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 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

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