Synthetic N-[[substitutedsulfamoyl]phenyl]acetamides as moderate chymotrypsin inhibitors

A facile method has been implemented for the synthesis of different N-substituted sulfamoylacetamides by reacting 4-acetamidobenzenesulfonyl chloride [1] with different alkyl/aralkyl/aryl amines [2a-q] in basic aqueous media under controlled pH to afford -[[Substitutedsulfamoyl] phenyl]acetamides [3a-q] which were confirmed through spectral analysis like FT-IR, EIMS and [1]H-NMR. Moreover, the synthesized derivatives were screened against alpha-Chymotrypsin. The enzyme inhibitory results revealed that most of the synthesized compounds were found to be moderate enzyme inhibitors

Lonicera quinquelocularis: a rich source of antioxidant for protection against chronic diseases

The purpose of the research work was to examine the in vitro antioxidant activity of the different aqueous and organic fractions of Lonicera quinquelocularis Hardwicke. The methanol extract was dissolved in distilled water and fractioned with n-hexane, chloroform, ethyl acetate and n-butanol, successively. The antioxidant potential of the remaining aqueous and organic fractions was determined by using 1,1-diphenyl-2-picrylhydrazyl radical [DPPH] scavenging activity, total antioxidant activity, ferric reducing antioxidant power [FRAP] assay, ferric thiocyanate assay and total phenolics method. Among these fractions ethyl acetate fraction displayed the maximum antioxidant activity with IC[50] of [11.13+/-0.12micro g/ml]. It also exhibited the highest total antioxidant activity [0.595+/-0.00], FRAP value [128.2+/-4.54micro g/mL] and total phenolic contents [66.89+/-7.73micro g/g] as compared to other organic fractions. Phytochemical investigation of the above mentioned fractions showed the presence of flavanoids, phenolics, terpenoids, sugars, alkaloids, tannins, saponins and cardiac glycosides in appreciable amounts, which have major contribution towards antioxidant activity

Synthesis and antibacterial screening of S-substituted derivatives of 5-[3,4-methylenedioxyphenyl]-1,3,4-oxadiazol-2-thiol

The most emerging class among the heterocyclic compounds is 1,3,4-oxadiazoles for their diverse biological activities. In the present research work, piperonylic acid [1] was converted consecutively into corresponding ester [2], hydrazide [3] and 1,3,4-oxadiazole [4] through intermolecular cyclization. The synthesized compound 4 was subjected further to S-alkylation/aralkylation, using alkyl/aralkyl halides [5a-m] and S-substituted-1,3,4-oxadiazole derivatives were synthesized [6a-m]. The structure elucidation of the synthesized molecules was processed through [1]H-NMR, IR and mass spectral data. The antibacterial activity showed these molecules moderately good inhibitors of gram-negative and gram-positive bacteria

Synthesis of 2-[[5-phenyl-1,3,4-Oxadiazol-2-yl]sulfanyl]-N-substituted acetamides as potential antimicrobial and hemolytic agents

A new series of N-substituted derivatives of 2-[[5-phenyl-1,3,4-Oxadiazol-2-yl]sulfanyl] acetamides was synthesized. The synthesis was carried out by converting benzoic acid [1] into ethyl benzoate [2], benzohydrazide [3] and then 5-pheny-1,3,4-Oxadiazol-2-thiol [4] step by st0ep. The target compounds 6a-p were synthesized by reaction of compound 4 with equimolar ratios of different N-alkyl/aryl substituted 2-bromoacetamide [5a-p] in the presence of DMF and sodium hydride [NaH]. The spectral [EI-MS, IR, 1H-NMR] characterization of all the synthesized compounds reveal their successful synthesis. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. But 6h was the most active against the selected panel of microbes. This series showed less toxicity and may be considered for further biological screening and application trial except 6m, possessing higher cytotoxicity

Synthesis, spectral analysis and antibacterial evaluation of N'- substituted-2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2- ylthio]acetohydrazide derivatives

The biological potential of N'-substituted-2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2-ylthio]acetohydrazide [8ap] has been evaluated against bacterial strains of Gram-negative and Gram-positive bacteria. The multistep synthesis involved the conversion of 3-chlorobenzoic acid [1] to ethyl 3-chlorobenzoate [2], 3-chlorobenzohydrazide [3], 5-[3- chlorophenyl]-1,3,4-Oxadiazol-2-thiol [4], ethyl 2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2-ylthio] acetate [5] and 2-[5-[3- chlorophenyl]-1,3,4-Oxadiazol-2-ylthio]acetohydrazide [6]. The last step involved the reaction of 6 and aryl aldehydes, 7a-p, in methanol to synthesize the Schiff bases, 8a-p, with better yields. The structures of all the molecules were corroborated by spectral analysis. The Schiff bases were further evaluated for the antibacterial activity and found to be moderately good inhibitors of bacterial strains of Gram-bacteria

Synthesis, spectral analysis and biological evaluation of Nalkyl/ aralkyl/aryl-4-chlorobenzenesulfonamide derivatives

