Repositioning Candidate Details
| Candidate ID: | R0404 |
| Source ID: | DB01103 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Quinacrine |
| Synonyms: | 2-methoxy-6-chloro-9-diethylaminopentylaminoacridine; 3-chloro-7-methoxy-9-(1-methyl-4-diethylaminobutylamino)acridine; 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxyacridine; Mepacrine; N4-(6-chloro-2-methoxy-9-acridinyl)-N1,N1-diethyl-1,4-pentanediamine |
| Molecular Formula: | C23H30ClN3O |
| SMILES: | CCN(CC)CCCC(C)NC1=C2C=C(OC)C=CC2=NC2=C1C=CC(Cl)=C2 |
| Structure: |
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| DrugBank Description: | An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2. |
| CAS Number: | 83-89-6 |
| Molecular Weight: | 399.957 |
| DrugBank Indication: | For the treatment of giardiasis and cutaneous leishmaniasis and the management of malignant effusions. |
| DrugBank Pharmacology: | Quinacrine has been used as an antimalarial drug and as an antibiotic. It is used to treat giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus erythematosus, an inflammatory disease that affects the joints, tendons, and other connective tissues and organs. Quinacrine may be injected into the space surrounding the lungs to prevent reoccurrence of pneumothorax. The exact way in which quinacrine works is unknown. It appears to interfere with the parasite's metabolism. |
| DrugBank MoA: | The exact mechanism of antiparasitic action is unknown; however, quinacrine binds to deoxyribonucleic acid (DNA) in vitro by intercalation between adjacent base pairs, inhibiting transcription and translation to ribonucleic acid (RNA). Quinacrine does not appear to localize to the nucleus of Giaridia trophozoites, suggesting that DNA binding may not be the primary mechanism of its antimicrobial action. Fluorescence studies using Giardia suggest that the outer membranes may be involved. Quinacrine inhibits succinate oxidation and interferes with electron transport. In addition, by binding to nucleoproteins, quinacrine suppress the lupus erythematous cell factor and acts as a strong inhibitor of cholinesterase. |
| Targets: | DNA intercalation; 85/88 kDa calcium-independent phospholipase A2 inhibitor; Cytosolic phospholipase A2 inhibitor; Inactive phospholipase C-like protein 1 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class |
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