Ritika Sharma

Distant C-H Activation/Functionalization: A New Horizon of Selectivity Beyond Proximity

Activation/functionalization of inert C-H bond has undergone rapid growth in last decade and provides novel retro-synthetic disconnections for the synthesis of valuable molecules. The selectivity is often achieved by the use of directing group and is mainly limited to the proximal C-H bond. Initially, meta C-H activations were based on electronic or steric control and now it can be achieved by employing nitrile-based end-on-template as the directing group. The compilation of the remote C-H activation strategy will provide the useful linkage to the scientific community. This article is focused on recent progress in remote C-H activation, mechanistic understanding, and its applications in the field of total synthesis of targeted molecules.

Water-Mediated Synthesis of Benzazole and Thiourea Motifs by Reacting Naturally Occurring Isothiocyanate with Amines

Abstract An efficient, green, and facile method has been developed for the synthesis of benzazole and thiourea analogues from naturally occurring erucin in moderate to good yields. The reaction was carried out in water without using any metal catalyst or base. The present method tolerated the various functional groups on aromatic rings and also applicable for other isothiocyanates. GRAPHICAL ABSTRACT

To Analyze the Amelioration of Phenobarbital Induced Oxidative Stress by Erucin, as Indicated by Biochemical and Histological Alterations

PURPOSE Phenobarbital is a commonly employed antidepressant and anti-epileptic drug. The cancer promoting activity of this genotoxic xenobiotic is often ignored. It is responsible for oxidative stress leading to modulation in xenobiotic and antioxidative enzymes. Glucosinolates and more specifically their hydrolytic products are known for their antioxidative and anticancer activities. The present study involves the analysis of hepatoprotective effect of erucin (isolated from Eruca sativa (Mill.) Thell.) against phenobarbital mediated hepatic damage in male wistar rats. METHODS The liver homogenate was analyzed for oxidative stress (superoxide dismutase, catalase, guaiacol peroxidase, ascorbate peroxidase, glutathione reductase and lactate dehydrogenase), other oxidative parameters (thiobarbituric acid reactive species, conjugated dienes and lipid hydroperoxide), phase I enzymes (NADPH-cytochrome P450 reductase, NADH-cytochrome b5 reductase, cytochrome P420, cytochrome P450 and cytochrome b5), phase II enzymes (γ-glutamyl transpeptidase, DT-diaphorase and glutathione-S-transferase), serum parameters (alkaline phosphatase, serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, direct bilirubin and total bilirubin) and certain histological parameters. RESULTS Erucin accorded protection from phenobarbital induced hepatic damage by normalizing antioxidative enzymes, other oxidative parameters, phase I, II, and serum parameters. CONCLUSIONS Erucin, an analogue of sulforaphane has the potential to act as an anticancer agent by regulating various biochemical parameters.

Evaluation of antiplasmodial potential of C-2 and C-8 modified quinolines: in vitro and in silico study

BACKGROUND Malaria remains a common life-threatening infectious disease across the globe due to the development of resistance by Plasmodium parasite against most antimalarial drugs. The situation demands new and effective drug candidates against Plasmodium. OBJECTIVES The objective of this study is to design, synthesize and test novel quinoline based molecules against the malaria parasite. METHOD C-2 and C-8 modified quinoline analogs obtained via C-H bond functionalization approach were synthesized and evaluated for inhibition of growth of P. falciparum grown in human red blood cells using SYBR Green microtiter plate based screening. Computational molecular docking studies were carried out with top fourteen molecules using Autodoc software. RESULT The biological evaluation results revealed good activity of quinoline-8-acrylate 3f (IC50 14.2 µM), 2-quinoline-α-hydroxypropionates 4b (IC50 6.5 µM), 4j (IC50 5.5 µM) and 4g (IC50 9.5 µM), and against chloroquine sensitive pf 3D7 strain. Top fourteen molecules were screened also against chloroquine resistant Pf INDO strain and the observed resistant indices were found to lie between 1 and 7.58. Computational molecular docking studies indicated a unique mode of binding of these quinolines to Falcipain 2 and heme moiety, indicating these to be probable targets of their antiplasmodial action. CONCLUSION An important finding of our work is the fact that unlike chloroquine which shows a resistance Index of 15, the resistance indices for the most promising molecules studied by us were about one indicating equal potency against drug sensitive and resistant strains of malaria parasite.

Influence of Gibberellic Acid and Blossom Removal on Fruit Quality of Strawberry (Fragaria x ananassa Duch.) CV. Belrubi

A study were carried out to investigate the effect of gibberellic acid (GA3) and blossom removal on fruit quality of strawberry cv. belrubi under subtropical region. Various quality parameters were monitored with the application of three concentrations of gibberellic acid (GA3) 50 ppm, 100 ppm and 150 ppm and two levels of blossom removal partial and without deblossoming. Results of experimental showed that the highest juice content of fruits (86.70/86.46%), TSS (7.56/7.43°Brix), sugar content (4.33/4.26%), pH of fruit (3.87/3.86) were recorded in lower concentration of gibberellic acid 50 ppm treated plants with partial deblossoming during both the years of experimentations (2003–04 and 2004–05). However, the highest vitamin-C (63.75/63.66 mg/100g) was obtained with treatment combination 100 ppm GA3 with partial deblossoming. In addition, the highest acidity of fruit (0.77 and 0.79%) was registered in control (water spray without deblossoming) during both the years. From this study, it can be concluded that spraying of 50 ppm GA3 with partial blossom removal treated plants showed improve of fruit quality.