Synthesis, pharmacological screening and computational analysis of some 2-[l-Indol-3-yl]-A [[un]substituted phenylmethylidene] acetohydrazides and 2-[l-Indol-3-yl]-7V[[un]substituted benzoyl/2-thienylcarbonyl] acetohydrazides

The undertaken research was initiated by transforming 2-[l-Indol-3-yl]acetic acid [1] in catalytic amount of sulfuric acid and ethanol to ethyl 2-[l-Indol-3-yl]acetate [2], which was then reacted with hydrazine monohydrate in methanol to form 2-[l-Indol-3-yl]acetohydrazide [3]. Further, The reaction scheme was designed into two pathways where, first pathway involved The reaction of 3 with substituted aromatic aldehydes [4a-o] in methanol with few drops of glacial acetic acid to generate 2-[l-Indol-3-yl]-AD-[[un]substitutedphenylmethylidene]acetohydrazides [5a-o] and in second pathway 3 was reacted with acyl halides [6a-e] in basic aqueous medium [pH 9-10] to afford 2-[l-Indol-3-yl]-AD-[[un]substitutedbenzoyl/2-thienylcarbonyl]acetohydrazides [7a-e]. All The synthesized derivatives were characterized by IR, EI-MS and !H-NMR spectral techniques and evaluated for their anti-bacterial potentials against Gram positive and Gram negative bacterial strains and it was found that compounds 7a-d exhibited antibacterial activities very close to standard Ciprofloxacin. The synthesized derivatives demonstrated moderate to weak anti-enzymatic potential against oc-Glucosidase and Butyrylcholinesterase [BChE] where, compounds 7c and 5c exhibited comparatively better inhibition against these enzymes respectively. Compounds 7a, 7d and 7e showed excellent anti-enzymatic potentials against Lipoxygenase [LOX] and their IC[5]o values were much lower than the reference standard Baicalein. Enzyme inhibitory activities were also supported by computational docking results. Compounds 5c, 7a, 7b and 7c also showed low values of % hemolytic activity as well, showing that these molecules were not toxic, indicating that these molecules can be utilized as potential therapeutic agents against inflammatory ailments

Pyrus pashia: a persuasive source of natural antioxidants

Pyrus pashia Buch. and Ham. was subjected to extraction with methanol. Methanolic extracts of fruit, bark and leaf were partitioned separately with four organic solvents in order of increasing polarity, asn-hexane, chloroform, ethyl acetate and n-butanol after dissolving in distilled water. Phytochemical screening revealed the presence of phenolics, flavonoides, alkaloids and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol soluble fractions. The antioxidant activity of crude methanolic extracts, all the obtained fourorganic fractions and remaining aqueous fractions was evaluated by different methods such as: 1,1-diphenyl-2-picrylhydrazyl [DPPH] free radical scavenging activity, ferric reducing antioxidant power [FRAP] assay and total antioxidant activity by phosphomolybdenum complex method as well as determination of total phenolics. The results of antioxidant activity exhibited that chloroform soluble fraction of fruit showed the highest value of percent inhibition of DPPH [48.16 +/- 0.21 microg/ml] at the concentration of 10microg/ml. Ethyl acetate soluble fraction displayed the lowest antioxidant activity having/C[50] value of bark as [8.64 +/- 0.32microg/ml] relative to butylated hydroxytoluene [BHT], having IC[50] of 12.1 +/- 0.92microg/ml. The ethyl acetate soluble fraction of bark revealed the highest FRAP[s] value [174.618 +/- 0.11 TE microM/ml] among all the three parts. This fraction also showed the highest value of total antioxidant activity as [1.499 +/- 0.90], determined by phosphomolybdenum complex method. Moreover, this fraction also conferred the highest phenolic content [393.19 +/- 0.72] as compared to other studied fractions of fruit and leaf

Cotinus coggyria: a rich source of antioxidants

Methanolic extract of Cotinus coggyria Scop. was mixed in distilled water and partitioned first with the n-hexane, then with chloroform, then ethyl acetate and at the end with n-butanol. The phytochemical screening of plant showed presence of the phenolics, cardiac glycosides and flavonoides in large amount in the chloroform, n-butanol and ethyl acetate soluble fraction. Antioxidant activity of these four fractions and the left behind aqueous fraction was measured by four methods such as: 1,1-diphenyl-2-picrylhydrazyl [DPPH] free radical scavenging activity, ferric thiocyanate assay, ferric reducing antioxidant power [FRAP] assay and total antioxidant activity. Total phenolics were also measured. Noteworthy antioxidant potential was shown by the chloroform, n-butanol and ethyl acetate soluble fraction showed. Ethyl acetate fraction showed highest% inhibition of the DPPH radical when compared with the other studied fractions i.e. 81.64 +/- 1.29% inhibition of the DPPH radical at the concentration of 30 microg/ml. Its IC[50] value was found to be 15.58 +/- 0.09 microg/ml, comparative to the butylated hydroxytoluene [BHT], which has IC[50] value 12.6 +/- 0.85microg/mL. This fraction also showed the highest lipid peroxidation inhibition [61.41 +/- 1.16%], as well as highest values of FRAP [697.76 +/- 1.98 microg of trolox equivalents] total antioxidant activity [1.02 +/- 0.09] and total phenolic contents [229.34 +/- 0.57] comparative to the other studied fractions. The chloroform and n-butanol soluble fraction also showed good results for all the studied antioxidant assays

In vitro assessment of relief to oxidative stress by different fractions of Boerhavia procumbens

Methanolic extract of Boerhavia procumbens Bank ex Roxb. was partitioned with n-hexane, chloroform, ethyl acetate and n-butanol sequentially after dissolving in distilled water. Phytochemical screening showed presence of phenolics, flavonoides and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol soluble fraction. The antioxidant activity of all these fractions and the remaining aqueous fraction was evaluated by four methods such as: 1,1-diphenyl-2-picrylhydrazyl [DPPH] free radical scavenging activity, ferric reducing antioxidant power [FRAP] assay, total antioxidant activity and ferric thiocyanate assay. Total phenolics were also determined. Some fractions showed noteworthy antioxidant activity. The results of the antioxidant activity revealed that the ethyl acetate soluble fraction showed the highest value of percent inhibition of DPPH [82.54 +/- 0.62] at the concentration of 125 micro g/ml. The IC[50] of this fraction was 37.11 +/- 0.23 micro g/ml, compared with butylated hydroxytoluene [BHT], which have IC[50] of 12.1 +/- 0.92 micro g/mL. It also showed the highest FRAP value [251.08 +/- 1.46 micro g of trolox equivalents] as well as the highest value of lipid peroxidation inhibition [57.21 +/- 52%], the highest total antioxidant activity [0.549 +/- 0.08] and also the highest total phenolic contents [77.1 +/- 0.6] as compared to the studied fractions. Phytochemical screening showed high percentage of phenolics, flavonoides and cardiac glycosides in this fraction