Synthesis and Evaluation of Thiadiazole-based Antileishmanial Agents

Farshid Hassanzadeh; Elham Jafari; Mozhgan Saeedi; Sedigheh Saberi

doi:10.4103/jrptps.JRPTPS_3_20

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https://doi.org/10.4103/jrptps.JRPTPS_3_20

Synthesis and Evaluation of Thiadiazole-based Antileishmanial Agents

Author(s):

Farshid Hassanzadeh¹,

Elham Jafari^1,*,

Mozhgan Saeedi¹,

Sedigheh Saberi

²

1Department of Medicinal Chemistry, Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran

2Department of Mycology and Parasitology, School of Medicine, Isfahan University of Medical Sciences, Isfahan, I.R. Iran

Journal of Reports in Pharmaceutical Sciences:Vol. 9, issue 2; 189-95

Published online:Oct 07, 2020

Article type:Research Article

Received:Feb 09, 2020

Accepted:May 10, 2020

How to Cite:Farshid HassanzadehElham JafariMozhgan SaeediSedigheh SaberiSynthesis and Evaluation of Thiadiazole-based Antileishmanial Agents.J Rep Pharm Sci.9(2):e147112.https://doi.org/10.4103/jrptps.JRPTPS_3_20.

Abstract

Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity.
Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino- 1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major.
Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 μM and 64.7 μM, respectively.
Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72 h incubation.

Keywords

Amastigote

antileishmanial activity

Leishmania major

promastigote

thiadiazole

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Author(s):

Farshid Hassanzadeh:[PubMed][Scholar]
Elham Jafari:[PubMed][Scholar]
Mozhgan Saeedi:[PubMed][Scholar]
Sedigheh Saberi:[PubMed][Scholar]