Synthesis of some new N-[alkyl/aralkyl]-N-[2,3-dihydro-1,4-benzodioxan-6-yl]-4-chlorobenzenesulfonamides as possible therapeutic agents for Alzheimer's disease and Type-2 Diabetes

In the current research work, a series of new N-[alkyl/aralkyl]-N-[2,3-dihydro-1,4-benzodioxan-6-yl]-4-chlorobenzenesulfonamides has been synthesized by reacting 1,4-benzozzdioxan-6-amine [1] with 4-chlorobenzenesulfonyl chloride [2] to yield N-[2,3-dihydro-1,4-benzodioxan-6-yl]-4-chlorobenzenesulfonamide [3] which was further reacted with different alkyl/aralkyl halides [4a-n] to afford the target compounds [5a-n]. Structures of the synthesized compounds were confirmed by IR, 1H-NMR, EI-MS spectral techniques and CHN analysis data. The results of enzyme inhibition showed that the molecules, N-2-phenethyl-N-[2,3-dihydro-1,4-benzodioxin-6-yl]-4- chlorobenzenesulfonamide [5j] and N-[1-butyl]-N-[2,3-dihydro-1,4-benzodioxin-6-yl]-4-chlorobenzenesulfonamide [5d], exhibited moderate inhibitory potential against acetylcholinesterase with IC50 values 26.25+/-0.11 ?M and 58.13+/-0.15 ?M respectively, whereas, compounds N-benzyl-N-[2,3-dihydro-1,4-benzodioxin-6-yl]-4-chlorobenzenesulfonamide [5i] and N-[pentane-2-yl]-N-[2,3-dihydro-1,4-benzodioxin-6-yl]-4-chlorobenzenesulfonamide [5f] showed moderate inhibition against ?-glucosidase enzyme as evident from IC50 values 74.52+/-0.07 and 83.52+/-0.08 µM respectively, relative to standards Eserine having IC50 value of 0.04+/-0.0001 µM for cholinesterases and Acarbose having IC50 value 38.25+/-0.12 µM for ?-glucosidase, respectively

Development and validation of a stability-indicating RP-HPLC-FLD method for determination of 5-[[4-chlorophenoxy] methyl]-1, 3, 4- oxadiazole-2-thiol; A novel drug candidate

The present study describes the development and validation of a simple high performance liquid chromatographic method for the determination of a novel drug candidate, 5-[[4-chlorophenoxy] methyl]-1, 3, 4- oxadiazole-2-thiol. The stability-indicating capacity of the method was evaluated by subjecting the compound's solution to hydrolytic, oxidative, photolytic, transition metal- and thermal- stress. The chromatographic separation was achieved over a C18 column [Promosil, 5 microm, 4.60 × 250 mm], maintained at 25°C, using an isocratic mobile phase comprising a mixture of acetonitrile and acidified water of pH 2.67 [1:1, v/v], at a flow rate of 1.00 mL/min and detection using a fluorescent light detector [excitation at 250 nm and emission at 410 nm]. The Beer's law was followed over the concentration range 2.50-50.00 microg/mL. The recovery [98.56-100.19%, SD <5%], intraday accuracy and precision [97.31-100.81%, RSD<5%] and intermediate accuracy and precision [98.10-99.91%, RSD<5%] indicated that the method was reliable, repeatable, reproducible and rugged. The resolution and selectivity factors of the compound's peak from the nearest resolving peak, particularly in case of dry heat and copper metal stress, were found to be greater than 2 and 1, respectively, which indicated specificity and selectivity. The compound was extensively decomposed in alkaline-hydrolytic, oxidative, metal- and dry heat- stress. However, the compound in acidic and neutral conditions was resistant to photolysis. The results of the present study indicate that the developed method is specific, selective, sensitive and suitable, hence, may be used for quality control, stability testing and preformulation studies

Synthesis of some new 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides as potent antibacterial agents

In this work, a new series of 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides has been synthesized and evaluated for their antibacterial potential. The synthesis was initiated by the reaction of different aryl/aralkyl amines [1a-u] with 2-bromoacetylbromide [2] to obtain N-aryl/aralkyl-2-bromoacetamides [3a-u]. Equimolar quantities of different N-aryl/aralkyl-2-bromoacetamides [3a-u] and 2-furoyl-1-piperazine [4] was allowed to react in acetonitrile and in the presence of K2CO3, to form 2-[4-[2-furoyl]-1-piperazinyl]-N-aryl/aralkyl acetamides [5a-u]. The structural elucidation was done by EI-MS, IR and 1 H-NMR techniques of all the synthesized compounds. All of the synthesized molecules were active against various Gram positive and Gram negative bacterial strains. Among them 5o and 5c showed very excellent MIC values. The cytotoxicity of the molecules was also checked to find their utility as possible therapeutic agents, where 5c [0.51%] and 5g [1.32%] are found to be least toxic in the series

2-[[5-(Substituted-phenyl]-1,3,4-oxadiazol-2-yl]sulfanyl]-N-[1,3-thiazol-2-yl]acetamides: new bi-heterocycles as possible therapeutic agents

