Structure-activity relationship of pyrazolo pyrimidine derivatives as inhibitors of mitotic kinesin Eg5 and anticancer agents.

Human kinesin Eg5 is a potential inhibiting site for cancer chemotherapy. Blocking metaphase by binding foreign inhibitors with Eg5 eventually leads to apoptotic cell death. Here, we report the pyrazolopyrimidine derivates as potent inhibitors of Eg5 that prevents mitotic kinesin progression.

Dihydroactinidiolide, a natural product against Aβ induced toxicity in Neuro2a cells: Synthesis, in silico and in vitro studies.

Synthesis of natural products has speeded up drug discovery process by minimizing the time for their purification from natural source. Several diseases like Alzheimer's disease (AD) demand exploring multi targeted drug candidates, and for the first time we report the multi AD target inhibitory potential of synthesized dihydroactinidiolide (DA). Though the activity of DA in several solvent extracts have been proved to possess free radical scavenging, anti bacterial and anti cancer activities, its neuroprotective efficacy has not been evidenced yet.

Synthesis of N-(1-(6-acetamido-5-phenylpyrimidin-4-yl) piperidin-3-yl) amide derivatives as potential inhibitors for mitotic kinesin spindle protein.

Kinesin Spindle Protein (KSP) or Eg5 is an essential kinesin that is involved in spindle separation process during mitosis and also unregulated in certain cancer cells. Inhibitors of this enzyme have proved to be effective to block spindle separation followed by mitotic arrest and apoptosis of the cancer cells. Since this enzyme has two allosteric inhibitor binding sites, it's an excellent target for developing drugs for cancer chemotherapy.

Improved conductivity and antibacterial activity of poly(2-aminothiophenol)-silver nanocomposite against human pathogens.

A rapid and simple chemical synthesis of poly(2-aminothiophenol)‑silver (P2ATP-Ag) nanocomposite using conductive and electroactive silver nanoparticles (AgNPs) is reported. The AgNPs was synthesized by chemical reduction method using tri‑sodium citrate as reducing agent and poly(N-vinyl-2-pyrrolidone) (PVP) as stabilizing agent. P2ATP-Ag nanocomposite was synthesized by using potassium peroxodisulphate as oxidant and the samples were characterized.

A highly sensitive electrochemical biosensor for catechol using conducting polymer reduced graphene oxide-metal oxide enzyme modified electrode.

The fabrication, characterization and analytical performances were investigated for a catechol biosensor, based on the PEDOT-rGO-Fe2O3-PPO composite modified glassy carbon (GC) electrode. The graphene oxide (GO) doped conducting polymer poly (3,4-ethylenedioxythiophene) (PEDOT) was prepared through electrochemical polymerization by potential cycling. Reduction of PEDOT-GO was carried out by amperometric method.

Nanomaterials for Electrochemical Sensing and Decontamination of Pesticides.

We are all aware of growing environmental concerns, and the need to provide new and improved means for maintaining a healthy environment. Pesticides are the only toxic chemicals released intentionally into the environment to kill living organisms. Pesticide detection and destruction has become a very important and inevitable area of research because of the rapid expansion of agriculture and stringent environmental protection acts.

Synthesis of mononuclear copper(II) complexes of acyclic Schiff's base ligands: spectral, structural, electrochemical, antibacterial, DNA binding and cleavage activity.

The mononuclear copper(II) complexes (1&2) of ligands L(1) [N,N'-bis(2-hydroxy-5-methylbenzyl)-1,4-bis(3-iminopropyl)piperazine] or L(2) [N,N'-bis(2-hydroxy-5-bromobenzyl)-1,4-bis(3-iminopropyl) piperazine] have been synthesized and characterised. The single crystal X-ray study had shown that ligands L(1) and L(2) crystallize in a monoclinic crystal system with P21/c space group. The mononuclear copper(II) complexes show one quasireversible cyclic voltammetric response near cathodic region (-0.

Ethyl 3-(4-chloro-phen-yl)-2-phenyl-3-(4-phenyl-1,2,3-selena-diazol-5-yl)propano-ate.

In the title compound, C25H21ClN2O2Se, the selena-diazole ring is almost planar [maximum deviation = 0.004 (2) Å], and the adjacent benzene ring is twisted by 50.6 (1)° with respect to this ring.

