An Update on Synthesis of Coumarin Sulfonamides as Enzyme Inhibitors and Anticancer Agents

Coumarin is an important six-membered aromatic heterocyclic pharmacophore, widely distributed in natural products and synthetic molecules. The versatile and unique features of coumarin nucleus, in combination with privileged sulfonamide moiety, have enhanced the broad spectrum of biological activities. The research and development of coumarin, sulfonamide-based pharmacology, and medicinal chemistry have become active topics, and attracted the attention of medicinal chemists, pharmacists, and synthetic chemists. Coumarin sulfonamide compounds and analogs as clinical drugs have been used to cure various diseases with high therapeutic potency, which have shown their enormous development value. The diversified and wide array of biological activities such as anticancer, antibacterial, anti-fungal, antioxidant and anti-viral, etc. were displayed by diversified coumarin sulfonamides. The present systematic and comprehensive review in the current developments of synthesis and the medicinal chemistry of coumarin sulfonamide-based scaffolds give a whole range of therapeutics, especially in the field of oncology and carbonic anhydrase inhibitors. In the present review, various synthetic approaches, strategies, and methodologies involving effect of catalysts, the change of substrates, and the employment of various synthetic reaction conditions to obtain high yields is cited.     

Dosimetric characteristics of aqueous solution of crystal violet for applications in food irradiation

Aqueous solution of crystal violet has been evaluated spectrophotometrically as a gamma-ray chemical dosimeter. The response of the chemical dosimetric system has also been investigated under different environmental conditions, such as light and temperature. In the present study the response has been measured at two wavelengths; 588 nm (λ_max of the irradiated solution) and 500 nm. The response of the crystal violet dosimeter was linear in the dose range of 50–550 Gy at pH 5.6 when absorption measurements were made at 588 and 500 nm. The response of the crystal violet dosimeter during post-irradiation storage at room temperature in dark showed slight decrease in absorbance at 588 and 510 nm but the response was almost stable at 460 nm. For higher doses, the change in the response was greater as compared to the low doses. Post-irradiation stability during diffused sunlight showed significant decrease in the response for higher dose at 588 and 510 nm and slower decrease in the response for lower dose at the above mentioned wavelengths. However the response was almost stable up to 97 days at 460 nm for higher and lower doses. At 4 °C, the decrease in the absorbance was slower at 588 and 510 nm while the response was almost constant at 460 nm. At higher temperatures, such as 40 °C, the decrease in the absorbance was greater at 588 and 510 nm while at 460 nm the absorbance was almost constant for about 3 months.     

Enhanced infrared transmission through subwavelength coaxial metallic arrays

We report the observation of enhanced near-infrared transmission through arrays of subwavelength coaxial metallic structures compared with that through comparable diameter hole arrays as a result of localized electromagnetic modes supported by the complex coaxial unit cell. Polarization and angle-dependent transmission measurements clearly demonstrate the coupling between this localized mode and delocalized surface plasmon modes. A generalized, multiple discrete states Fano line shape provides a good fit to the experimental results.     

Synthesis,Spectroscopy, Semi‐empirical and Biological Activities of Organotin(IV) Complexes with o‐Isopropyl Carbonodithioic Acid

New organotin(IV) complexes have been synthesized by treating potassium o‐isopropyl carbonodithioate with R₂SnCl₂/R₃SnCl in 1 : 2/1 : 1 M/L ratio. All complexes have been characterized by IR and NMR (¹H, ¹³C) spectroscopy. IR results shows that ligand acts as bidentate which is also confirmed by semi‐empirical study. NMR data reveals four coordinated geometry in solution. Computed positive heat of formation shows that complex 5 is thermodynamically unstable. UV/visible spectroscopy was used to assess the mode of interaction and binding of the complexes with DNA which shows that complex 5 exhibits higher binding constant as compared to complex 3 . In protein kinase inhibition assay, compound 3 was found most active, while other biological activities shows that triorganotin(IV) complexes are biologically more active as compared to diorganotin(IV) complexes.     

Some fixed point theorems in convex metric spaces

The concept of a convex metric space was introduced by Takahashi [10]. He observed that it is possible to generalize fixed point theorems in Banach spaces. Subsequently, Machado [8], Itoh [5], Naimpally, Singh and Whitfield [9] and Beg and Azam [2], among others have studied fixed point theorems in convex metric spaces. This paper is a continuation of these investigations.     

Cytotoxic flavonoids from two Lonchocarpus species

A new isoflavone, 4′-prenyloxyvigvexin A (1) and a new pterocarpan, (6aR,11aR)-3,8-dimethoxybitucarpin B (2) were isolated from the leaves of Lonchocarpus bussei and the stem bark of Lonchocarpus eriocalyx, respectively. The extract of L. bussei also gave four known isoflavones, maximaisoflavone H, 7,2′-dimethoxy-3′,4′-methylenedioxyisoflavone, 6,7,3′-trimethoxy-4′,5′-methylenedioxyisoflavone, durmillone; a chalcone, 4-hydroxylonchocarpin; a geranylated phenylpropanol, colenemol; and two known pterocarpans, (6aR,11aR)-maackiain and (6aR,11aR)-edunol. (6aR,11aR)-Edunol was also isolated from the stem bark of L. eriocalyx. The structures of the isolated compounds were elucidated by spectroscopy. The cytotoxicity of the compounds was tested by resazurin assay using drug-sensitive and multidrug-resistant cancer cell lines. Significant antiproliferative effects with IC₅₀ values below 10 μM were observed for the isoflavones 6,7,3′-trimethoxy-4′,5′-methylenedioxyisoflavone and durmillone against leukemia CCRF-CEM cells; for the chalcone, 4-hydroxylonchocarpin and durmillone against its resistant counterpart CEM/ADR5000 cells; as well as for durmillone against the resistant breast adenocarcinoma MDA-MB231/BCRP cells and resistant gliobastoma U87MG.ΔEGFR cells.     

