Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity
Abstract
:1. Introduction
2. Results and Discussion
2.1. Synthesis of New Thiosemicarbazides
2.2. Optimization of the Chemical Reactions for Obtaining the Thiosemicarbazides V–VII
2.3. Study of Tuberculostatic Activity of Thiosemicarbazides V–VII
3. Materials and Methods
3.1. Chemical Compounds and Analysis
3.2. Optimization of the Chemical Reactions
3.3. Biological Tests
4. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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No. | x1; T (°C) | x2; t (h) | x1x2 | η (%) | ||
---|---|---|---|---|---|---|
1 | –1 (64) | –1 (2.5) | 1 | 1/3 | 1/3 | 72 |
2 | –1 (64) | 0 (3) | 0 | 1/3 | –2/3 | 76 |
3 | –1 (64) | 1 (3.5) | –1 | 1/3 | 1/3 | 70 |
4 | 0 (64.5) | –1 (2.5) | 0 | –2/3 | 1/3 | 76 |
5 | 0 (64.5) | 0 (3) | 0 | –2/3 | –2/3 | 80 |
6 | 0 (64.5) | 1 (3.5) | 0 | –2/3 | 1/3 | 77 |
7 | 1 (65) | –1 (2.5) | –1 | 1/3 | 1/3 | 75 |
8 | 1 (65) | 0 (3) | 0 | 1/3 | –2/3 | 76 |
9 | 1 (65) | 1 (3.5) | 1 | 1/3 | 1/3 | 72 |
No. | x1; T (°C) | x2; t (h) | x1x2 | η (%) | ||
---|---|---|---|---|---|---|
1 | –1 (64) | –1 (3.0) | 1 | 1/3 | 1/3 | 80 |
2 | –1 (64) | 0 (3.5) | 0 | 1/3 | –2/3 | 83 |
3 | –1 (64) | 1 (4.0) | –1 | 1/3 | 1/3 | 78 |
4 | 0 (64.5) | –1 (3.0) | 0 | –2/3 | 1/3 | 82 |
5 | 0 (64.5) | 0 (3.5) | 0 | –2/3 | –2/3 | 84 |
6 | 0 (64.5) | 1 (4.0) | 0 | –2/3 | 1/3 | 83 |
7 | 1 (65) | –1 (3.0) | –1 | 1/3 | 1/3 | 79 |
8 | 1 (65) | 0 (3.5) | 0 | 1/3 | –2/3 | 82 |
9 | 1 (65) | 1 (4.0) | 1 | 1/3 | 1/3 | 78 |
No. | x1; T (°C) | x2; t (h) | x1x2 | η (%) | ||
---|---|---|---|---|---|---|
1 | –1 (64) | –1 (3.5) | 1 | 1/3 | 1/3 | 84 |
2 | –1 (64) | 0 (4.0) | 0 | 1/3 | –2/3 | 88 |
3 | –1 (64) | 1 (4.5) | –1 | 1/3 | 1/3 | 83 |
4 | 0 (64.5) | –1 (3.5) | 0 | –2/3 | 1/3 | 86 |
5 | 0 (64.5) | 0 (4.0) | 0 | –2/3 | –2/3 | 89 |
6 | 0 (64.5) | 1 (4.5) | 0 | –2/3 | 1/3 | 85 |
7 | 1 (65) | –1 (3.5) | –1 | 1/3 | 1/3 | 84 |
8 | 1 (65) | 0 (4.0) | 0 | 1/3 | –2/3 | 87 |
9 | 1 (65) | 1 (4.5) | 1 | 1/3 | 1/3 | 83 |
Compound | x1; T (°C) | x2; t(h) | η (%) |
---|---|---|---|
V | 0.11 (64.55) | –0.09 (3 h 57 min 18 s) | 79.83 |
VI | –0.05 (64.47) | 0.11 (3 h 33 min 25 s) | 84.22 |
VII | –0.05 (64.47) | –0.07 (3 h 57 min 54 s) | 89.24 |
Compound | The Concentration of Thiosemicarbazides in the Culture Medium (μg/mL) | MIC (μg/mL) | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
5 | 10 | 20 | 30 | 40 | |||||||
6 Days | 15 Days | 6 Days | 15 Days | 6 Days | 15 Days | 6 Days | 15 Days | 6 Days | 15 Days | ||
V | ++ | +++ | ++ | ++ | ++ | + | – | – | – | – | 35 |
VI | ++ | +++ | ++ | + | – | – | – | – | – | – | 20 |
VII | ++ | +++ | + | – | – | – | – | – | – | – | 15 |
IAH | – | – | – | – | – | – | – | – | – | – | 10 |
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Popovici, C.; Pavel, C.-M.; Sunel, V.; Cheptea, C.; Dimitriu, D.G.; Dorohoi, D.O.; David, D.; Closca, V.; Popa, M. Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity. Int. J. Mol. Sci. 2021, 22, 12139. https://doi.org/10.3390/ijms222212139
Popovici C, Pavel C-M, Sunel V, Cheptea C, Dimitriu DG, Dorohoi DO, David D, Closca V, Popa M. Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity. International Journal of Molecular Sciences. 2021; 22(22):12139. https://doi.org/10.3390/ijms222212139
Chicago/Turabian StylePopovici, Corina, Cristina-Maria Pavel, Valeriu Sunel, Corina Cheptea, Dan Gheorghe Dimitriu, Dana Ortansa Dorohoi, Diana David, Valentina Closca, and Marcel Popa. 2021. "Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity" International Journal of Molecular Sciences 22, no. 22: 12139. https://doi.org/10.3390/ijms222212139