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2-Phenitidine derivatives as suitable inhibitors of butyrylcholinesterase BJPS
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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Augmented cytotoxic, mutagenic and genotoxic response triggered by carvedilol and celecoxib combinations BJPS
Attiq,Ali; Ashraf,Muhammad; Jalil,Juriyati; Javeed,Aqeel; Anjum,Aftab Ahmad; Ullah,Asad; Umair,Muhammad; Ali,Sarwat.
Abstract It is understood that drugs regardless of their order of administration can exhibit drug interactions. Established on the fact that treatment of hypertension may last for decades and prolong usage of multiple drug regimen may induce substantial pathophysiological changes. Hence, This study was designed to evaluate the possible synergistic toxic effects of anti-hypertensive (carvedilol), and anti-inflammatory drug (celecoxib) alone and in combinations. Well-established MTT assay, Single Cell Gel Electrophoresis (SCGE) and Ames assay were employed to evaluate the toxicity at cellular level. Results from MTT assay on Vero cell line revealed that drug combinations have more pronounced anti-proliferative activity with combine IC50 value of 13.7:47.8...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Carvedilol; Celecoxib; Mutagenicity; Genotoxicity; Cytotoxicity..
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000100622
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Convergent synthesis of new N -substituted 2-{[5-(1H -indol-3-ylmethyl)-1,3,4-oxadiazol-2-yl]sulfanyl}acetamides as suitable therapeutic agents BJPS
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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Safety and efficacy of ketamine xylazine along with atropine anesthesia in BALB/c mice BJPS
Jamal,Muhammad Ameen; Ahmed,Arslan Mahmood; Tahir,Muhammad; Ashraf,Muhammad; Sattar,Abdul; Ghafoor,Aamir; Munir,Shahzad; Ahmed,Irfan; Hussain,Mubashir; Riaz,Amjad.
Anesthetics are an indispensable prerequisite for surgical intervention and pharmacological animal studies. The objective of present study was to optimize the dose of ketamine (K) and xylazine (X) along with atropine sulfate (A) in order to achieve surgical tolerance in BALB/c mice. Several doses of ketamine (100, 150, 200 mg/kg) and xylazine (10, 15, 20 mg/kg) were mixed and combination of nine doses (K/X: 100/10, 100/15, 100/20, 150/10, 150/15, 150/20, 200/10,200/15,200/20) were evaluated (n=9 per combination). A constant dose of atropine (0.05 mg/kg) was also used to counter side effect. Time-related parameters were evaluated on the basis of reflexes. KX at dose 200/20 mg/kg produced surgical tolerance in all nine mice with duration 55.00±6.87 minutes....
Tipo: Info:eu-repo/semantics/article Palavras-chave: Ketamine hydrochloride; Xylazine hydrochloride; Atropine sulfate; Surgical tolerance; BALB/c mice.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100556
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Salt tolerance and regulation of gas exchange and hormonal homeostasis by auxin-priming in wheat PAB
Iqbal,Muhammad; Ashraf,Muhammad.
The objective of this work was to assess the regulatory effects of auxin-priming on gas exchange and hormonal homeostasis in spring wheat subjected to saline conditions. Seeds of MH-97 (salt-intolerant) and Inqlab-91 (salt-tolerant) cultivars were subjected to 11 priming treatments (three hormones x three concentrations + two controls) and evaluated under saline (15 dS m-1) and nonsaline (2.84 dS m-1) conditions. The priming treatments consisted of: 5.71, 8.56, and 11.42 × 10-4 mol L-1 indoleacetic acid; 4.92, 7.38, and 9.84 × 10-4 mol L-1 indolebutyric acid; 4.89, 7.34, and 9.79 × 10-4 mol L-1 tryptophan; and a control with hydroprimed seeds. A negative control with nonprimed seeds was also evaluated. All priming agents diminished the effects of salinity...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Triticum aestivum; Hormonal balance; Plant growth regulators; Salinity; Seed priming; Stomatal regulation.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-204X2013000900004
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Synthesis and in silico study of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives as suitable therapeutic agents BJPS
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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Synthesis of new 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl) sulfonyl]amino}-N-(un/substituted-phenyl)acetamides as α-glucosidase and acetylcholinesterase inhibitors and their in silico study BJPS
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
Registros recuperados: 7
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