MD4519B1 - Use of (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one as antituberculous agent - Google Patents
Use of (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one as antituberculous agent Download PDFInfo
- Publication number
- MD4519B1 MD4519B1 MDA20170068A MD20170068A MD4519B1 MD 4519 B1 MD4519 B1 MD 4519B1 MD A20170068 A MDA20170068 A MD A20170068A MD 20170068 A MD20170068 A MD 20170068A MD 4519 B1 MD4519 B1 MD 4519B1
- Authority
- MD
- Moldova
- Prior art keywords
- triazol
- dimethyl
- pent
- nitrophenyl
- antituberculous
- Prior art date
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- HSYXNSUUVTWJTP-JYRVWZFOSA-N (z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1,2,4-triazol-1-yl)pent-1-en-3-one Chemical compound C1=NC=NN1/C(C(=O)C(C)(C)C)=C\C1=CC=C([N+]([O-])=O)C=C1 HSYXNSUUVTWJTP-JYRVWZFOSA-N 0.000 title abstract 2
- 239000000814 tuberculostatic agent Substances 0.000 title abstract 2
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- VRDBIJCCXDEZJN-UHFFFAOYSA-N 2-piperidin-1-ylacetic acid Chemical compound OC(=O)CN1CCCCC1 VRDBIJCCXDEZJN-UHFFFAOYSA-N 0.000 abstract 1
- FMWWRALTYIWZEB-UHFFFAOYSA-N 3,3-dimethyl-1-(1,2,4-triazol-1-yl)butan-2-one Chemical compound CC(C)(C)C(=O)CN1C=NC=N1 FMWWRALTYIWZEB-UHFFFAOYSA-N 0.000 abstract 1
- BXRFQSNOROATLV-UHFFFAOYSA-N 4-nitrobenzaldehyde Chemical compound [O-][N+](=O)C1=CC=C(C=O)C=C1 BXRFQSNOROATLV-UHFFFAOYSA-N 0.000 abstract 1
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical class C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 abstract 1
- 241000186359 Mycobacterium Species 0.000 abstract 1
- 230000002365 anti-tubercular Effects 0.000 abstract 1
- 238000010533 azeotropic distillation Methods 0.000 abstract 1
- 239000003054 catalyst Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000009833 condensation Methods 0.000 abstract 1
- 230000005494 condensation Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000010992 reflux Methods 0.000 abstract 1
- JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 abstract 1
- 229960001225 rifampicin Drugs 0.000 abstract 1
- 201000008827 tuberculosis Diseases 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to pharmaceutical chemistry and can be used in the development of new agents for the treatment of tuberculosis of the 1,2,4-triazole class.Summary of the invention consists in that it is proposed as antituberculous agent the (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one with the formula:.The compound exhibits antituberculous activity against Mycobacterium tuberculosisH37Rv (ATCC 27294) comparable to rifampicin.The isomeric compound is obtained by selective aldol-crotonic condensation of 3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one with 4-nitrobenzaldehyde, which occurs during reflux in benzene, with azeotropic distillation of the formed water, in the presence of a piperidine-acetic acid catalyst (70%, m.p. 114…116°C).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MDA20170068A MD4519C1 (en) | 2016-12-21 | 2016-12-21 | Use of (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one as antituberculous agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MDA20170068A MD4519C1 (en) | 2016-12-21 | 2016-12-21 | Use of (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one as antituberculous agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MD4519B1 true MD4519B1 (en) | 2017-10-31 |
| MD4519C1 MD4519C1 (en) | 2018-05-31 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20170068A MD4519C1 (en) | 2016-12-21 | 2016-12-21 | Use of (Z)-4,4-dimethyl-1-(4-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)pent-1-en-3-one as antituberculous agent |
Country Status (1)
| Country | Link |
|---|---|
| MD (1) | MD4519C1 (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1168248A (en) * | 1980-07-25 | 1984-05-29 | Erik Regel | Triazolylpropenol derivatives, a process for their preparation and their use as plant growth regulators and fungicides |
| US4749716A (en) * | 1979-03-20 | 1988-06-07 | Sumitomo Chemical Company, Limited | Geometrical isomer of 1-substituted-1-triazolystyrenes |
-
2016
- 2016-12-21 MD MDA20170068A patent/MD4519C1/en not_active IP Right Cessation
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4749716A (en) * | 1979-03-20 | 1988-06-07 | Sumitomo Chemical Company, Limited | Geometrical isomer of 1-substituted-1-triazolystyrenes |
| CA1168248A (en) * | 1980-07-25 | 1984-05-29 | Erik Regel | Triazolylpropenol derivatives, a process for their preparation and their use as plant growth regulators and fungicides |
Non-Patent Citations (4)
| Title |
|---|
| Funaki Y., Ishiguri Y., Kato T. and Tanaka S. Structure-Activity Relationships of Vinyl Triazole Fungicide. J. Pesticide Sci. 9, 229-236 (1984). regăsit în Internet la 2017.06.08, url: https://www.jstage.jst.go.jp/article/jpestics1975/9/2/9_2_229/_pdf Pages 229, 230; Table 1, compounds 7 and 15 * |
| Pawan Kumar Mishra, Jaya Dwivedi, Rajani Chauhan. Triazoles as potential antitubercular agent: a review. Journal of Advanced Scientific Research, 2016, 7(1), 9-13 * |
| R. Singh and A. Chouhan. IMPORTANT METHODS OF SYNTHESIS AND BIOLOGICAL SIGNIFICANCE OD 1,2,4-TRIAZOLES DERIVATIVES. WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES, Vol. 3, Issue 8, 874-906, 2014. Regăsit îm Internet la 2017.08.01, url: http://www.wjpps.com/download/article/1406694109.pdf pag. 894-895, Antitubercular activity * |
| Rangappa S. Keri, Siddappa A. Patil, Srinivasa Budagumpi, Bhari Mallanna Nagaraja. Triazole: A Promising Antitubercular Agent. Chem Biol Drug Des 2015, 86, 410-423. Regăsit în Internet la 2017.07.31, url: http://www.sciensage.info/journal/1457099361JASR_2409151.pdf * |
Also Published As
| Publication number | Publication date |
|---|---|
| MD4519C1 (en) | 2018-05-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG4A | Patent for invention issued | ||
| KA4A | Patent for invention lapsed due to non-payment of fees (with right of restoration) | ||
| MM4A | Patent for invention definitely lapsed due to non-payment of fees |