scholarly journals A Facial Synthesis and Antimicrobial Activity of Some Pyrazole Derivatives Carrying Indole

2010 ◽  
Vol 7 (3) ◽  
pp. 745-750 ◽  
Author(s):  
K. Narasimha Sarma ◽  
M. C. S. Subha ◽  
K. Chowdoji Rao
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Carboxylic Acid ◽  
Hydrazine Hydrate ◽  
Elemental Analysis ◽  
Antimicrobial Activities ◽  
Subsequent Treatment ◽  
Spectral Studies ◽  
Pyrazole Derivatives

The title compounds (7a-h) were prepared by esterification of indole-5-carboxylic acid (1) and subsequent treatment with hydrazine hydrate in methanolviathe hydrazide (3). Finally hydrazide (3) condensed with different substituted aldol (6) in acetic acid / PTSA catalytic media produced (3,5-subsituted-4,5-dihydropyrazol-1-yl)(1H-indol-5-yl)methanone (7a-h) in good yields. All the newly synthesized compounds are by elemental analysis and spectral studies and evaluated for antimicrobial activities.

scholarly journals Microwave Irradiative Synthesis of Triazine Substituted Pyrazoles and Study of Antitubercular and Antimicrobial Activities

2019 ◽  
Vol 31 (5) ◽  
pp. 1087-1090 ◽  
Author(s):  
Pradip P. Deohate ◽  
Roshani S. Mulani
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Structural Investigation ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Gram Negative ◽  
Mass Spectral ◽  
The Relationship ◽  
Substituted Pyrazoles ◽  
Structure And Activity

Microwave irradiative synthesis of triazine substituted pyrazoles i.e. (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted benzoyl/isonicotinoyl/cinnamoyl-pyrazol-3-yl)-amines have been achieved by the cyclocondensation of N-(4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-3-oxo butyramide with substituted acid hydrazides. Synthesis of required butyramide was done by reacting 2,4-diamino-6-methyl-[1,3,5]-triazine with benzaldehyde and then condensing the product with ethyl acetoacetate. Structural investigation of synthesized compounds has been done by chemical transformation, elemental analysis and IR, 1H NMR, mass spectral studies. Study of antitubercular and antimicrobial activity of title compounds against some selected Gram-positive and Gram-negative microorganisms was performed to establish the relationship between structure and activity of compound.

Synthesis of Novel Tetra-Substituted Pyrazole Derivatives from 2,3- Furandione

2019 ◽  
Vol 16 (11) ◽  
pp. 891-897 ◽  
Author(s):  
Hasan Genç ◽  
Volkan Taşdemir ◽  
İsrafil Tozlu ◽  
Erdal Ögün
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Solid State ◽  
Carboxylic Acid ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Gram Positive Bacteria

Synthesis of pyrazole-3-carboxylic acid was progressed via two different protocols, one of which is solid state. Pyrazole-3-carboxylic acid was converted into different derivatives such as ester, urea, amide and nitrile. The amide compound was converted to nitrile using SOCl2 and DMF. Solid state heating of carboxylic acid gave decarboxylated product. Cyclization of tetra-substituted pyrazole with hydrazines resulted in pyrazolopyridazinones. The antimicrobial activities of the synthesized pyrazole derivatives against Bacillus cereus, Escherichia coli, Micrococcus luteus, Staphylococcus aureus, and Saccharomyces cerevisiae were evaluated. One of the pyrazole derivatives which possess nitro group showed antimicrobial activity in only B. cereus, a Gram-positive bacteria, with an MIC of 128 μg/mL.

scholarly journals Synthesis of new derivatives of 1-(3-amino-phenyl)-4- benzoyl-5-phenyl-1h-pyrazole-3-carboxylic acid

2010 ◽  
Vol 75 (12) ◽  
pp. 1625-1635 ◽  
Author(s):  
Rahmi Kasimogullari ◽  
Belma Zengin ◽  
Makbule Maden ◽  
Samet Mert ◽  
Cavit Kazaz
Keyword(s):  
Carboxylic Acid ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Mass Spectroscopy ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Pyrazole Derivatives ◽  
Cyclocondensation Reaction ◽  
Derivatives Of

