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Chapter – 6 Biological evaluation of newly..... ND = Not Done Sr. No. Representative Compound Bp Se Sp Sa1 1 DNJ-601 8 ND 32 8 2 DNJ-602 ND 8 8 4 3 DNJ-603 64 16 16 16 4 DNJ-604 32 ND ND >32 5 DNJ-605 16 32 8 8 6 Linezolid 4 4 4 2 6.1.3 RESULTS AND DISCUSSION From the above mentioned MIC values of antibacterial activity of DNJ- 101 to DNJ-111, it could be concluded that DNJ-101, DNJ-102, DNJ-104 and DNJ-108 were found to be highest potent with the MIC value of 0.5 µg/ml against the Bacillus pumilus MTCC 1607 and Staphylococcus epidermidis MTCC 155 respectively, which were having more inhibitory effect than the standard drug Linezolid. DNJ-102 to DNJ-111 were also found to have good inhibitory effect with the MIC value between 1-8 µg/ml on both of the bacterial strains. Thus it could be concluded that compounds having subunits like piperidine, morpholine, piperazine etc and alkyl chains having one to four carbons were found to possess good antibacterial activity. While DNJ-104, DNJ-109, DNJ-110 and DNJ-111 were found to be moderate active with the higher MIC values (i.e. >16, 16, 32 and >32 µg/ml respectively) against Staphylococcus pyogenes MTCC 442. DNJ-102 to DNJ- 104 and DNJ-107 to DNJ-109 were found to be moderate active with the higher MIC values (i.e. 16, 32, >16 µg/ml and >8, >32, 16 µg/ml) against Staphylococcus aureus MTCC 96. DNJ-105 to DNJ-107 were found to be moderate active with the higher MIC values (i.e. >16, 32 and 16 µg/ml) against Enterococcus faecalis MTCC 439. Thus rests of the compounds were found to be good active with the MIC value between 1-8 µg/ml against all the three bacterial strains. From above data it is clear that all the compounds are good active against Bacillus pumilus MTCC 1607 and Staphylococcus epidermidis MTCC 155 while they are moderate active against Department of Chemistry, Saurashtra University, Rajkot – 360 005 331
Chapter – 6 Biological evaluation of newly..... Staphylococcus pyogenes MTCC 442, Staphylococcus aureus MTCC 96 and Enterococcus faecalis MTCC 439. In case of second series of compounds (i.e. DNJ-201 to DNJ-210), only one compound DNJ-203 was found to possess highest potency and lowest MIC value (i.e. 0.5 µg/ml) against Bacillus pumilus MTCC 1607 which was having more inhibitory effect than the standard drug Linezolid. Thus the compound possessing trifluoromethyl group has more inhibitory effect than the other functional groups and shows highest antibacterial activity. While the compound having chloro group possesses second lowest MIC value (i.e. 1 µg/ml) against Bacillus pumilus MTCC 1607. In short, molecules having halogen group show more inhibition to the growth of afore mentioned bacterias. Rests of the compounds were found to be good active against the same bacterial strain. DNJ-209 and DNJ-210 were found to be moderate active against Bacillus pumilus MTCC 1607 with the MIC values >8 and 16 µg/ml respectively. All the compounds of this series were found to be good active against Staphylococcus pyogenes MTCC 442 with the MIC value between 1-8 µg/ml. All these compounds did not show good inhibitory effect against rests of the three bacterial strains i.e. Staphylococcus epidermidis MTCC 155, Staphylococcus aureus MTCC 96 and Enterococcus faecalis MTCC 439, only few compounds were found to possess good activity. Results of antibacterial screening of DNJ-301 to DNJ-305 showed that all the compounds were moderate active against all the four bacterial strains i.e. Bacillus pumilus MTCC 1607, Staphylococcus epidermidis MTCC 155, Staphylococcus pyogenes MTCC 442 and Staphylococcus aureus MTCC 96. Only one compound, DNJ-305 was found to possess good inhibitory effect with the MIC values of 4 µg/ml and 2 µg/ml on Staphylococcus epidermidis MTCC 155 and Staphylococcus pyogenes MTCC 442 respectively. Thus long alkyl chain possessing three carbon atoms on nitrogen atom of indoline nucleus having secondary amine on the another end did not affect the inhibition of the bacterial growth, only the compound (DNJ-305) having benzyl piperazine subunit could show good inhibition. Department of Chemistry, Saurashtra University, Rajkot – 360 005 332
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Saurashtra University Re - Accredit
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Statement under O. Ph. D. 7 of Saur
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ACKNOWLEDGEMENT It is a moment of g
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Jignesh Lunagariya, Hitesh Sarvaiya
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CONTENT Content General Remarks 6 A
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Content 3.2 Reaction scheme 149 3.3
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5.14 Conclusion 313 5.15 Spectral r
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MF Molecular Formula MW Molecular W
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GABA Gamma Amino Butyric Acid MES M
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PART - A STUDIES ON 2-METHYL INDOLI
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Part-A Studies on 2-methyl indoline
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CHAPTER - 1 PREPARATION AND YIELD O
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Chapter - 1 Preparation and Yield o
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Chapter - 2 Microwave assisted simp
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Part - B Studies on isatin derivati
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CHAPTER - 3 PREPARATION OF SMALL LI
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Chapter - 3 Preparation of small li
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CHAPTER - 4 STUDIES ON DIFFERENT TY
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Chapter - 4 Studies on different ty
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Chapter - 5 Synthesis and Character
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Chapter - 5 Synthesis and Character
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