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

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.

Author(s):  
Shalabh Sharma ◽  
Kuldeep K Saxena

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.   


2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

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.


2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah

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. .


2006 ◽  
Vol 71 (7) ◽  
pp. 713-720 ◽  
Author(s):  
P.T. Chovatia ◽  
J.D. Akabari ◽  
P.K. Kachhadia ◽  
P.D. Zalavadia ◽  
H.S. Joshi

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.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Hanan A. Mohamed ◽  
Ehab Abdel-Latif ◽  
Bakr F. Abdel-Wahab ◽  
Ghada E. A. Awad

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.


2012 ◽  
Vol 25 (1) ◽  
pp. 62-70 ◽  
Author(s):  
Md Anwarul Hoque ◽  
Md Arzu Miah ◽  
Md Nurul Abser ◽  
Abul K Azad ◽  
Kamrun N Khan ◽  
...  

Treatment of 2-Mercaptothiazoline, 2-Mercaptobenzimidazole, 2-Mercapto-1- methylimidazole with [M2(CO)10] (M = Re and Mn) at ambient temperature in presence of decarbonylating reagent Me3NO give the complexes [Mn2(?-?2-C3H4NS2)2(CO)6] (1), [Re2(?-?2-C3H4NS2)2(CO)6] (2), [Mn2(?-?2-C7H5SN2)2(CO)6] (3), [Re2(?-?2- C7H5SN2)2(CO)6] (4), [Re2(?-?2-C4H5N2S)2(CO)6] (5) and [Re2(?1-C4H5N2SH)(CO)9] (6) respectively. All the compounds have been characterized by IR, 1H NMR and mass spectral data. The heterocyclic ligands are expected to be coordinated to two or single metal atom through the nitrogen and sulfur atoms or via only sulfur atom.DOI: http://dx.doi.org/10.3329/jbcs.v25i1.11775 Journal of Bangladesh Chemical Society, Vol. 25(1), 62-70, 2012> 


2006 ◽  
Vol 60 (1) ◽  
Author(s):  
I. Malík ◽  
E. Sedlárová ◽  
J. Csöllei ◽  
F. Andriamainty ◽  
P. Kurfürst ◽  
...  

AbstractThe phenylcarbamic acid derivatives with N-phenylpiperazine moiety in the molecule have been prepared. The structure has been confirmed by elemental analysis, IR, 1H NMR, and mass spectral data. For the prepared set of the compounds the lipophilicity parameters have been determined. The experimentally obtained lipophilicity parameters have been correlated with theoretical entries obtained by different computer programs based on the neural network and fragmental methods.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.


2021 ◽  
Vol 68 (2) ◽  
pp. 395-403
Author(s):  
Nataliia Krasovska ◽  
Viktor Stavytskyi ◽  
Inna Nosulenko ◽  
Oleksandr Karpenko ◽  
Oleksii Voskoboinik ◽  
...  

The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-с]quinazolines that were used as initial compounds for chemical modification aimed to the introduction of amide fragment to the molecule. The IR, 1H NMR and chromato-mass spectral data of obtained compounds were studied and discussed. Obtained substances were studied for anti-inflammatory activity using carrageenan-induced paw inflammation model. Amides of ([1,2,4]triazolo[1,5-с]quinazoline-2-yl)alkyl carboxylic acids were detected as promising class of anti-inflammatory agents for further purposeful synthesis and profound study of anti-inflammatory activity.


Author(s):  
PRABHAKER WALMIK

Objective: The objective of the study was to synthesis of 1,2,3,4-tetrahydro-4-oxo-6-(5-substituted 2-phenyl-1H-indol-3-yl)-2-thioxopyrimidine-5- carbonitrile derivatives (4a-c). Methods: The structures of all these unknown compounds have been confirmed with the help of physical and spectral techniques such as IR, 1H, and 13C NMR and mass spectral data and these newly synthesized compounds were evaluated for in-vitro antimicrobial and antitubercular activities. Results: Screening studies have demonstrated that the newly synthesized compound 4a exhibited promising antimicrobial and antitubercular properties. Conclusion: The final results revealed that compound 4a exhibited promising antimicrobial and antitubercular properties when compared to the standard drugs.


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