4-Benzoyl-1-(3-aminophenyl)-5-phenyl-1H-pyrazole-3- carboxylic acid (1) was synthesized according to the literature.1 2-(3- Aminophenyl)-3,4-diphenyl-2H-pyrazolo[3,4-d]pyridazin-7(6H)-one (5) was obtained by the cyclocondensation reaction of 1 with hydrazine hydrate. New pyrazole derivatives of compounds 1 and 5 were synthesized by their reaction with ?-diketones, ?-ketoesters, ?-naphthol, phenol and various other reagents. The structures of the synthesized compounds were characterized by 1H-NMR, 13C-NMR, IR and Mass spectroscopy, as well as elemental analysis.

Synthesis of Novel Oxazin Analogs of Thio-4-azaspiro[4.5]decan-3-one for their Antimicrobial Activity

2021 ◽  
Vol 6 (2) ◽  
pp. 116-120
Author(s):  
Raj Bahadur Singh ◽  
Krishna Srivastava ◽  
Ram Prakash Tiwari ◽  
Jyoti Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Absorption Spectroscopy ◽  
Elemental Analysis ◽  
Spectral Studies ◽  
Good Activity ◽  
Mass Spectral ◽  
E Coli

The present work reports the synthesis of 4-(1-(substituted phenyl)-1H-naphtho[1,2-e][1,3]oxazin- 2(3H)-yl)-1-thia-4-azaspiro-[4.5]-decan-3-one IV(a-h) by 4-(((substituted phenyl)(2-hydroxynaphthalen- 1-yl) ethyl)amino)-1-thia-4-azaspiro[4.5]decan-3-one with formaldehyde in acetonitrile, containing a spiro ring obtained from the reaction of cyclohexylidene hydrazine and thioglycollic acid in DMF (cyclohexanone reacts with hydrazine hydrate in pyridine). The structures of the synthesized compounds have been established on the basis of elemental analysis, UV-vis absorption spectroscopy, IR, 1H NMR and mass spectral studies. The in vitro antimicrobial screening of all novel compounds was done against S. aureus, E. coli, P. aeruginosa and B. subtilis. The activity of compounds IVb, IVc, IVe and IVf compounds showed moderate to good activity against the tested microbes.

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

scholarly journals Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives

2009 ◽  
Vol 1 (2) ◽  
pp. 317-325 ◽  
Author(s):  
M. I. Hossain ◽  
M. M. H. Bhuiyan
Keyword(s):  
Antimicrobial Activity ◽  
Formic Acid ◽  
Hydrazine Hydrate ◽  
Thionyl Chloride ◽  
Good Yield ◽  
Initial Treatment ◽  
Antimicrobial Activities

Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6  dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitrile 1 with formic acid, affording 5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one 2, which is chlorinated with thionyl chloride and then hydrazinated with hydrazine hydrate. Finally hydrazino compound 4 is reacted with formic acid, acetic anhydrate, benzaldehyde, p-hydroxybenzaldehyde, p-toluayldehyde, p-nitrobenzaldehyde and p-chlorobenzaldehyde to give thienotriazolopyrimidines 5-6 and thienopyrimidines 7-11 respectively. All the compounds have been screened for their antimicrobial activity. Keywords: Fused pyrimidines; Hydrazino compound; Thienotriazolopyrmidines; Thienopyrimidines; Antimicrobial activity.© 2009 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.DOI: 10.3329/jsr.v1i2.2299

scholarly journals 6-[1-Acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-yl]-2(3H)-benzoxazolone

Molbank ◽  
10.3390/m1021 ◽  
2018 ◽  
Vol 2018 (4) ◽  
pp. M1021
Author(s):  
Yordanka Ivanova ◽  
Antonya Todorova ◽  
Christo Chanev ◽  
Ognyan Petrov
Keyword(s):  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Title Compound ◽  
Target Compound

The title compound, 6-[1-acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl]-2(3H)-benzoxazolone, was synthesized by condensation of 6-[3-(4-methoxyphenyl)-2-propenoyl]-2(3H)-benzoxazolone (1) and hydrazine hydrate in acetic acid in 84% yield. The structure of the target compound was confirmed using 1H-NMR, 13C-NMR, IR, MS, and elemental analysis.

