Prva potpuna sinteza i biološko vrednovanje himenamida E

A new potent bioactive, proline-rich cyclic heptapeptide hymenamide E (13) was synthesized using the solution phase technique by cyclization of the linear peptide Boc-Phe-Pro-Thr-Thr-Pro-Tyr-Phe-OMe (12) after proper deprotection at carboxyl and amino terminals. Linear peptide segment was prepared by coupling the tripeptide unit Boc-Phe-Pro-Thr-OH (10a) with the tetrapeptide unit Thr-Pro-Tyr-Phe-OMe (11a) using dicyclohexylcarbodiimide as the coupling agent and N-methylmorpholine as the base. Structures of all new compounds were characterized by IR, 1H NMR spectral data as well as elemental analyses. In addition, the structure of compound 13 was verified by 13C NMR, fast atom bombardment mass spectroscopy and differential scanning calorimetry. The newly synthesized cyclopeptide was screened for its antibacterial, antifungal and anthelmintic activities against eight pathogenic microbes and two earthworm species. Compound 13 showed potent antifungal activity against Candida albicans and Ganoderma species comparable to that of griseofulvin as a reference drug and potent anthelmintic activity against earthworms Megascoplex konkanensis and Eudrilus species in comparison to piperazine citrate.Novi biološki aktivni ciklički heptapeptid himenamid E (13) sintetiziran je ciklizacijom linearnog peptida Boc-Phe-Pro-Thr-Thr-Pro-Tyr-Phe-OMe (12) nakon uklanjanja zaštitnih skupina sa C-terminalnih i N-terminalnih aminokiselina. Linearni peptidni segment pripravljen je spajanjem tripeptidne jedinice Boc-Phe-Pro-Thr-OH (10a) s tetrapeptidnom jedinicom Thr-Pro-Tyr-Phe-OMe (11a) u prisutnosti dicikloheksilkarbodiimida i N-metilmorfolina kao baze. Strukture novih spojeva potvrđene su IR i 1H NMR spektroskopijom i elementarnom analizom, a struktura spoja 13 i 13C NMR, spektroskopijom masa i diferencijalnom pretražnom kalorimetrijom. Novosintetizirani ciklopeptid testiran je na antibakterijsko, antifungalno i anthelmintičko djelovanje na osam patogenih mikroorganizama i dva parazita. Spoj 13 snažno djeluje antifungalno na gljivice Candida albicans i vrste Ganoderma i anthelmintički na nametnike Megascoplex konkanensis i vrste Eudrilus. Kao poredbene ljekovite tvari uporabljeni su grizeofulvin i piperazin citrat

Prva potpuna sinteza i biološko vrednovanje himenamida E

A new potent bioactive, proline-rich cyclic heptapeptide hymenamide E (13) was synthesized using the solution phase technique by cyclization of the linear peptide Boc-Phe-Pro-Thr-Thr-Pro-Tyr-Phe-OMe (12) after proper deprotection at carboxyl and amino terminals. Linear peptide segment was prepared by coupling the tripeptide unit Boc-Phe-Pro-Thr-OH (10a) with the tetrapeptide unit Thr-Pro-Tyr-Phe-OMe (11a) using dicyclohexylcarbodiimide as the coupling agent and N-methylmorpholine as the base. Structures of all new compounds were characterized by IR, 1H NMR spectral data as well as elemental analyses. In addition, the structure of compound 13 was verified by 13C NMR, fast atom bombardment mass spectroscopy and differential scanning calorimetry. The newly synthesized cyclopeptide was screened for its antibacterial, antifungal and anthelmintic activities against eight pathogenic microbes and two earthworm species. Compound 13 showed potent antifungal activity against Candida albicans and Ganoderma species comparable to that of griseofulvin as a reference drug and potent anthelmintic activity against earthworms Megascoplex konkanensis and Eudrilus species in comparison to piperazine citrate.Novi biološki aktivni ciklički heptapeptid himenamid E (13) sintetiziran je ciklizacijom linearnog peptida Boc-Phe-Pro-Thr-Thr-Pro-Tyr-Phe-OMe (12) nakon uklanjanja zaštitnih skupina sa C-terminalnih i N-terminalnih aminokiselina. Linearni peptidni segment pripravljen je spajanjem tripeptidne jedinice Boc-Phe-Pro-Thr-OH (10a) s tetrapeptidnom jedinicom Thr-Pro-Tyr-Phe-OMe (11a) u prisutnosti dicikloheksilkarbodiimida i N-metilmorfolina kao baze. Strukture novih spojeva potvrđene su IR i 1H NMR spektroskopijom i elementarnom analizom, a struktura spoja 13 i 13C NMR, spektroskopijom masa i diferencijalnom pretražnom kalorimetrijom. Novosintetizirani ciklopeptid testiran je na antibakterijsko, antifungalno i anthelmintičko djelovanje na osam patogenih mikroorganizama i dva parazita. Spoj 13 snažno djeluje antifungalno na gljivice Candida albicans i vrste Ganoderma i anthelmintički na nametnike Megascoplex konkanensis i vrste Eudrilus. Kao poredbene ljekovite tvari uporabljeni su grizeofulvin i piperazin citrat

