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

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.   

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.


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.


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.


2006 ◽  
Vol 10 (07) ◽  
pp. 996-1002 ◽  
Author(s):  
Ayhan Nazli ◽  
Ergün Gonca ◽  
Ahmet Gül

Magnesium porphyrazinate substituted with eight (1-naphthyl) groups on the peripheral positions has been synthesized by cyclotetramerization of 3,4-(1-naphthyl)pyrroline-2,5-diimine, 4-(1-naphthyl)pyrroline-2,5-diimine in the presence of magnesium butanolate. Its demetalation by treatment with trifluoroacetic acid, resulted in a partially oxidized product, namely, octakis(1-naphthyl)-2-seco-porphyrazine-2,3-dione. Further reaction of this product with copper(II) acetate, zinc(II) acetate and cobalt(II) acetate led to the metallo derivatives, [octakis(1-naphthyl)-2-seco-2,3-dioxoporphyrazinato]M(II) ( M = Cu , Zn or Co ). These new compounds have been characterized by elemental analysis, together with FT-IR, 1 H NMR, UV-vis and mass spectral data.


Author(s):  
Vijay N. Bhadani ◽  
Piyush A. Patel ◽  
Heta D. Purohit ◽  
Dipak M. Purohit

A series of an easy and efficient route for the synthesis of some new 2-amino-3-cyanopyridine (4a-4i) and 2-methoxy-3-cyanopyridine (5a-5i) derivatives were synthesized through the reaction of various chalcone (3a-3i) with malononitrile in presence of ammonium acetate and sodium methoxide, respectively. The constitutions of the all synthesized compounds have been established by the IR, 1H-NMR, Mass spectral data and Elemental analysis. Furthermore, all the synthesized products were screened for their antimicrobial activity.


2009 ◽  
Vol 6 (4) ◽  
pp. 1055-1062 ◽  
Author(s):  
Manish Srivastav ◽  
MD. Salahuddin ◽  
S. M. Shantakumar

A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with various substituted amine. The compounds (IIa-d) prepared by treating 2-[(chloroacetyl) amino] benzoic acid with different 2-amino-6-substituted benzothiazole. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolines-4-one derivative were investigated for their anti-inflammatory and antibacterial activity.


2002 ◽  
Vol 70 (3) ◽  
pp. 277-286 ◽  
Author(s):  
Khan M.S.Y. ◽  
Husain A. ◽  
Hasan S.M. ◽  
Akhter M.

Various amide-based prodrugs of sulphonamides have been synthesised by condensing appropriate sulphonamide moiety with different β-aroyl propionic acids. All the compounds have been evaluated for their antimicrobial and anti-inflammatory activities. Their structures were established on the basis of elemental analysis, 1H NMR and Mass spectral data. Some of these compounds were found to have significant activity


2020 ◽  
Vol 32 (8) ◽  
pp. 2007-2012
Author(s):  
Mahendra B. Bodake ◽  
Ghanshyam R. Jadhav ◽  
Vijay J. Medhane ◽  
Avinash D. Bholay

A series of new molecules containing pyrrolidine and thiazole moiety (4a-l) were designed and synthesized. The structures of the synthesized compounds were characterized by IR, 1H NMR and mass spectral data. All the synthesized compounds were screened for their antibacterial activity against strains of bacteria as well as antifungal activity against fungal strains. Minimum inhibitory concentrations (MICs) of all the synthesized compounds were determined. The screening of title compounds revealed that most of the tested compounds showed moderate to good microbial inhibitions


2019 ◽  
Vol 54 (2) ◽  
Author(s):  
Yu Lin Hu ◽  
Xiang Liu ◽  
Ming Lu

A series of 6-substituted purines were synthesized from commercially available 2-amino-6-chloropurine with appropriate reagents, and nine new compounds 7, 8, and 11-17 have been discovered. The compounds synthesized were identified by elemental analysis, 1H NMR, as well as mass spectral data. All the title compounds were screened for their antifungal activities, under the method of the disc diffusion, using three species of fungi — Bacillus subtillis, Aspergillus niger, and Candida tropicalis— and some of the compounds showed promising activities.


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 16-22
Author(s):  
N. Kumar ◽  
D Pathak ◽  

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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