MA27360A1 - SYNTHESIS AND APPLICATION OF SPIRO-ISOXAZOLINES AS ANTI-TUBERCULAR AGENTS - Google Patents
SYNTHESIS AND APPLICATION OF SPIRO-ISOXAZOLINES AS ANTI-TUBERCULAR AGENTSInfo
- Publication number
- MA27360A1 MA27360A1 MA27961A MA27961A MA27360A1 MA 27360 A1 MA27360 A1 MA 27360A1 MA 27961 A MA27961 A MA 27961A MA 27961 A MA27961 A MA 27961A MA 27360 A1 MA27360 A1 MA 27360A1
- Authority
- MA
- Morocco
- Prior art keywords
- tuberculosis
- isoxazolines
- spiro
- activity
- site
- Prior art date
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Synthèse et Application des Spiro-Isoxazolines comme Agents anti-Tuberculeux Nous rapportons dans ce brevet la conception et l'activité antituberculeuse de certains dérivés spiroisoxazoline disubstitutés en positions 3',4' ; sur la base d'une structure hypothétique de site pharmacophore conçue pour agir sur le site biologique inconnu de la bactérie, Mycobacterium Tuberculosis ; responsable de la maladie dite Tuberculose. L'évaluation anti-tuberculeuse in vitro de ces composés nous a permis d'identifier sept (07) nouveaux inhibiteurs non-nucléosides efficaces contre la Tuberculose humaine [% inhibition = 90-93 %], déclarés comme antituberculeux potentiels par TAACF/USA respectivement dans l'ordre d'activité décroissante ; sous les codes 157162, 157166, 157161, 157165, 157172, 157163 et 157169, avec des valeurs de Concentration d'Inhibition Minimale (MIC) égale ou inférieure à 6.25 micro-g/mL ce qui nous offre une nouvelle famille d'agents antituberculeux non nucléosides ayant une activité respectable. Gr??ce au rôle principal du site pharmacophore spiranique, de structure générale [ X-(C)n-Y , avec X,Y = N, O , S et n = 2, 3]; ces composés Spiro-Isoxazolines (SO) ont acquis une activité anti-Tuberculose potentielle qui reste gouvernée par des conditions géométriques et électroniques bien précises. Mots Clés : Spiro-Isoxazolines, Tuberculose, Design, Site Pharmacophore spécifique.Synthesis and Application of Spiro-Isoxazolines as Anti-Tuberculosis Agents We report in this patent the design and anti-tuberculosis activity of certain spiroisoxazoline derivatives disubstituted in positions 3 ', 4'; based on a hypothetical pharmacophore site structure designed to act on the unknown biological site of the bacteria, Mycobacterium Tuberculosis; responsible for the so-called Tuberculosis disease. The in vitro anti-tuberculosis evaluation of these compounds enabled us to identify seven (07) new non-nucleoside inhibitors effective against human Tuberculosis [% inhibition = 90-93%], declared as potential anti-tuberculosis drugs by TAACF / USA respectively. in decreasing order of activity; under the codes 157162, 157166, 157161, 157165, 157172, 157163 and 157169, with Minimum Inhibition Concentration (MIC) values equal to or less than 6.25 micro-g / mL which gives us a new family of anti-tuberculosis agents non-nucleosides with respectable activity. Thanks to the main role of the spiranic pharmacophore site, of general structure [X- (C) n-Y, with X, Y = N, O, S and n = 2, 3]; these Spiro-Isoxazolines (SO) compounds have acquired potential anti-tuberculosis activity which remains governed by very precise geometric and electronic conditions. Keywords: Spiro-Isoxazolines, Tuberculosis, Design, Specific Pharmacophore Site.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MA27961A MA27360A1 (en) | 2004-11-23 | 2004-11-23 | SYNTHESIS AND APPLICATION OF SPIRO-ISOXAZOLINES AS ANTI-TUBERCULAR AGENTS |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MA27961A MA27360A1 (en) | 2004-11-23 | 2004-11-23 | SYNTHESIS AND APPLICATION OF SPIRO-ISOXAZOLINES AS ANTI-TUBERCULAR AGENTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA27360A1 true MA27360A1 (en) | 2005-06-01 |
Family
ID=34859125
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA27961A MA27360A1 (en) | 2004-11-23 | 2004-11-23 | SYNTHESIS AND APPLICATION OF SPIRO-ISOXAZOLINES AS ANTI-TUBERCULAR AGENTS |
Country Status (1)
| Country | Link |
|---|---|
| MA (1) | MA27360A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11179396B2 (en) | 2016-06-16 | 2021-11-23 | Janssen Sciences Ireland Uc | Heterocyclic compounds as antibacterials |
| US11180472B2 (en) | 2015-07-02 | 2021-11-23 | Janssen Sciences Ireland Uc | Antibacterial compounds |
| US11224596B2 (en) | 2017-03-01 | 2022-01-18 | Janssen Sciences Ireland Unlimited Company | PZA and cytochrome bc1 inhibitor combination treatment |
-
2004
- 2004-11-23 MA MA27961A patent/MA27360A1/en unknown
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11180472B2 (en) | 2015-07-02 | 2021-11-23 | Janssen Sciences Ireland Uc | Antibacterial compounds |
| US11866419B2 (en) | 2015-07-02 | 2024-01-09 | Janssen Sciences Ireland Unlimited Company | Antibacterial compounds |
| US11179396B2 (en) | 2016-06-16 | 2021-11-23 | Janssen Sciences Ireland Uc | Heterocyclic compounds as antibacterials |
| US11224596B2 (en) | 2017-03-01 | 2022-01-18 | Janssen Sciences Ireland Unlimited Company | PZA and cytochrome bc1 inhibitor combination treatment |
| US11918575B2 (en) | 2017-03-01 | 2024-03-05 | Janssen Sciences Ireland Unlimited Company | PZA and cytochrome Bc1 inhibitor combination treatment |
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