Geospatial Technologies in the extraction of Groundwater Potential Zones

The utmost source which is contributing to the supply of water to the society is groundwater. Depletion of undergroundwater is enormously caused by eruptive growing rate of human population along with needs in the form of industrialand urbanized growth, indigent practices in irrigation methods and deforestation. As surface fresh water is very limit, waterdemand is drastically increasing for the needs. In this connection, there is immense predominant for the natural sourcecalled groundwater. It is mandatory for the communities not only to targeting the resource called groundwater but also toprovide remedial measures to replenishment the groundwater. Enormous investigations are in the process globally, to meetthe requirement to compensate resource for the needs in all aspects. Geospatial techniques are playing vital role in theextraction of groundwater resources by means of spatial and temporal data variations along with its integration analysis inthe form of separable layers to derive the solutions. In this connection, Nandyal mandal of Kurnool is selected to demarcatethe potential zones of groundwater by using this geospatial technology.The main motto of the research work is to identifythe effective potential groundwater zones by applying methodsand integration techniques of Geographic InformationSystem and remote sensing. This gives more information for the planning and management of the ground water.Byemploying geospatial technologies, the integrated composite output for potential zones is demarcated with help of keyparameters such as drainage, lineament, slope, geology, geomorphology, land use land cover and existing groundwaterlevels. All these thematic layers are extracted by using the satellite data and other available sources by using remote sensingand GIS. All these themes are demarcated using basic elements to identify the respective classes. Proper weightages areassignedtoeachclassofallthemesintheformofseparatecategorybasedonimportanceofweightagefromexcellenttopoor based on suitability to avail the groundwater sources. This process is applied for the considered themes and isreclassified based on results. It is then integrated with weighted overlay operation in ARCGIS environment. Appropriateweightage percentages which are equal to 100%, are given prior to overlay analysis of hydrology tools of ArcGIS. Variouszones like excellent, very good, good, moderate, poor are categorized for the integrated potential zones of groundwatersource. The use of suggested methodology is applied and demonstrated for a selected case study area in Nandyal Mandal ofKurnool District of Andhra Pradesh, India. Integrated output layout will be effectively useful in the demarcation of potentialresource zones. This demarcation area zone system is not only to identify the zones but also helpful in the replenishing theresources of the study area. The digital elevation model is also used to extract slope and drainage themes of the study area.The groundwater potential zones were obtained by overlaying all the thematic maps in terms of weighted overlay analysismethod using the spatial analysis tool in ArcGIS 10.1. This ground water potential information will be useful for effectiveidentificationofsuitablelocationsfor extractionofsuchgroundwater

In vitro incompatibility study of Valsartan and Hydrochlorothiazide by spectroscopic and RP-HPLC Method

1120-1127The present investigation is based on an in vitro incompatibility study between valsartan and hydrochlorothiazide by spectroscopic and reverse-phase high-pressure liquid chromatography (RP-HPLC) methods. The method has been developed and validated by ultraviolet (UV) spectroscopic method using methanol and water (1:4) as the solvent. The RP-HPLC study has been carried out using acetonitrile, methanol and 50 Mm phosphate buffer (20:50:30 %) adjusted to pH 3 with orthophosphoric acid. The methods show linearity at the concentration range of 1-5 μg/ml with correlation coefficient 0.9994 for valsartan and 0.9978 for hydrochlorothiazide in the concentration range of 1-5 μg/ml. Both the methods have shown a percentage relative standard deviation values less than 2. The in vitro incompatibility study has been carried out by UV-spectroscopic and RP-HPLC methods. The results of the study show that there is a change in the concentration level of both drugs in combination. The structure of the interacting compound has been determined by spectral analysis using IR, 1H NMR and LC-MS study. The spectral analysis confirms the formation of the new complex between valsartan and hydrochlorothiazide. The results obtained from the LC-MS study also correlate the reason behind an increase in the concentration of valsartan and decreases the concentration of hydrochlorothiazide during recovery study by spectroscopic and RP-HPLC method

2-[5-(4-Meth­oxy­phen­yl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-6-methyl-1,3-benzothia­zole

In the title compound, C24H21N3OS, the pyrazole ring makes dihedral angles of 5.40 (7) and 6.72 (8)° with the benzo[d]thiazole ring system and the benzene ring, respectively, and a dihedral angle of 85.72 (8)° with the meth­oxy-substituted benzene ring. In the crystal structure, the mol­ecules are linked by C—H⋯π inter­actions

Synthetic and biological studies on 5-(p-chlorophenyl)furan-2-carboxyl peptides and 4-[2'-(5'-formyl)furyl]benzoyl peptides

370-37

7-Chloro-3-phenyl­benzo[4,5]thia­zolo[2,3-c][1,2,4]triazole

In the title compound, C14H8ClN3S, the dihedral angle between the approximately planar triple-fused ring system (r.m.s. deviation = 0.065 Å) and the pendant phenyl ring is 62.25 (5)°. In the crystal, mol­ecules are linked into infinite chains along the c-axis direction by C—H⋯N hydrogen bonds. Aromatic π–π stacking inter­actions [centroid–centroid distances = 3.7499 (8) and 3.5644 (8) Å] and weak C—H⋯π inter­actions are also observed

1-(6-Fluoro-1,3-benzothia­zol-2-yl)-3-phenyl-1H-pyrazole-4-carbaldehyde

The asymmetric unit of the title compound, C17H10FN3OS, consists of two crystallographically independent mol­ecules. In one mol­ecule, the pyrazole ring makes dihedral angles of 6.51 (7) and 34.02 (9)°, respectively, with the terminal 1,3-benzothia­zole ring system and the phenyl ring, while in the other mol­ecule these values are 6.41 (8) and 23.06 (9)°. In the crystal, the molecules are linked by weak π–π [centroid–centroid distance = 3.7069 (10) Å] and C—H⋯π inter­actions