A kinetic study on the formation of poly(4 aminodiphenylamine)/copper nanocomposite using UV-visible spectroscopy.

The course of the reaction between copper sulfate (CuSO4) and 4-aminodiphenylamine (4ADPA) was monitored by UV-visible spectroscopy in p-toluene sulfonic acid (p-TSA). Formation of poly(4-aminodiphenylamine)/copper nanoparticle composite (P4ADPA/CuNC) was witnessed through the steady increase in absorbance at 410, 580 and >700 nm. The absorbance at 410 nm as well as >700 nm are correlated to the amount of P4ADPA/CuNC formation and was subsequently used to determine the rate of formation of P4ADPA/CuNC (RP4ADPA/CuNC) at any time during the course of the reaction.

5-[1-(4-Methyl-phen-yl)-2-nitro-but-yl]-4-phenyl-1,2,3-selenadiazole.

In the title compound, C19H19N3O2Se, the selenadiazole ring is roughly planar [maximum deviation 0.033 (6) Å]. The attached phenyl ring is twisted away at an angle of 47.

4-(5-Chloro-thio-phen-2-yl)-1,2,3-selenadiazole.

In the title compound, C6H3ClN2SSe, the selenadiazole and chloro-thio-phene rings are almost coplanar [dihedral angle = 5.24 (15)°]. In the crystal, C-H⋯N inter-actions link the mol-ecules into chains extending along the b-axis direction.

Ethyl 3-(4-meth-oxy-phen-yl)-2-phenyl-3-(4-phenyl-1,2,3-selenadiazol-5-yl)propano-ate.

In the title compound, C(26)H(24)N(2)O(3)Se, the selenadiazole ring is planar [maximum deviation = 0.002 (2) Å]. The dihedral angle between the selenadiazole ring and the attached phenyl ring is 49.

5-[1-(4-Meth-oxy-phen-yl)-2-nitro-but-yl]-4-phenyl-1,2,3-selenadiazole.

In the title compound, C(19)H(19)N(3)O(3)Se, the selenadiazole ring is essentially planar (r.m.s.

Evaluation of the individuality of white rot macro fungus for the decolorization of synthetic dye.

Introduction: A biosorbent was developed by simple dried Agaricus bisporus (SDAB) and effectively used for the biosorption of cationic dyes, Crystal Violet and Brilliant Green.

Materials And Methods: For the evaluation of the biosorbent system, all the batch equilibrium parameters like pH, biomass dose, contact time, and temperature were optimized to determine the decolorization efficiency of the biosorbent. The maximum yields of dye removal were achieved at pH 4.

5-(2-Nitro-1-phenyl-but-yl)-4-phenyl-1,2,3-selenadiazole.

In the title compound, C(18)H(17)N(3)O(2)Se, the selenadiazole ring is planar [maximum deviation = 0.012 (2) Å for the ring C atom bearing the phenyl substituent]. The dihedral angle between the selenadiazole ring and the attached benzene ring is 46.

1-(2-Naphth-yl)-3-phenyl-3-(4,5,6,7-tetra-hydro-1,2,3-benzoselenadiazol-4-yl)propan-1-one.

In the title compound, C(25)H(22)N(2)OSe, the fused six-membered cyclo-hexene ring of the 4,5,6,7-tetra-hydro-1,2,3-benzoselenadiazole group adopts a near half-chair conformation and the five-membered 1,2,3-selenadiazole ring is essentially planar (r.m.s.

A facile synthesis of carbocycle-fused mono and bis-1,2,3-selenadiazoles and their antimicrobial and antimycobacterial studies.

A series of mono and bis-1,2,3-selenadiazole derivatives have been synthesized by the oxidative cyclization of mono and bis semicarbazones of 2-(3-oxo-1,3-diarylpropyl)-1-cyclohexanones using selenium(IV) oxide. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 11632) and Candida albicans (ATCC 90028) and in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB). Among these compounds, 1,3-di(4-chlorophenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2h) and 3-(4-chlorophenyl)-1-(4-methylphenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2g) were found to be the most active compounds with MIC of 3.

Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies.

