scholarly journals AN EFFICIENT THREE COMPONENT ONE-POT SYNTHESIS OF -1,2,3,4-TETRAHYDRO-4-OXO- 6-(5-SUBSTITUTED 2-PHENYL-1H-INDOL-3-YL)-2-THIOXOPYRIMIDINE-5-CARBONITRILE AS ANTIMICROBIAL AND ANTITUBERCULAR AGENTS

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.

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.


2019 ◽  
Vol 31 (4) ◽  
pp. 965-970 ◽  
Author(s):  
Veerabhadrayya S. Negalurmath ◽  
Obelannavar Kotresh ◽  
Mahantesha Basanagouda

In the present study, a series of benzofuran-oxadiazole conjugates 7(a-o) was designed, synthesized and characterized through IR, 1H NMR, 13C NMR and mass spectral data. All the compounds were screened for preliminary antitubercular activity against Mycobacterium phlei and Mycobacterium tuberculosis H37RV. Among all the target compounds, the compound possessing chlorine (7k, MIC 1.56 μg/mL) and bromine (7m, MIC 1.56 μg/mL) on 6th position of benzofuran showed highest activity against Mycobacterium phlei. Whereas, bromine on either 5th position (7l, MIC 3.125 μg/mL) or 6th position (7m MIC 3.125 μg/mL) on benzofuran exhibited highest activity for Mycobacterium tuberculosis (H37 RV).


2010 ◽  
Vol 64 (5) ◽  
Author(s):  
Abd Khalil ◽  
Moged Berghot ◽  
Moustafa Gouda

AbstractDibenzobarrelene (I) was used as a starting compound for the synthesis of some new 3a,4,9,9a-tetrahydro-4,9-[1,2]benzeno-1H-benzo[f]isoindole-1,3(2H)-diones, N-substituted with: 4-toluenesulfonyloxy, III; butoxy, IV; 3-bromopropoxy, V; 3-(4-phenylpiperazin-1-yl)propoxy, VI; 3-chloro-3-oxopropyl, VIII; 3-(4-phenylpiperazin-1-yl)-3-oxopropyl, IXa; 3-(4-methylpiperazin-1-yl)-3-oxopropyl, IXb; 3-oxo-3-(piperidin-1-yl)propyl, X; 3-morpholino-3-oxopropyl, XI; 3-phenylamino-3-oxopropyl, XII; 2-acetylaminoethyl, XIV; 2-aminoethyl, XV, and 2-acetoxyethyl, XVI. Newly synthesized compounds were characterized by IR, 1H and 13C NMR, and mass spectral data. Selected products were tested for antimicrobial activity.


2009 ◽  
Vol 74 (7) ◽  
pp. 733-743 ◽  
Author(s):  
T. Karabasanagouda ◽  
Vasudeva Adhikari ◽  
G. Parameshwarappa

A series of new 4-aryl-2'-[(4-hydroxyphenyl)thio]-6oxo-1,6-dihydro- 2,4'-bipyridine-5-carbonitriles (3a-k) and 6-amino-4aryl-2'-[(4-hydroxyphenyl) thio]-2,4'-bipyridine-5-carbonitriles (4a-h) were synthesized from 4-hydroxythiophenol (1). The reaction of 4-hydroxythiophenol with 4-acetyl-2-chloropyridine yielded 1-{2-[(4-hydroxyphenyl)thio]pyridin-4-yl}ethanone (2). Further treatment of 2 with ethyl cyanoacetate in the presence of ammonium acetate with various aromatic aldehydes furnished the compounds 3a-k. On the other hand, condensation of 2 with aromatic aldehydes in the presence of alcoholic malononitrile in ammonium acetate gave compounds 4a-h. The structures of the newly synthesized compounds were established on the basis of their elemental analysis, as well as their IR, 1H- and 13C-NMR and mass spectral data. All the title compounds were subjected to in vitro antibacterial testing against two strains and antifungal screening against two fungi. Some of the compounds showed promising activity.


