scholarly journals Synthesis and selective antitubercular and antimicrobial inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1h)-pyrazole derivatives

2006 ◽  
Vol 71 (7) ◽  
pp. 713-720 ◽  
Author(s):  
P.T. Chovatia ◽  
J.D. Akabari ◽  
P.K. Kachhadia ◽  
P.D. Zalavadia ◽  
H.S. Joshi
Keyword(s):  
Hydrazine Hydrate ◽  
Antimycobacterial Activity ◽  
Antimicrobial Activities ◽  
Proteus Vulgaris ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Mycobacterium Tuberculosis H37rv ◽  
Aryl Ketones ◽  
New Compounds

The new compounds 1-aryl-3-{1-phenyl-3-[p (methylthio)phenyl]pyrazol-4-yl}-2-propen-1-ones 2a?l were prepared by the condensation of 1-phenyl-3-[p (methylthio)phenyl]-4-formylpyrazole 1 with different aryl ketones. Compounds 2a?l in reaction with hydrazine hydrate yielded 3-aryl-5-{1-phenyl-3-[p-(methylthio)phenyl]pyrazol-4 yl}-4,5-dihydro-(1H)-pyrazoles 3a?l and in the presence of hydrazine hydrate in glacial acetic acid gave 1-acetyl-3-aryl 5-{1-phenyl-3-[p-(methylthio)phenyl]pyrazol-4-yl}-4,5 dihydro-(1H)-pyrazoles 4a?l. These compounds were tested in vitro for their antitubercular and antimicrobial activities. The in vitro antimycobacterial activity of the newly synthesized compounds was investigated against Mycobacterium tuberculosis H37RV (ATCC 27294) in BACTEC 12B medium using the ALAMAR radiometric system. The antimicrobial in vitro activity was tested against Bacillus coccous, Bacillus subtilis Escherichia coli, Proteus vulgaris and antifungal activity against Aspergillus niger. The structures of the synthesized compounds were assigned on the basis of elemental analysis IR, 1H NMR and mass spectral data.

scholarly journals Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives

2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Mass Spectral Data ◽  
Pyrimidine Derivatives ◽  
Plate Method ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
New Compounds

The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidines 1a-j are compared with those of known chosen standard drugs, viz. ampicillin, chloramphenicol, ciprofloxacin, norfloxacin and griseofulvin. .

scholarly journals Synthesis of thiourea derivatives bearing the benzo[b]thiophene nucleus as potential antimicrobial agents

2005 ◽  
Vol 70 (6) ◽  
pp. 807-815 ◽  
Author(s):  
K.M. Thakar ◽  
D.J. Paghdar ◽  
P.T. Chovatia ◽  
H.S. Joshi
Keyword(s):  
Spectral Data ◽  
1H Nmr ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Thiourea Derivatives ◽  
Mass Spectral ◽  
New Compounds

The synthesis of a group of thiohydantoins and thiobarbiturates derived from 2-N-arylthiopyridocarbonyl-3,5-dichlorobenzo[b]thiophene is described. The structures of the new compounds are supported by IR, 1H-NMR and mass spectral data. These compounds were tested in vitro for their antimicrobial activities.

scholarly journals Synthesis, Antibacterial and Antifungal Evlaution of Novel Pyrazoline Derivatives

2018 ◽  
Vol 17 (2) ◽  
pp. 221-226
Author(s):  
BC Revanasiddappa ◽  
MS Jisha ◽  
M Vijay Kumar ◽  
Hemanth Kumar
Keyword(s):  
Good Activity ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Acetic Acid Medium ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Alcohol Medium ◽  
Antibacterial And Antifungal ◽  
New Compounds

A new series of chalcones (2a-j) were prepared by reacting substituted aldehydes and substituted ketones in alcohol medium in presence of NaOH. The chalcones underwent selective cyclization with guanicol hydrazide (1) in glacial acetic acid medium to yield the title compounds 1,3,5-trisubstituted pyrazolines (3a-j). The new compounds were characterized on the basis of 1H-NMR, IR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro antibacterial and antifungal activities. Some of the tested compounds 3a and 3e showed good activity against bacterial strains and compounds 3d and 3h revealed good activity against fungal strains. Dhaka Univ. J. Pharm. Sci. 17(2): 221-226, 2018 (December)

Synthesis, Characterization and Evaluation of Azetidinylquinolines and Thiazolidinylquinolines as Antibacterial Agents

2014 ◽  
Vol 7 (3) ◽  
pp. 2536-2543
Author(s):  
Shalabh Sharma ◽  
Kuldeep K Saxena
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Antibacterial Agents ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
New Compounds

Several molecules were synthesized like 8-ethoxy-4-methyl-2-amino-(3’-chloro-2’-oxo-4’-substitutedaryl-1’-azeti-dinyl)-quinolines 8-12 and 8-ethoxy-4-methyl-2-amino-(2’-substitutedaryl-4’-oxo-1’,3’-thiazolidin-3’-yl)quinolines 13-17 from 8-ethoxy-4-methyl-2-(substitutedarylidenylimino amino)-quinolines 3-7, and screened to evaluate their antibacterial activity against numerous strains of bacteria        in vitro. The structures of new compounds were established on the basis of their elemental analysis, IR, 1H-NMR and mass spectral data. The results showed that three compounds 10, 11 and 16 were found to exhibit promising antibacterial activity as compared to the standard drug amphicillin.   