New potent organic compounds were synthesized with an aim of good biological activities such as antibacterial and anti-enzymatic. Three series of sulfonamide derivatives were synthesized by treating N-alkyl/aryl substituted amines [2a-f] with 4-chlorobenzensulfonyl chloride [1] to yield N-alkyl/aryl-4-chlorobenzenesulfonamide[3af] that was then derivatized by gearing up with ethyl iodide [4], benzyl chloride [5] and 4-chlorobenzyl chloride [6] using sodium hydride as base to initialize the reaction in a polar aprotic solvent [DMF] to synthesize the derivatives, 7a-f, 8afand 9a-f respectively. Structure elucidation was brought about by IR, 1H-NMR and EIMS spectra for all the synthesized molecules which were evaluated for their antibacterial activities and inhibitory potentials for certain enzymes

Synthesis, biological screening and molecular docking studies of some ethylated sulfonamides having 1,4-Benzodioxane moiety

The presented study comprises the synthesis of a new series of ethylated sulfonamides in which 1,4- benzodioxane moietyhas been incorporated. The reaction of 1,4-benzodioxane-6-amine [1] with ethane sulfonyl chloride [2] yielded N-[2,3-dihydrobenzo[1,4]dioxin-6-yl] ethanesulfonamide [3], which further on treatment with various alkyl/aralkyl halides, 4a-r, in N,N-dimethylformamide [DMF] and in the presence of lithium hydride [LiH] acting as a weak base and catalyst;yielded derivativesofN-alkyl/aralkyl substituted N-[2,3-dihydrobenzo [1,4] dioxin-6- yl] ethanesulfonamides [5a-r]. The characterization of these derivatives was carried out by different spectroscopic techniques like infra red, proton-NMR and mass spectrometry; then screened against various enzymes i.e. acetylcholinesterase, butyrylcholinesterase, lipoxygenase and alpha-glucosidase enzymes and five different bacterial strains. The synthesized compounds were found to be good inhibitors of lipoxygenase but moderate inhibitors of AChE, BChE and alpha-glucosidase; whereas compounds 3, 5a, 5f, 5n and 5r were found good antibacterial compounds. The interaction between inhibitors and target enzymes [cholinestrases and lipoxygenase] was computationally observed which correlated with the experimental results

Synthesis and screening of some new N-alkyl/aralkyl-N-[3,4-methylenedioxybenzyl]-4-substituted benzenesulfonamides as potential antibacterial agents

The various p-substituted benzenesulfonyl chlorides [2a-e] were treated with [3,4-methylenedioxy] benzylamine [1] in the presence of aqueous Na2CO3 solution to synthesize N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [3a-e]. The synthesized molecules were further converted into corresponding Nethyl/benzyl/4-flourobenzyl-N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [7a-e, 8a-e, 9a-e] on reaction with ethyl iodide [4], benzyl chloride [5] and 4-flourobenzyl chloride [6] in the presence of sodium hydride using N,N-dimethylformamide as solvent. The structure elucidation was processed through different spectral techniques including IR, [1]H-NMR and EIMS. The screening of the synthesized molecules against Gram-bacterial strains, to evaluate antibacterial activity, showed them moderately good inhibitors as shown by their low MIC values

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

Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated coumarin

Coumarins have much importance in dyes, drugs, perfumes and pesticides. In the demonstrated research work, a benignant series of chlorinated coumarins was synthesized and screened against different enzymes. First, 6-Chloro-7-hydroxy-4-methyl-2H-chromen-2-one [3] was geared up by the reaction of 4-chlororesorcinol [1] and ethyl acetoacetate [2] in the presence of concentrated H[2]SO[4]. Second, various O-substituted derivatives of chlorinated coumarins, 5a-j, were set up by pairing different alkyl/aralkyl halides, 4a-j, with 3 in the presence of NaH in DMF as solvent. The structures of all the synthesized compounds were clarified through spectral analysis using EI-MS, IR and [1]H-NMR. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were acetyl cholinesterase [AChE], butyryl cholinesterase [BChE] and lipoxygenase [LOX]. The most proficient activity was shown against both cholinesterase enzymes

Synthesis, spectral characterization and enzyme inhibition studies of different chlorinated sulfonamides

Sulfonamides are adherent to a biologically dynamic category of compounds and are under consideration of many organic synthetic researches to synthesize pharmacologically important compounds. In this demonstrated research work, a benignant series of chlorinated sulfonamides were synthesized and screened against different enzymes. These various chlorinated sulfonamides [3a-i] were set up by pairing of different substituted anilines [2a-i] with 4-chlorobenzenesulfonyl chloride [1] under basic pH in an aqueous media. The structures of the synthesized chlorinated sulfonamides were furnished by [1] H-NMR, IR and EI-MS. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were urease, butyrylcholinesterase [BChE] and lipoxygenase [LOX]. All the compounds exhibited good inhibitory activities against these enzymes but the strong activity was shown against BChE and hence can be employed for discovery of 'lead' compounds against Alzheimer's disease [AD]

