate method. Compounds 4f, 4g, 4h, 5f, 5g and 5h possessed very good antibacterial as well as antifungal activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Heterosis in single cross inter and intra-specific hybrids of Desi cotton (Gossipium arboreum and G. herbaceaum) for their seed cotton yield, fibre quality and seed oil content

The present investigation was carried out to assess the expression of per se performance and heterotic effect for fibre quality and seed oil content besides seed cotton yield, studied involving ten desi cotton (Gossipium arboreum and G. herbaceaum) genotypes and their 45 cross combinations in half diallel analysis. F-1 hybrids GBhv-282 x G 27 (67.36%), GBhv- 287 x 824 (58.14%), GBhv- 282 x GAM- 173 (35.00%), GBhv- 286 x G 27 (20.50%), and GBhv- 283 x 824 (18.75%) recorded highest per se performance and significant positive standard heterosis while the maximum heterobeltiosis for seed cotton yield per plant was exhibited by the hybrid GBhv- 287 x 824(155.60 %) followed by GBhv- 282 x G 27 (151.29%) and GBhv- 282 x GAM- 173 (130.30%). Similar trend of heterosis for numbers of boll per plant were observed in above hybrids. For fibre quality traits none of the cross showed consistent high performance for all the characters. Cross GBhv- 283 x 824 was exhibited high standard heterosis for 2.5 % span length, fibre strength, fibre elongation percentage as well as for short fibre index (SFI) while cross GBhv- 286 x 824 were promising for 2.5 per cent span length, fibre strength and fibre fineness. In case of oil content intraarboreum crosses resulted as better crosses and among them cross combination 824 x GAM- 173 was best. Desi cotton hybrids are having lower fibre quality and yield. So, improvement for yield and fibre quality of diploid native varieties through heterosis breeding provided better hybrids for rainfed farming

Pyridine clubbed coumarin analogues: Their synthesis and biological studies as antimicrobials and antioxidants

1713-1720The major aim of this study is to develop the new class of coumarin candidate clubbed with dihydropyridine-3-carbonitrile with an improved potency as an antimicrobial and antioxidant agent. The key intermediate 6-nitro-4-methyl coumarin-yl chloro acetate 5 have been linked to the 6-(4-fluorophenyl)-2-oxo-4-phenyl-1,2-dihydro pyridine-3-carbonitrile IIa-j derivative to afford 4-methyl-6-nitro-2-oxo-2H-chromen-7-yl-2-(3-cyano-6-(4-fluoro phenyl)-4-(substituted-phenyl) pyridin-2-yl-oxy) acetates 7a-j via efficient organic transformations. All the new derivatives have been characterized by spectral studies (IR, 1H and 13C NMR and mass spectroscopy). In vitro antimicrobial activity have been carried out using the broth microdilution method and antioxidant potency using DPPH bioassays. Bioassay results reveal that compound 7e are equipotent against E. coli with MIC value 50 µg/ mL compared to standard drug ciprofoloxacin. A final analogue 7c with 4-chlorophenyl substituent indicated better antifungal potency against C. albicans with MIC value 100 µg/ mL compared to standard drug griseofulvin. In addition, newly synthesized analogues have been found to be significant scavengers of DPPH radical with IC50 values of 32.11 μg/mL. It has been observed that the potent antibacterial candidate has proved to possess significant antioxidant activity. The presence of chlorine and hydroxy group on phenyl ring plays an important role for the potency in above mentioned biological assay