An electrophile, N-[1,3-thiazol-2-yl]-2-bromoacetamide [3], was synthesized by the reaction of 1,3-thiazole-2- amine [1] and 2-bromoethanoyl bromide [2] in an aqueous medium. A series of carboxylic acids, 7a-j, were converted into 1,3,4-oxadiazole heterocyclic core, through a series of three steps. The final compounds, 8a-j, were synthesized by stirring 7a-j and 3 in an aprotic polar solvent. The structural elucidation of the synthesized compounds was supported by IR, EI-MS, 1 H-NMR, and 13C-NMR spectral data. Title compounds were evaluated for enzyme inhibition against cholinesterases and alpha-glucosidase enzymes and their cytotoxic behavior was monitored using brine shrimp assay. The enzyme inhibitor potential of compounds was supported by molecular docking studies

Synthesis, spectral analysis and antibacterial activity of some novel 5- substituted-2-[[6-bromo-3,4-methylenedioxybenzyl]thio]-1,3,4- oxadiazole derivatives

A number of novel 5-substituted-2-[[6-bromo-3,4-methylenedioxybenzyl]thio]-1,3,4-Oxadiazole derivatives [6a-l] have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids [1a-l] as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols [4a-l] were yielded in good amounts.The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride [5] in DMFto synthesize the required compounds. All the synthesized molecules were well characterized by IR, [1]H-NMR, [13]C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential

Synthesis of 2-Furyl [[4-aralkyl]-1-piperazinyl] methanone derivatives as suitable antibacterial agents with mild cytotoxicity

The aim of the present research work was synthesis of some 2-furyl [[4-aralkyl]-1-piperazinyl] methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl[-1-piperazinyl] methanone [1] in N,N-dimethylformamide [DMF] and lithium hydride with different aralkyl halides [2a-j] to afford 2-furyl[[4-aralkyl]-1piperazinyl] methanone derivatives [3a-j]. The structural confirmation of all the synthesized compounds was done by IR, EI-MS, 1H-NMR and 13C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative [S. typhi, E. coli, P. aeruginosa] and Gram-positive [B. subtilis, S. aureus] bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52 +/- 0.[micro]g/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45 +/- 0.58[micro]g/mL

In silico and BSA binding study of some new biological analogs of 1, 2, 4-triazole pendant with azinane through microwave and conventional synthesis

Microwave and conventional techniques were employed to synthesize a novel array of compounds 7a-g with 1, 2, 4-triazole and piperidine rings having great biological importance. The microwave assisted method has a better operational scope with respect to time and yield comparative to the conventional method. 1H-NMR, 13C-NMR and IR techniques were employed to justify the structure of synthesized compounds. The antioxidant, butyrylcholinesterase inhibition and urease inhibition potential of every synthesized compound was evaluated. Every member of the synthesized series was found potent against mentioned activities. Compound 7g was the most active anti-urease agent having IC50 [microM] value 16.5 +/- 0.09 even better than the thiourea with an IC50 [microM] value of 24.3 +/- 0.24. The better urease inhibition potential of 7g was also elaborated and explained by docking and bovine serum albumin [BSA] binding studies

Synthesis, in vitro and in silico studies of S-alkylated 5-[4methoxyphenyl]-4-phenyl-4H-1, 2, 4-triazole-3-thiols as cholinesterase inhibitors

The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide [1] was cyclized with phenyl isothiocyanate [2] via 2-[4methoxybenzoyl]-N-phenylhydrazinecarbothioamide [3]; an intermediate to 5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4triazol-3-thiol [4]. The electrophiles; alkyl halides 5[a-g] were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4-triazole-3-thiols 6[a-g]. Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-[n-heptylthio]-5-[4-methoxyphenyl]-4-phenyl-4H-1,2,4triazole; 6g against AChE [IC50; 38.35 +/- 0.62?M] and BChE [IC50; 147.75 +/- 0.67micro M] enzymes. Eserine [IC50; 0.04 +/- 0.01?M] was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96 % cell viability [6g] at 25 micro M and with 2.41% cell viability at 50?M among library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics

Anti-psychotics induced sexual dysfunction

Background: Sexual dysfunction associated with the use of antipsychotic drugs is quite prevalent affecting the patients' quality of life and one of the reasons for non-compliance. This important aspect is underestimated and overlooked by the treating professionals, partly because patients rarely talk about their dysfunction. Due to the scarcity of local data on the subject the objective of the present study was to explore and compare the prevalence of sexual dysfunction associated with antipsychotic drugs

Methods: This was a hospital-based cross-sectional study comprising of comparative assessment among five antipsychotics being consumed by 91 male patients under this study

Results: Risperidone, haloperidol and olanzapine collectively as a group were associated with increased incidence of sexual dysfunction [42.43%] compared to quetiapine and aripiprazole group [16%] which was statistically significant. Individually risperidone [48%] and haloperidol [45.81%] were associated with highest incidence of sexual dysfunction followed by olanzapine [29.41%]. Quetiapine [16.67%] and aripiprazole [15.38%] were associated with the lowest incidence of sexual dysfunction

