Synthesis of primaquine glyco-conjugates as potential tissue schizontocidal antimalarial agents
| Autor: | Anil K. Saxena, Arif Jamal Siddiqui, Nitya Anand, Jyoti Bhardwaj, Mridula Saxena, Sunil K. Puri, G.P. Dutta, Chandra S. Azad |
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| Rok vydání: | 2017 |
| Předmět: |
Male
Drug Plasmodium Primaquine media_common.quotation_subject Pharmacology 010402 general chemistry 01 natural sciences Biochemistry Antimalarials Mice chemistry.chemical_compound Glucoside Drug Discovery Malaria Vivax medicine Animals Antimalarial Agent media_common 010405 organic chemistry Organic Chemistry Oxidative deamination medicine.disease Macaca mulatta Galactoside Malaria 0104 chemical sciences chemistry Molecular Medicine Female Plasmodium vivax Glycoconjugates Plasmodium cynomolgi medicine.drug Conjugate |
| Zdroj: | Chemical Biology & Drug Design. 90:254-261 |
| ISSN: | 1747-0277 |
| Popis: | Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side-effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system, the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to direct the drug to the liver, where hypnozoites resides. All the synthesized compounds were fully characterized and evaluated for their radical curative activities. The three compounds viz glucoside (15a), galactoside (15b) and mannoside (15c) with high activity were tested for their activity in rhesus monkeys where the most active compound 15b showed twofold activity (100% radical curative activity at 1.92 mmol/kg) than the standard drug PQ diphosphate (3.861 mmol/kg). It is proposed that results from these studies may be advantageous to develop a new potent tissue schizonticide antimalarial compound. |
| Databáze: | OpenAIRE |
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