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Mini review on tricyclic compounds as an inhibitor of trypanothione reductase.

Kumar S, Ali MR, Bawa S - J Pharm Bioallied Sci (2014)

Bottom Line: Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species.The disease affects millions of people all over the world and associated with high morbidity and mortality rates.In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

ABSTRACT
Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species. The disease affects millions of people all over the world and associated with high morbidity and mortality rates. The review discuss briefly on current treatment of these parasitic diseases and trypanothione reductase (TryR) as potential targets for rational drug design. The enzyme trypanothione reductase (TryR) has been identified as unique among these parasites and has been proposed to be an effective target against for developing new drugs. The researchers have selected this enzyme as target is due to its substrate specificity in contrast to human analogous glutathione reductase and its absence from the host cell which makes this enzyme an ideal target for drug discovery. In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed.

No MeSH data available.


Related in: MedlinePlus

Structures of various tricyclic drug having potent trypanothione reductase inhibiting activity and selectivity of human glutathione reductase
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Figure 3: Structures of various tricyclic drug having potent trypanothione reductase inhibiting activity and selectivity of human glutathione reductase

Mentions: To further address the need for new compounds and new compound classes, Richardson et al.[10] initiated screening of 1266 pharmacologically active compounds from the Sigma-Aldrich LOPAC1280 library. These compounds were screened against TryR and the top hits counter-screened against GR and live T. brucei parasites, yielding the IC values, selectivity for TryR over GR and antiparasitic activity. Among all the 1266 compounds from Sigma-Aldrich LOPAC1280 library, several tricyclic derivatives were identified as a potent inhibitor TryR [Figure 3].


Mini review on tricyclic compounds as an inhibitor of trypanothione reductase.

Kumar S, Ali MR, Bawa S - J Pharm Bioallied Sci (2014)

Structures of various tricyclic drug having potent trypanothione reductase inhibiting activity and selectivity of human glutathione reductase
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4231380&req=5

Figure 3: Structures of various tricyclic drug having potent trypanothione reductase inhibiting activity and selectivity of human glutathione reductase
Mentions: To further address the need for new compounds and new compound classes, Richardson et al.[10] initiated screening of 1266 pharmacologically active compounds from the Sigma-Aldrich LOPAC1280 library. These compounds were screened against TryR and the top hits counter-screened against GR and live T. brucei parasites, yielding the IC values, selectivity for TryR over GR and antiparasitic activity. Among all the 1266 compounds from Sigma-Aldrich LOPAC1280 library, several tricyclic derivatives were identified as a potent inhibitor TryR [Figure 3].

Bottom Line: Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species.The disease affects millions of people all over the world and associated with high morbidity and mortality rates.In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

ABSTRACT
Trypanosomiasis and leishmaniasis are two most ruinous parasitic infectious diseases caused by Trypanosoma and Leishmania species. The disease affects millions of people all over the world and associated with high morbidity and mortality rates. The review discuss briefly on current treatment of these parasitic diseases and trypanothione reductase (TryR) as potential targets for rational drug design. The enzyme trypanothione reductase (TryR) has been identified as unique among these parasites and has been proposed to be an effective target against for developing new drugs. The researchers have selected this enzyme as target is due to its substrate specificity in contrast to human analogous glutathione reductase and its absence from the host cell which makes this enzyme an ideal target for drug discovery. In this review we have tried to present an overview of the different tricyclic compounds which are potent inhibitors of TryR with their inhibitory activities against the parasites are briefly discussed.

No MeSH data available.


Related in: MedlinePlus