Synthesis of some new biologically active N-substituted-2''- [[phenylsulfonyl][piperidin-1-yl]amino]acetamide derivatives

A new series of N-aryl/aralkyl substitued-2"-[[phenylsulfonyl][piperidin-1-yl]amino]acetamide [7a-k] was synthesized. These derivatives were geared up by the pairing of benzenesulfonyl chloride [4] with 1-aminopiperidine [5] under dynamic pH control in aqueous media to afford parent compound N-[Piperidin-1-yl] benzenesulfonamide [6], followed by the substitution at nitrogen atom with different electrophiles N-aryl/aralkyl-substituted-2-bromoacetamides [3a-k] in the presence of sodium hydride [NaH] and N,N-Dimethylformamide [DMF] to give a new series of Nsubstituted derivatives of acetamide [7a-k] bearing piperidine moiety. All the synthesized compounds were confirmed on the basis of IR, EIMS and 1H-NMR spectral data. The synthesized compounds were evaluated against acetylcholinesterase and butyrylcholinesterase [AChE and BChE] respectively and lipoxygenase [LOX] enzymes. Almost all the synthesized compounds displayed promising activity but few of them remained inactive against lipoxygenase enzymes.

Synthesis, characterization and biological screening of N-substituted derivatives of 5-benzyl-1,3,4-oxadiazole-2yl-2''-sulfanyl acetamide

A series of new N-substituted derivatives of 5-benzyl-1, 3, 4-oxadiazole-2yl-2''-sulfanyl acetamide [6a-n] were synthesized in three phases. The first phase involved the sequentially converting phenyl acetic acid into ester, hydrazide and finally cyclized in the presence of CS[2] to afford 5-benzyl-1, 3, 4-oxadiazole-2-thiol. In the second phase N-substituted-2-bromoacetamides were prepared by reacting substituted amines with bromoacetyl bromide in basic media. In the third phase, 5-benzyl-1,3,4-oxadiazole-2-thiol was stirred with N-substituted-2-bromoacetamides in the presence of N,N-dimethyl formamide [DMF] and sodium hydride [NaH] to get the target compounds. Spectral techniques were used to confirm the structures of synthesized compounds. Synthesized compounds were screened against butyrylcho linesterase [BChE], acetylcholinesterase [AChE], and lipoxygenase enzymes [LOX] and were found to be relatively more active against acetylcholinesterase

Synthesis of biologically active O-substituted derivatives of 1-[[3, 5-dichloro-2-hydroxyphenyl]sulfonyl]piperidine

In the present work, a series of 2-O-substituted derivatives of 1-[[3,5-dichloro-2-hydroxy phenyl] sulfonyl]piperidine [5a-j] were synthesized. These derivatives were geared up by the coupling of 3,5-dichloro-2-hydroxy benzenesulfonyl chloride [1] with piperidine [2] under dynamic pH control in aqueous media to form parent compound 1-[[3,5-dichloro-2-hydroxyphenyl]sulfonyl]piperidine [3], followed by the substitution at oxygen atom with different electrophiles [4a-j] in the presence of sodium hydride [NaH] and dimethyl formamide [DMF] to give a series of Osubstituted derivatives of sulfonamides bearing piperidine nucleus 5a-j. The synthesized O-substituted sulfonamides were spectrally characterized. The bioactivity of all the synthesized compounds were evaluated against lipoxygenase [LOX], acetylcholinesterae [AChE] and butyrylcholinesterase [BChE] enzymes and found to be having talented activity against butyrylcholinesterase enzyme

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

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

Synthesis, characterization and biological screening of sulfonamides derived form 2-phenylethylamine

In the present study, a series of N-substituted derivatives of 2-phenylethylamine has been synthesized. The reaction of 2-phenylethylamine [1] with benzene sulfonyl chloride [2] yielded N-[2-phenylethyl] benzenesulfonamide [3], which further on treatment with alkyl/acyl halides [4a-i] in the presence of sodium hydride furnished into Nsubstituted sulfonamides [5a-i]. These derivatives were characterized by IR, [1]H-NMR and EI-MS and then screened against acetyl cholinesterase [AChE], butyryl cholinesterase [BChE] and lipoxygenase enzyme [LOX] and were found to be potent inhibitors of butyryl cholinesterase only

Preparation of new formulations of perfumes and their persistency

Sweat is released from the glands to cool down the body temperature by thermoregulation. By the bacterial action this sweat produces smell which may become intolerable for the person himself and also for the surrounding people. This study is related to the formation of samples of perfumes to cope with the discussed problem. Four samples were prepared and their quantitative analysis was performed for their respective odour value and period of sensation

Preparation of new formulations of balm as a remedy of flu and their efficacy

Influenza, called the flu, is an acute, highly contagious infection of the respiratory tract, which commonly occurs in children or adults of any age mostly in the winter. In the present study three new formulations of petroleum jelly and essential oils based balm were prepared for the treatment of flu and their efficacy was studied on different age group people i.e. infants, adults, and old age. Results showed that the prepared balms not only gave relief from headache, fever, cough etc., but also they reduced the intensity of viral infection