Conclusion: Risperidone and haloperidol are associated with a higher rate of sexual dysfunction compared to olanzapine. Quetiapine and aripiprazole have a significantly lower profile of adverse effects on sexual function

Enzyme inhibitory, antifungal, antibacterial and hemolytic potential of various fractions of Colebrookia oppositifolia

The purpose of the present investigation was to assess the enzyme inhibition, antifungal, antibacterial and hemolytic activities of various fractions of Colebrookia oppositifolia Smith. The MeOH extract of plant was dissolved in dist. water and partitioned with n-hexane, CHCl[3], EtOAc and n-BuOH sequentially. Enzyme inhibition studies were done against four enzymes i.e. alpha-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Ethyl acetate fraction possessed very good activity against alpha-glucosidase [IC[50] 57.38 +/- 1.23 micro g/mL]. CHCl3 fraction displayed good activity against alpha-glucosidase and lipoxygenase while moderate activity against butyryl cholinesterase. EtOAc fraction displayed good activity against lipoxygenase. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Aqueous fraction displayed good activity against G. lucidum and A. flavus. Antibacterial activity was checked against Staphylococcus aureus, Bacillus subtilis, Pasturella multocida and Escherichia coli by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform, ethyl acetate and aqueous fraction showed good activity against E. coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%

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, 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

Outcomes of intravitreal bevacizumab and macular photocoagulation for treatment of diabetic macular edema in a tertiary care eye hospital at Karachi

Objective: To study the outcomes of intravitreal injection of Bevacizumab and laser photocoagulation in the treatment of diabetic macular edema [DME]

Methods: Seventy-two eyes of 59 patients with diabetic macular edema were divided into two groups of 41 eyes [Group-A] and 31 eyes [Group-B]. Subjects in group-A were treated with three intravitreal injections of Bevacizumab [IVB], and that of group-B with macular photocoagulation. Duration of study was 9 months. Follow up pattern for both groups was 1,2,3 and 6 months. Best Corrected Visual acuity on log AAAR [BCVA] for distance as well as near in each visitwas recorded. Retinal OCT for central macular thickness [CMT] was performed on baseline. SPSS version 20.0 was used to analyze the data

Results: Mean age of the patients was 53.76 +/- 8.82 ranging to 36-71 years. Out of 59 patients, 40 [67.8%] were male and 19 [32.2%] female. It was observed that the difference of results among both groups was not significant. Fig.2 documents visual acuity recorded as Improved; Stable and Worse. in BCVA has been almost similar between both the treatment groups although it was noted that JVB group showed early improvement in BCVA at follow-ups of 1 and 3 months. A long term follow-up is required in these cases to see the effect of both these treatment strategies

Synthesis and in silico study of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives as suitable therapeutic agents

Abstract In the study presented here, a new series of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives was targeted. The synthesis was initiated by the treatment of different secondary amines (1a-h) with 4-bromomethylbenzenesulfonyl chloride (2) to obtain various 1-{[4-(bromomethyl)phenyl]sulfonyl}amines (3a-h). 2-Furyl(1-piperazinyl)methanone (2-furoyl-1-piperazine; 4) was then dissolved in acetonitrile, with the addition of K2CO3, and the mixture was refluxed for activation. This activated molecule was further treated with equi-molar amounts of 3a-h to form targeted 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives (5a-h) in the same reaction set up. The structure confirmation of all the synthesized compounds was carried out by EI-MS, IR and 1H-NMR spectral analysis. The compounds showed good enzyme inhibitory activity. Compound 5h showed excellent inhibitory effect against acetyl- and butyrylcholinesterase with respective IC50 values of 2.91±0.001 and 4.35±0.004 µM, compared to eserine, a reference standard with IC50 values of 0.04±0.0001 and 0.85±0.001 µM, respectively, against these enzymes. All synthesized molecules were active against almost all Gram-positive and Gram-negative bacterial strains tested. The cytotoxicity of the molecules was also checked to determine their utility as possible therapeutic agents.

Synthesis, spectral analysis and pharmacological study of N'- substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazides

ABSTRACT A series of molecules bearing multiple functional groups were synthesized to study their antibiotic effect against Gram-positive and Gram-negative bacteria and lipoxygenase activity as well. 2,4-Dimethylcarbolic acid (1) was refluxed with ethyl 2-bromoacetate to synthesize ethyl 2-(2,4-dimethylphenoxy)acetate (2). Compound 2 was converted to the corresponding hydrazide 3, again on refluxing with hydrazine. The compound 5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-thiol (4) was synthesized by the reaction of 3 and CS2 in the presence of KOH. Compound 4 was further converted to the corresponding ester 5 and then 2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide (6). The final molecules N'-substituted-2-(5-((2,4-dimethylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetohydrazide, 8a-m, bearing ether, 1,3,4-oxadiazole, thioether, hydrazone and azomethine functional groups were synthesized by stirring the aryl carboxaldehydes 7a-m with 6 in methanol at room temperature. The depicted structures of all synthesized molecules were corroborated by IR, 1H-NMR and EIMS spectral data analysis. 8m and 8i showed substantial antibacterial activity and lipoxygenase inhibitory activity, respectively.

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, 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