SYNTHESIS AND EVALUATION OF ANTIOXIDANT ACTIVITY OF SOME KETONE DERIVATIVES OF GALLIC HYDRAZIDE DERIVED SCHIFF BASES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 56-62
Author(s):  
S. J Dighade ◽  
◽  
P. K. Parikh
Keyword(s):  
Nitric Oxide ◽  
Antioxidant Activity ◽  
Hydrazine Hydrate ◽  
Gallic Acid ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Anti Oxidant ◽  
Compound Ii ◽  
Derivatives Of

In the present study, a new series of 3,4,5-trihydroxy-N’-(1-phenylethylidene) benzohydrazide (III) has been synthesized. Methyl 3,4,5 trihydroxy benzoate (I) was synthesized from gallic acid and methanol in presence of conc. sulphuric acid. Intermediate, 3,4,5 trihydroxy benzohydrazide (II) was synthesized by reacting methyl 3,4,5 trihydroxy benzoate and hydrazine hydrate. The final compounds (IIIa-e) were synthesized by reacting compound (II) with various substituted acetophenones in presence of ethanol. The synthesized compounds have been characterized by IR, 1HNMR and Mass spectral data. The compounds were evaluated for in vitro anti-oxidant activity by DPPH and nitric oxide method. In general all compounds were found to exhibit good anti-antioxidant activity.

scholarly journals Design, synthesis and antimycobacterial evaluation of some new azaheterocycles with the 4,7-phenanthroline skeleton. Part VI

2016 ◽  
Vol 81 (2) ◽  
pp. 133-140 ◽  
Author(s):  
Matarneh Al ◽  
Catalina Ciobanu ◽  
Ionel Mangalagiu ◽  
Ramona Danac
Keyword(s):  
Antimycobacterial Activity ◽  
Alkylation Reaction ◽  
Design Synthesis ◽  
1H And 13C Nmr ◽  
Mycobacterium Tuberculosis H37rv ◽  
13C Nmr Analysis ◽  
New Compounds ◽  
Feasible Study ◽  
Influence Of Substituents

A feasible study concerning the synthesis, structure and in vitro antimycobacterial evaluation of new 4,7-phenanthroline derivatives is reported. The preparation is straight and efficient, involving an N-alkylation reaction of 4,7-phenanthroline. The structure of the new compounds have been proved by elemental and spectral (IR, 1H and 13C NMR) analysis. The in vitro antimycobacterial evaluation of five synthesized compounds was investigated against Mycobacterium tuberculosis H37Rv under aerobic conditions. A certain influence of substituents from the para position of the benzoyl moiety was observed, the 4,7-phenanthrolin-4-ium salt substituted with (p)chloro-benzoyl showing the most pronounced antimycobacterial activity.

scholarly journals Novel Antimicrobial Agents: Fluorinated 2-(3-(Benzofuran-2-yl) pyrazol-1-yl)thiazoles

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Hanan A. Mohamed ◽  
Ehab Abdel-Latif ◽  
Bakr F. Abdel-Wahab ◽  
Ghada E. A. Awad
Keyword(s):  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Elemental Analyses ◽  
Test Organisms ◽  
New Compounds

A new series of 2-pyrazolin-1-ylthiazoles 8a–d and 13–16 was synthesized by cyclization of N-thiocarboxamide-2-pyrazoline with different haloketones and 2,3-dichloroquinoxaline. The structures of the new compounds were confirmed by elemental analyses as well as NMR, IR, and mass spectral data. The newly synthesized compounds were evaluated for their antimicrobial activities, and also their minimum inhibitory concentration (MIC) against most of test organisms was performed. Amongst the tested ones, compound 8c displayed excellent antimicrobial activity.

scholarly journals Green Synthetic Protocol for (E)-1-Aryl-3-(2-morpholinoquinolin- 3-yl)prop-2-en-1-ones and Their Antimicrobial Activity

2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
13C Nmr ◽  
Mass Spectral Data ◽  
In Vitro Antimicrobial Activity ◽  
Mass Spectral ◽  
Fungal Organisms

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.

scholarly journals Synthesis and antimicrobial activities of novel n-substituted 8-(1-alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5-chloroquinolines

2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nitrogen Heterocycles ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Electrophilic Reagents ◽  
Almost All ◽  
And Staphylococcus Aureus

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NEWER BENZIMIDAZOLE DERIVATIVES BY MANNICH REACTION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 16-22
Author(s):  
N. Kumar ◽  
D Pathak ◽  
Keyword(s):  
Salicylic Acid ◽  
Elemental Analysis ◽  
Mannich Reaction ◽  
Anthelmintic Activity ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Good Activity ◽  
Mass Spectral Data ◽  
Mass Spectral

O-phenylenediamine and salicylic acid were used for the synthesis of 2-(1-(substituted phenylamino) methyl-1H benzo[d] imidazol-2-yl) phenol (2a-2h) derivatives by using various substituted aniline. In the first step, reaction of o-phenylenediamine and salicylic acid yielded 2-(1H-benzo[d]imidazol-2-yl) phenol (1), which on Mannich reaction with substituted aniline gave compounds (2a-2h). The structures of these compounds were characterized by IR, 1H NMR, mass spectral data and elemental analysis. Each analogue was tested in vitro for various types of pharmacological activity of this class of drugs including antibacterial, antifungal and anthelmintic activity. Among the synthesized compounds 2a act as vermifuge and no compound was found to be a vermicide. The compound 2c was found to be most active against E.coli and P. aeurigenosa and 2e be most active against B.subtilis and S.aureus. The derivative 2h shows good activity against C.albicans and A.niger.

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