A series of 3-heteroarylthioquinoline derivatives has been synthesized by the Friedlander annulation of 2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]-1-aryl-1-ethanone/2-(1,3-benzothiazol-2-ylsulfanyl)-1-aryl-1-ethanone/1-aryl-2-[(2-phenyl-2H-1,2,3,4-tetraazol-5-yl)sulfanyl]-1-ethanone with 2-aminobenzophenone in good yields using YbCl(3) as the catalyst. These compounds have been screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) and among the 21 compounds screened, 2-[2-(4-bromophenyl)-4-phenyl-3-quinolyl]sulfanyl-5-methyl-1,3,4-thiadiazole (5d) and 2-[2-(4-chlorophenyl)-4-phenyl-3-quinolyl]sulfanyl-5-methyl-1,3,4-thiadiazole (5c) were found to be the most active compounds with MIC of 3.2 and 3.

3-(4-Methyl-phen-yl)-1-phenyl-3-(4,5,6,7-tetra-hydro-1,2,3-benzoselenadiazol-4-yl)propan-1-one.

In the title compound, C(22)H(22)N(2)OSe, the fused six-membered ring of the 4,5,6,7-tetra-hydro-benzo[d][1,2,3] selenadiazole group adopts a near to envelope (E form) conformation and the five-membered 1,2,3-selenadiazole ring is essentially planar (r.m.s.

Biofilm formation by Streptococcus pyogenes: modulation of exopolysaccharide by fluoroquinolone derivatives.

Biofilm formation by Streptococcus pyogenes has been demonstrated as a potentially important mechanism contributing to antibiotic treatment failure. S. pyogenes is the frequent cause of purulent infections in humans and also, it could play a significant role in recurrent and chronic infections.

4-{(4-Chloro-phen-yl)[4-(4-methyl-phen-yl)-1,2,3-selenadiazol-5-yl]meth-yl}-4,5,6,7-tetra-hydro-1,2,3-benzoselenadiazole.

In the title compound, C(22)H(19)ClN(4)Se(2), the mean plane of the non-fused selenadiazole ring forms dihedral angles of 54.20 (16)° and 70.48 (11)°, respectively, with the essentially planar [maximum deviations of 0.

Course of poly(4-aminodiphenylamine)/Ag nanocomposite formation through UV-vis spectroscopy.

Kinetics of chemical oxidative polymerization of 4-aminodiphenylamine (4ADPA) was followed in aqueous 1 M p-toluene sulfonic acid (p-TSA) using silver nitrate (AgNO3) as an oxidant by UV-vis spectroscopy. The medium was found to be clear and homogeneous during the course of polymerization. The absorbances corresponding to the intermediate and the polymer were followed for different concentrations of 4ADPA and AgNO3 and at different reaction time.

Large-scale preparation of polyaniline nanospheres anchored with thiol-stabilized gold nanoparticles.

Reported herein is the preparation of a new nanostructured composite consisting of PANI(SH) (where PANI(SH) is poly(aniline-co-4-aminothio phenol)) and gold nanoparticles (AuNPs)) via "seed"-induced bulk polymerization. The PANI(SH)-AuNPs composite was designated as PANI(SH)-Au-NS(P). The composite was characterized in terms of its morphology and structural, thermal, and electrochemical properties.

Spectral Analysis and Crystal Structures of 4-(4-Methylphenyl)-6-Phenyl-2,3,3a, 4-Tetrahydro-1H-Pyrido[3,2,1-jk]Carbazole and 4-(4-Methoxyphenyl)-6-Phenyl-2,3,3a, 4-Tetrahydro-1H-Pyrido[3,2,1-jk]Carbazole.

The crystal structures of 4-(4-methylphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIa) and 4-(4-methoxyphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIb) were elucidated by single crystal X-ray diffraction. Compound (IIa), C28H25N, crystallizes in the triclinic system, space group P-1, with a = 8.936(2) Å, b = 10.

Preparation of poly(1,5 diamino naphthalene) nanobelts/nanodiscs through a "hard-soft combined templates" approach.

This is the first report on the preparation of nanobelts/nanodiscs of poly(1,5-diamino naphthalene) (PDAN-P) in bulk quantities through a "hard-soft combined templates" approach. PDAN was nanostructured within the channels of MCM-41 (hard template) in the presence of beta-napthalene sulfonic acid (beta-NSA) (soft template) and further used as the seed for the bulk preparation of pure PDAN nanobelts/nanodiscs of PDAN (PDAN-P). Field emision scanning electron microscope image reveals that a typical nanobelt has a length of approximately 3 microm, with a uniform breadth of approximately 150 nm and a thickness of approximately 50 nm.