Facile LC‐UV methods for simultaneous monitoring of ciprofloxacin and rosuvastatin in API,formulations and human serum

An efficient, selective and cost‐effective liquid chromatographic assay was developed and validated for the simultaneous quantification of ciprofloxacin and rosuvastatin in Active Pharmaceutical Ingredients (API), pharmaceutical formulations and in human serum. The chromatographic system consisted of mobile phase methanol–water, 90:10 v/v at pH 3.0 adjusted with o‐phosphoric acid, pumped at 1.0 mL/min through a prepacked Purospher Star C18 (5 µm, 25 × 0.46 cm) column and effluent was monitored at the isosbestic point (255 nm) as well as at the λ_max of individual drugs (243 and 271 nm). The method was validated over a linear concentration range of 0.25–15 µg/mL for ciprofloxacin and 0.33–20 µg/mL for rosuvastatin (r² ≥ 0.999). The ranges of reliable response (limits of detection and quantitation) for ciprofloxacin were 3–15 and 9–45 ng/mL and 17–29 and 52–88 ng/mL, respectively, for rosuvastatin in all API, pharmaceutical formulations and human serum. Analytical recovery from human serum was >98% and relative standard deviation (RSD) was <2. The accuracies were 97.13–102.55 and 97.41–101.31% and precisions in RSD were 0.04–1.90 and 0.02–1.23% for ciprofloxacin and rosuvastatin, respectively. No matrix interferences, ion suppression/enhancement and carry‐over were detected. The total assay run time was less than 5 min. In another study, for optimum performance the detector was programmed for multiwavelength scanning at the absorption maxima of each component. Consequently, the linearity range was improved and limit of detection and quantitation values were down to 1–4 and 4–12 ng/mL for ciprofloxacin and 3–5 and 9–15 ng/mL for rosuvastatin, respectively. The validation parameters fitted ICH guidelines through the isosbestic and individual λ_max approach. The small sample volume and simplicity of preparation make this method suitable for use in human serum samples, pharmaceutical formulations, quality control, drug–drug interaction studies, clinical laboratories, drug research centers and forensic medical centers. Copyright © 2014 John Wiley & Sons, Ltd.     

Optimization of process parameters and its effect on structure and morphology of CuO nanoparticle synthesized via the sol−gel technique

This article describes systematic basic research on the optimization of the processing parameters of sol?gel technique for synthesis of the high purity CuO nanoparticles. Effect of the synthesis parameters such as copper salt concentration, solvent and gelating agent, optimized one at a time, was investigated by employing XRD, TEM, FESEM, micro-Raman, UV-visible-NIR and PL spectroscopies. XRD results clearly demonstrate the monoclinic structure of CuO nanoparticles with traceable impurities at a lower molar concentration of Cu²⁺, transition of nucleation system from homogeneous to heterogeneous state with the increase in concentration of Cu²⁺ from 0.05 to 0.15?M. It was also found that the isopropyl alcohol offers better results in comparison to ethanol and water. Moreover, the lattice parameters, space group, and crystal system were determined by powder X-ray diffraction method. Further we propose the optimization of synthesis process using ethylene glycol and citric acid (EG:CA). The Raman analysis confirmed the influence of ethylene glycol and citric acid ratio and TEM observations confirmed that EG:CA 1:2 ratio formulate homogenous flower-like nanostructures. The optical absorption of CuO nanostructures can be easily tuned by varying the concentration of citric acid without changing other conditions; it shows the role of synthesis parameters more significant. Our results suggest that the prepared CuO nanostructures have a potential to be used as absorbing material in solar cell applications.

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Exploration of structural and physicochemical properties of small molecules to inhibit NMDA functionality

Structural Chemistry - The N-methyl-D-aspartate (NMDA) is the family of glutamate receptor, which is involved in controlling synaptic plasticity and memory function; but overactivation of this...     

Effect of Plant Growth Promoting Bacteria Associated with Halophytic Weed (<Emphasis Type="Italic">Psoralea corylifolia</Emphasis> L) on Germination and Seedling Growth of Wheat Under Saline Conditions

Halotolerant bacteria associated with Psoralea corylifolia L., a luxuriantly growing annual weed in salinity-affected semi-arid regions of western Maharashtra, India were evaluated for their plant growth-promoting activity in wheat. A total of 79 bacteria associated with different parts viz., root, shoot and nodule endophytes, rhizosphere, rhizoplane, and leaf epiphytes, were isolated and grouped based on their habitat. Twelve bacteria isolated for their potential in plant growth promotion were further selected for in vitro studies. Molecular identification showed the presence of the genera Bacillus, Pantoea, Marinobacterium, Acinetobacter, Enterobacter, Pseudomonas, Rhizobium, and Sinorhizobium (LC027447-53; LC027455; LC027457, LC027459, and LC128410). The phylogenetic studies along with carbon source utilization profiles using the Biolog® indicated the presence of novel species and the in planta studies revealed promising results under salinity stress. Whereas the nodule endophytes had minute plant growth-promoting (PGP) activity, the cell free culture filtrates of these strains enhanced seed germination of wheat (Triticum aestivum L). The maximum vigor index was monitored in isolate Y7 (Enterobacter sp strain NIASMVII). Indole acetic acid (IAA) production by the isolates ranged between 0.22 and 25.58 μg mL^?1. This signifies the need of exploration of their individual metabolites for developing next-generation bio-inoculants through co-inoculation with other compatible microbes. This study has potential in utilization of the weed-associated microbiome in terms of alleviation of salinity stress in crop plants.