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Introduction:.  JesusIntroduction:Pyrimidinones areremarkable scaffolds having wide range of biological importance.thiamine,uracil and  cytocine arepyrimidine bases and they are found in DNA and RNA respectively which playsvital role in biological  cell function .In recent years dihydropyrimidinones received more attention because theyexhibit wide range of biological and therapeutic activities such as anti tumor,anti viral, antimicrobial, anti-inflammatory activities1, potentcalcium channel modulators, anti hypertensive agents and neuropeptide Y (NPY)antagonists 2.dihydropyrimidinone also found in many marine natural products includingBetzelladine is an alkaloid which process HIVgp-120-CD4 inhibitingactivity3.Biginellireaction is the classical example for single pot multi-component reactioninvolving cyclocondensation of an aldehyde, active methelene group containgcompounds (?-keto ester, acetyl acetone..

,etc.). and urea in presence of acid4.EXPERIMENTALPART:MATERIALS ANDMETHODS: All the chemicals used in the synthesis were procured from SigmaAldrich. TLC plates for monitoring of reactions and silica gel (100-200 mesh)for column chromatography obtained from Merck.

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The Melting points weredetermined by using EZ-Melt automated melting point apparatus.  The FT-IR spectra were recorded on BRUKERALPHA-T FT.IR spectrophotometer using KBr pellet method. The Mass spectra wererecorded on Agilent 6320 Ion Trap LC-MS (Positive/Negative ion electro sprayionization method). The 1H NMR spectra of the compounds were recorded on BRUKER400 MHz NMR Spectophotometer.

Step: 1 synthesis of Dihydro pyrimidinonederivatives:A mixture of Aldehyde(10mmol),acetylacetone(11mmol),urea(13mmol) and citric acid (5mmol) were taken in a roundbottomed flask and refluxed for 6-12 hours at 800C. After completionof reaction as monitored by TLC, obtained crude product was transferred into a  beaker containing crushed ice, filtered,washed with ice cold water and recrysteallized using ethanol. spectral data of synthesied compound IR: 1688.73(C=O), 3333. 80(NH), 1124.11(OC2H5),1607.42(C=C), 1240.38(C-N)NMR: 1.

34(3H,CH3); 2.06 (3H,CH3 S); 2.27 (3H,COCH3 S );4.01(2H, OCH2);5.

18 (1H, C-H); 6.83(1H Ar –H S);6.62(1H,Ar-H); 6.

60(1H,Ar-H);9.09(1H,CONH); 8.85 (1H,OH);7. 69 (1, NH) Step:2 synthesis of chalcones of dihydropyrimidinones: A mixture ofcompound j(1mmol), aldehydes(1mmol) and ethanol(to soluble the contents) weretaken in a beaker and to that add 10 ml of 30% aqueous solution of NaOH andthen subjected to stirring up to 48 hours reaction was monitored by TLC. Aftercompletion of the reaction, reaction mixture was poured on to ice cold waterand acidified with dil.HCl.

Then obtained solid was filtered,washed with waterand obtained products were purified by column chromatography.IR :1688.73(C=O), 3333. 80(NH), 1124.11(OC2H5),1607.42(C=C), 1240.38(C-N)NMR: 1.34(3H,CH3); 2.

06 (3H,CH3 S); 2.27 (3H,COCH3 S );4.01(2H, OCH2);5.18 (1H, C-H); 6.83(1H Ar –H S);6.62(1H,Ar-H); 6.60(1H,Ar-H);9.

09(1H,CONH); 8.85 (1H,OH);7. 69 (1, NH)COMPOUND2             S.no stracture IUPAC name 1 a   2 b   3 c   4 d   5 e   6 f   7 g   8 h   9 i   10 j         s.

no Compound   code Structures IUPAC name 11 2a     12 2b     13 2c       14 2d     15 2e                ANTIBACTERIALACTIVITYTESTORGANISM :Grampositive:StaphylococcusaureusGramnegative:EscherichiacoliAntimicrobial activity was determined byusing agar cup plate method.The tested organism were sub cultured on nutrientagar medium for bacteria Ampicillinwas used as reference drug for bacterial strain.The medium used for theantibacterial study has the following composition g/L:Peptone, ; Beefextract, ; sodium chloride; and agar in distilled water  pH was adjusted at 7. Bacterial culture wasincubated at 37? C for 24 h.The solution of the test compounds were prepared bydissolving 0.5mg/1ml and 1mg/10ml of dimethylsulfoxide at a concentration of100µg/50µl and 250µg/50µl. The cups each of 10 in diameter were made byscooping out medium with a sterilized cork borer in a Petri.