scholarly journals Syntheses, Characterization, Crystal Structures and Antimicrobial Activity of Schiff Base Copper(II) Complexes Derived from 2-Bromo-6-((2-(isopropylamino) ethylimino)methyl)phenol

2021 ◽  
Vol 68 (4) ◽  
pp. 1008-1015
Author(s):  
Yong Yuan ◽  
Xi-Kun Lu ◽  
Gao-Qi Zhou ◽  
Xiao-Yang Qiu
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Single Crystal ◽  
Elemental Analysis ◽  
Structure Determination ◽  
Antimicrobial Activities ◽  
X Ray ◽  
Zwitterionic Form ◽  
Square Planar ◽  
Vis Spectroscopy

Three new copper(II) complexes, [Cu(LH)2]Br2 (1), [Cu(LH)2]NCS2 (2), and [Cu(LH)2](NO3)2 (3), where LH is the zwitterionic form of 2-bromo-6-((2-(isopropylamino)ethylimino)methyl)phenol (HL), were synthesized and characterized by elemental analysis, IR and UV-vis spectroscopy. The structures of the complexes were further confirmed by single crystal X-ray structure determination. All compounds are mononuclear copper(II) complexes. The Cu atoms in the complexes are coordinated by two imino N and two phenolate O atoms from two LH ligands, forming square planar coordination. The compounds were assayed for their antimicrobial activities.

Synthesis, Characterization, Antimicrobial Screening of 5-Bromobenzofuranyl Aryl Ureas and Carbamates

2019 ◽  
Vol 4 (4) ◽  
pp. 232-235
Author(s):  
H.M. Naveena Kumari ◽  
Manjunath Harihara Mathada ◽  
Mahesh Kumar ◽  
K.T. Suda ◽  
K.M. Basavaraja
Keyword(s):  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
Sodium Nitrite ◽  
Potassium Carbonate ◽  
Anhydrous Potassium Carbonate ◽  
Antimicrobial Activities ◽  
Anhydrous Toluene ◽  
Ethyl Carbamate ◽  
Primary Amines ◽  
Antimicrobial Screening

Present work reports the biologically important benzofuran aryl ureas and carbamates. The benzofuran ring was formed by reacting bromo salicylaldehyde with diethyl bromomalonate in presence of dry acetone and anhydrous potassium carbonate to obtain 5-bromo-2-ethyl carboxylate (1). The obtained ester (1) was converted into corresponding hydrazide (2) by treating with hydrazine hydrate in ethanol. Compound 2 was then converted into 5-bromobenzofuran-2-carbonyl azide (3) by treating it with sodium nitrite in dioxane and acetic acid. The compound 3 is converted into 5-bromobenzofuranyl aryl ureas (4a-e) after treating primary amines and anhydrous toluene. 5-Bromobenzofuranyl aryl carbamate (5) and ethyl carbamate (6) were also synthesized by treating compound 3 with substituted phenol in toluene and ethanol respectively. All the compounds were characterized by NMR, IR and screened for antimicrobial activities.

scholarly journals Synthesis, Characterization and Chelating Properties of 4-Butyrylsemicarbazone-1-phenyl-3-methyl-2-pyrazolin-5-one

2010 ◽  
Vol 7 (2) ◽  
pp. 357-362 ◽  
Author(s):  
J. D. Patel ◽  
P. J. Shah
Keyword(s):  
Antimicrobial Activity ◽  
Magnetic Properties ◽  
Elemental Analysis ◽  
Metal Chelates ◽  
Spectral Studies

4-Butyrylsemicarbazone-1-phenyl-3-methyl-2-pyrazolin-5-one (BUMP-SC) was prepared and its metal chelates of Cu2+, Ni2+, Co2+, Mn2+, Fe2+, Fe3+, Cr3+, UO2and OV were prepared. The ligands and its chelates were characterized by elemental analysis, metal:ligand (M:L) stoichiometry, IR-electronic spectral studies and magnetic properties. The compounds also were screened for their antimicrobial activity.

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