Cellular effects of leishmanial tubulin inhibitors on L. donovani

Havens, Courtney G.; Bryant, N.J.; Asher, Ludmila V.; Lamoreaux, Laurie; Perfetto, Steve; Brendle, James J.; Werbovetz, Karl A.

doi:10.1016/s0166-6851(00)00272-3

Cited by 62 publications

(61 citation statements)

References 30 publications

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“…It suggests that the 5-thioisocyanatomethyl group is an important feature for antikinetoplastid activity of this series (Table 3). 58 The prototype compound WR85915 (71), for its part, confirmed its activity against protozoan (IC 50 = 4. Table 4.…”

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 92%

“…50 It is also possible to find protocols employing heterogeneous catalyst systems to obtain 1,3,4-oxadiazoles in one step. Sanghshetti et al 51 described the reaction of hydrazide (56) and several aroyl aldehydes (57) in the presence of nanoparticles of ZnO-TiO 2 under microwave irradiation, affording the respective 1,3,4-oxadiazoles (58). Reduced reaction times (12-15 min) and high yields (91-96%) are interesting features of this protocol (Scheme 12).…”

Section: Synthesis Of 134-oxadiazolesmentioning

confidence: 99%

“…The authors pointed out the presence of the isothiocyanatophenyl moiety at the 3-position of 1,2,4-oxadiazolic ring as an important feature to anthelmintic activity. 57 Cottrell et al 58 designed a series of analogues based on the structure of WR85915 (71). 58 The prototype had been previously described as a tubulin inhibitor tested in vitro against Leishmania donovani (IC 50 = 5.6 μmol L -1 , promastigotes; IC 50 = 4.3 μmol L -1 , axenic amastigotes).…”

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

“…57 Cottrell et al 58 designed a series of analogues based on the structure of WR85915 (71). 58 The prototype had been previously described as a tubulin inhibitor tested in vitro against Leishmania donovani (IC 50 = 5.6 μmol L -1 , promastigotes; IC 50 = 4.3 μmol L -1 , axenic amastigotes). 59 The new molecules were assayed for antiprotozoal activity against L. donovani and Trypanosoma brucei.…”

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

“…Table 4. 58 Santos-Filho et al 60 described the synthesis, biological activity and docking results of a series of 3-(4-substitutedaryl)-1,2,4-oxadiazoles-N-acylhydrazones as antiTrypanosoma cruzi agents. The in vitro assessment for antiprotozoal activity was conducted against trypomastigotes of T. cruzi (Y strain).…”

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

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1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

Pitasse-Santos¹,

Sueth-Santiago²,

Lima³

2017

J. Braz. Chem. Soc.

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In this review, we present the potential use of the heterocyclic oxadiazole rings in the design and synthesis of new drugs to treat parasitic infections. We intend to compare herein all the four isomeric forms of oxadiazole rings as well as discuss the differences and similarities between them. In addition, we discuss aspects on their reactivity that justify the great importance of both 1,2,4-and 1,3,4-oxadiazoles isomers when compared with their other two isomers. Although some oxadiazole isomers satisfy Hückel's rule, there are differences concerning their aromaticity, which have a great impact on the possible interactions of the oxadiazole ring with biological receptors. The set of works selected from the literature and discussed herein points out the oxadiazole core as an important and versatile scaffold in the development of new chemical entities potentially useful as antiparasitic drugs.

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Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 92%

Section: Synthesis Of 134-oxadiazolesmentioning

confidence: 99%

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

Section: 24-oxadiazoles As Antiparasitic Agentsmentioning

confidence: 99%

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1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

Pitasse-Santos¹,

Sueth-Santiago²,

Lima³

2017

J. Braz. Chem. Soc.

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Drug Discovery and Development for Kinetoplastid Diseases

Caffrey

Steverding

Ferreira

et al. 2021

Burger's Medicinal Chemistry and Drug Discovery

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In this article, we review the disease, biology, and biochemistry of kinetoplastids, as well as the new drugs and drug candidates that have entered the clinic in the last decade. We also describe examples of the preclinical exploration of small molecules against various protein targets (e.g. cysteine proteases, the proteasome, and tubulin), as well as cutting‐edge molecular and computational strategies and technologies being brought to bear to discover and develop new antitrypanosomal drugs. For comprehensive descriptions of the disease, biology, and drug therapies prior to 2011, the reader is encouraged to review the article by P.M. Woster that appeared in 2010 in the seventh edition of Burger's Medicinal Chemistry, Drug Discovery, and Development, entitled Antiprotozoal/Antiparasitic Agents.

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Arsenite Resistance in Leishmania and Possible Drug Targets

Singh

Jayanarayan

Dey

Advances in Experimental Medicine and Biology

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Pregarded as the second-most dreaded parasitic disease after malaria (WHO). Visceral leishmaniasis or kala-azar, caused by Leishmania donovani, is the most fatal form of leishmaniasis afflicting millions of people worldwide. No vaccination is available against leishmaniasis and fast spreading drug resistance in these parasitic organisms is posing a major medical threat. All these emphasize the need for new drugs and molecular targets along with reappraisal of existing therapeutics. Identification and characterization of cellular targets and answering the problem of drug resistance in Leishmania has always been the main thrust of protozoal research worldwide. Model drug resistance phenotypes against drugs, viz. arsenite (an antimony related metal ion, the first line of treatment against leishmaniasis), have been widely used to address and understand mechanism of drug resistance. The present discussion is an attempt to understand the different factors associated with arsenite resistance in Leishmania.

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Cellular effects of leishmanial tubulin inhibitors on L. donovani

Cited by 62 publications

References 30 publications

1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

Drug Discovery and Development for Kinetoplastid Diseases

Arsenite Resistance in Leishmania and Possible Drug Targets

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