The solutions ofeach test compound (50 µL) were added separately in the cups and petri disheswere subsequently incubated at 37 0C for 24 hours. Zone of inhibition producedby each compound was measured in . Compounds were screened for theirantibacterial activity.Test results: S.NO COMPOUNDS                         Zone of inhibition(mm) Staphylococcus aureus Escherichia coli 50µg/ml 100 µg/ml 50µg/ml 100µg/ml 1 1a 10 12 12 13 2 1b 10 13 – 10 3 1c 11 14 13 18 4 1d 13 15 11 15 5 1e 11 16 15 16 6 1f 11 13 11 14 7 1g 12 14 12 17 8 1h 13 17 15 17 9 1i 12 14 13 14 10 1j 11 13 10 12        11 2a 14 16 15 16 12 2b 15 17 16 17 13 2c 15 18 16 19 14 2d 15 18 15 19 15 2e 14 17 14 17 16 Ampicillin 17 19 19 21  Results and discussions:All the dihydropyrimidinonene derivatives(1a-1j) and their chalcones(2a-2e)were evaluated for their antibacterialagainst both gram positive (Staphylococcus areus) and gram negative (E.

coli),by using cup plate method. The results of antibacterial activity were given intable no: interestingly all the synthesized dihydropyrimidinone derivativeswere shown mild to moderate antibacterial activity at 50µg/ml and 100µg/mlconcentration , when compared with the standard drug (Ampicillin) at sameconcentrations . Compounds 1c, 1e, 1i, 2c and 2d were shown good antibacterialactivity against both gram positive and gram negative organisms.

 ANTIFUNGAL ACTIVITYTest  Organism:Aspergillus nigerAntifungal activity was determined byusing agar cup plate method. The tested organism Aspergillus niger was sub cultured on potato-dextrose agar (PAD) for fungi. Fluconazole was used as positivecontrol for fungi. Fungal culture was incubated at 25-30 0C for 4-5 days. .

Thesolution of the test compounds were prepared by dissolving /1ml and 5mg/1ml ofdimethylsulfoxide at a concentration of 50µg/1ml and 100µg/1ml. The cups eachof 10 in diameter were made by scooping out medium with a sterilized cork borerin a Petri dish. The solutions of each test compound (50µL) were addedseparately in the cups and petri dishes were subsequently incubated incubatedat 25-30 0C for 4-5 days.. Zone of inhibition produced by each compound wasmeasured in .

Compounds was screened for their antifungal activity.All the dihydropyrimidinonenederivatives (1a-1j) and their chalcones(2a-2e)were evaluated for theirantibacterial against both gram positive (Staphylococcus areus) and gramnegative (E.coli), by using cup plate method. The results of antibacterialactivity were given in table no: interestingly all the synthesizeddihydropyrimidinone derivatives were shown mild to moderate antibacterialactivity at 50µg/ml and 100µg/ml concentration , when compared with thestandard drug (Ampicillin) at same concentrations . Compounds 1c, 1e, 1i, 2cand 2d were shown good antibacterial activity against both gram positive andgram negative organisms.

 Results and discussions:All the dihydropyrimidinonenederivatives (1a-1j) and their chalcones(2a-2e)were evaluated for theirantifungal acticity against  Aspargillusniger, by using cup plate method. The results of antifungal activity were givenin table no: it is noticed that all the synthesized dihydropyrimidinonederivatives were shown mild to moderate antifungal activity at 50µg/ml and100µg/ml concentration , when compared with the standard drug (Fluconazole) atsame concentrations . Compounds 1c, 1i,2b and 2d were shown goodantifungal activity.               S.NO COMPOUNDS Zone of inhibition(mm) Asparagillus niger 50 µg/ml 100 µg/ml 1 1a 13 15 2 1b 14 16 3 1c 16 20 4 1d 16 18 5 1e 14 16 6 1f 15 18 7 1g 15 17 8 1h 15 20 9 1i 15 16 10 1j 14 16 11 2a 17 19 12 2b 17 23 13 2c 16 20 14 2d 17        22 15 2e 17 20 16 Fluconozole 22 25                  

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