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| Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Qureshi,Muhammad Zahid; Khan,Farhan Mehmood; Khan,Khalid Mohmmed; Ashraf,Muhammad; Afzal,Iftikhar. |
| This manuscript reports the synthesis of a series of N-substituted derivatives of 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzene sulfonyl chloride (2) yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which further on treatment with sodium hydride and alkyl halides (4a-g) furnished into new sulfonamides (5a-g). Second, the phenitidine reacted with benzoyl chloride (6) and acetyl chloride (8) to yield the reported N-benzoyl phenitidine (7) and N-acetyl phenitidine (9), respectively. These derivatives were characterized by infrared spectroscopy, ¹H-NMR, and EI-MS, and then screened against acetylcholinesterase, butylcholinesterase, and lipoxygenase enzyme, and were found to be potent inhibitors of butyrylcholinesterase alone. |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 2-Phenitidine/inhibitor activity; Sulfonamides; Acetamide; Benzamide; Butyrylcholinesterase. |
| Ano: 2013 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100014 |
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| Iqbal,Javed; Rehman,Aziz-ur-; Abbasi,Muhammad Athar; Siddiqui,Sabahat Zahra; Rasool,Shahid; Ashraf,Muhammad; Iqbal,Ambar; Hamid,Sujhla; Chohan,Tahir Ali; Khalid,Hira; Laulloo,Sabina Jhaumeer; Shah,Syed Adnan Ali. |
| We synthesized a series of compounds bearing pharmacologically important 1,3,4-oxadiazole and piperidine moieties. Spectral data analysis by 1H-NMR, 13C-NMR, IR and EI-MS was used to elucidate the structures of the synthesized molecules. Docking studies explained the different types of interaction of the compounds with amino acids, while bovine serum albumin (BSA) binding interactions showed their pharmacological effectiveness. Antibacterial screening of these compounds demonstrated moderate to strong activity against Salmonella typhi and Bacillus subtilis but only weak to moderate activity against the other three bacterial strains tested. Seven compounds were the most active members as acetyl cholinesterase inhibitors. All the compounds presented... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 1; 3; 4-Oxadiazole Acetylcholinesterase (AChE) inhibition Antibacterial activity Piperidine Sulfonamide Urease inhibition. |
| Ano: 2020 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100596 |
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| Rubab,Kaniz; Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Siddiqui,Sabahat Zahra; Ashraf,Muhammad; Shaukat,Ayesha; Ahmad,Irshad; Lodhi,Muhammad Arif; Khan,Farman Ali; Shahid,Muhammad; Akhtar,Muhammad Nadeem. |
| abstract A series of N-substituted 2-{[5-(1H-indol-3-ylmethyl)-1,3,4-oxadiazol-2-yl]sulfanyl}acetamides (8a-w) was synthesized in three steps. The first step involved the sequential conversion of 2-(1H-indol-3-yl)acetic acid (1) to ester (2) followed by hydrazide (3) formation and finally cyclization in the presence of CS2 and alcoholic KOH yielded 5-(1H-indole-3-yl-methyl)-1,3,4-oxadiazole-2-thiol (4). In the second step, aryl/aralkyl amines (5a-w) were reacted with 2-bromoacetyl bromide (6) in basic medium to yield 2-bromo-N-substituted acetamides (7a-w). In the third step, these electrophiles (7a-w) were reacted with 4 to afford the target compounds (8a-w). Structural elucidation of all the synthesized derivatives was done by 1H-NMR, IR and EI-MS... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 1H-indol-3-acetic acid N-substituted 2-{[5-(1H-indol-3-ylmethyl)-1; 3; 4-oxadiazol-2-yl] sulfanyl}acetamides/antibacterial activity N-substituted 2-{[5-(1H-indol-3-ylmethyl)-1; 3; 4-oxadiazol- 2-yl]sulfanyl} acetmides/hmolytic activity α-Glicosidase Butirylcholinesterase Lipoxygenase. |
| Ano: 2015 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000400931 |
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| Hussain,Ghulam; Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Siddiqui,Sabahat Zahra; Shah,Syed Adnan Ali; Ashraf,Muhammad; Qurat-ul-Ain,; Ahmad,Irshad; Malik,Rabia; Lodhi,Muhammad Arif; Khan,Farman Ali; Shahid,Muhammad; Fatima,Hina. |
| 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... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Piperazine derivatives/antimicrobial activity; Piperazine derivatives/in silico; Piperazine derivatives/Cholinesterase assays; Piperazine derivatives/ hemolytic activity.. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100613 |
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| Abbasi,Muhammad Athar; Riaz,Sajid; Rehman,Aziz-ur-; Siddiqui,Sabahat Zahra; Shah,Syed Adnan Ali; Ashraf,Muhammad; Lodhi,Muhammad Arif; Khan,Farman Ali. |
| The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data.... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Benzodioxane; Acetamide; Spectral analysis; A-Glucosidase; Acetylcholinesterase; Molecular docking. |
| Ano: 2019 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100518 |
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| Sattar,Almas; Aziz-ur-Rehman,; Abbasi,Muhammad Athar; Siddiqui,Sabahat Zahra; Rasool,Shahid; Ahmad,Irshad. |
| ABSTRACT Keeping in mind the pharmacological importance of the 1,3,4-oxadiazole moiety, a series of new S-substituted derivatives, 5a-h, of 5-(1-(4-tosyl)piperidin-4-yl)-1,3,4-oxadiazol-2-thiol (3) were synthesized. The reaction of p-toluenesulfonyl chloride (a) and ethyl isonipecotate (b) produced ethyl 1-(4-tosyl)piperidin-4-carboxylate (1) which was further transformed into 1-(4-tosyl)piperidin-4-carbohydrazide (2) by hydrazine hydrate in methanol. Compound 2 was refluxed with CS2 in the presence of KOH to synthesize 5-(1-(4-tosyl)piperidin-4-yl)-1,3,4-oxadiazol-2-thiol (3). The desired compounds, 5a-h, were synthesized by stirring 3 with aralkyl halides, 4a-h, in DMF using NaH as an activator. The structures of synthesized compounds were elucidated by... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: 1; 3; 4-Oxadiazole/antibacterial activity. 1; 3; 4-Oxadiazole/enzyme inhibitory activity. Isonipecotate. Sulfonamide.. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000100009 |
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| Rasool,Shahid; Aziz-ur-Rehman,; Abbasi,Muhammad Athar; Siddiqui,Sabahat Z; Shah,Syed Adnan Ali. |
| 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... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Acetohydrazides/ Synthesis; Acetohydrazides/Antibacterial activity/ Acetohydrazides/Lipoxygenase/inhibition activity.. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000300471 |
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