Molbank ◽  
10.3390/m1187 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1187
Author(s):  
Stanimir Manolov ◽  
Iliyan Ivanov ◽  
Dimitar Bojilov

The title compound was obtained in high yield in the reaction between tryptamine and naproxen. The newly synthesized naproxen derivative was fully analyzed and characterized via 1H, 13C-NMR, UV, IR, and mass spectral data.


Molbank ◽  
10.3390/m1199 ◽  
2021 ◽  
Vol 2021 (2) ◽  
pp. M1199
Author(s):  
Milene A. G. Fortunato ◽  
Filipa Siopa ◽  
Carlos A. M. Afonso

Using environmentally friendly conditions, the nucleophilic ring-opening reaction of 6-azabicyclo[3.1.0]hex-3-en-2-ol with 1-methyl-1H-tetrazole-5-thiol provided a novel thiol-incorporated aminocyclopentitol, (1R,4S,5S)-5-((3-hydroxypropyl)amino)-4-((1-methyl-1H-tetrazol-5-yl)thio)cyclopent-2-en-1-ol, in excellent yield (95%). The newly synthesized compound was analyzed and characterized via 1H, 13C-NMR, HSQC, and mass spectral data.


2021 ◽  
Vol 33 (8) ◽  
pp. 1723-1728
Author(s):  
Ramachandraiah Dasari ◽  
Gangadhar Thalari ◽  
Jayaprakash Rao Yerrabelly ◽  
Prasad Rao Chitneni

A new series of 4-phenyl-2H-chromene-3-benzimidazoles (8a-o) were synthesized by the condensation of 4-phenyl-2H-chromene-3-carbaldehyde with o-phenylene diamines. The products were purified through column chromatography and structures of these compounds were characterized by IR, 1H & 13C NMR and mass spectral data. All the final compounds were screened for their antimicrobial activity and their efficacy were matched with ciprofloxacin. Five compounds (8b, 8d, 8i, 8l and 8o) were found to be most effective compounds of this series and with activities improved than ciprofloxacin under the tested conditions


2008 ◽  
Vol 3 (2) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Ahmed Elkhateeb ◽  
Masahiro Yamasaki ◽  
Yoshimitsu Maede ◽  
Ken Katakura ◽  
Kensuke Nabeta ◽  
...  

The medicinal plant Brucea javanica (L.) Merr. (Simaroubaceae), grown in China, was examined for anti-babesial properties. The anti-babesial activity of the fruit was found to be attributed to its quassinoid constituents. Ten active compounds were isolated and purified from a chloroform extract. The identities of these compounds were confirmed from NMR spectroscopic and mass spectral data as brusatol (1), bruceantin (2), bruceine A (3), bruceantinol (4), dehydrobruceine B (5), dehydrobrusatol (6), dehydrobruceine A (7), bruceine D (8), bruceoside A (9), and yadanzioside G (10). When tested in vitro against Babesia gibsoni, compounds 1–10 had IC50 values of 0.74, 13.4, 4.0, 12.0, 308.2, 10.5, 835.0, >1000, and >1000 ng/mL, respectively. Compounds 1–4, 6 and 7 had far higher activity than the commercial anti-babesial drug diminazene aceturate, which possesses an IC50 value of 70.5 ng/mL. Except for bruceine A (3), bruceantinol (4) and bruceine D (8), this is the first report of the anti-babesial activity of these isolated quassinoids.


2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.


Molbank ◽  
10.3390/m1031 ◽  
2018 ◽  
Vol 2018 (4) ◽  
pp. M1031
Author(s):  
Stanimir Manolov ◽  
Iliyan Ivanov ◽  
Yulian Voynikov

The compound in the title was prepared by reaction between tryptamine and ibuprofen using N,N′-dicyclohexylcarbodiimide as a “dehydrating” reagent. The structure of the newly synthesized compound was determined by nuclear magnetic resonance (NMR) (1H-NMR and 13C-NMR), UV, IR, and mass spectral data.


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