Literature DB >> 23964165

Inhibition of growth of Leishmania donovani promastigotes by newly synthesized 1,3,4-thiadiazole analogs.

Ahmed Al-Qahtani1, Yunus M Siddiqui, Adnan A Bekhit, Ola A El-Sayed, Hassan Y Aboul-Enein, Mohammed N Al-Ahdal.   

Abstract

Leishmania donovani, the causative agent of visceral leishmaniasis, is transmitted by sand flies and replicates intracellularly in their mammalian host cells. The emergence of drug-resistant strains has hampered efforts to control the spread of the disease worldwide. Forty-four 1,3,4-thiadiazole derivatives and related compounds were tested in vitro for possible anti-leishmanial activity against the promastigotes of L. donovani. Micromolar concentrations of these agents were used to study the inhibition of multiplication of L. donovani promastigotes. Seven compounds were identified with potential antigrowth agents of the parasite. Compound 4a was the most active at 50 μM followed by compound 3a. These compounds could prove useful as a future alternative for the control of visceral leishmaniasis.

Entities:  

Keywords:  Antileishmanial; Antiparasite; Leishmania donovani; Thiadiazoles

Year:  2009        PMID: 23964165      PMCID: PMC3731026          DOI: 10.1016/j.jsps.2009.08.005

Source DB:  PubMed          Journal:  Saudi Pharm J        ISSN: 1319-0164            Impact factor:   4.330


  33 in total

1.  Thiadiazole: a new family of intercalative photonuclease with electron transfer and radical mechanisms.

Authors:  Yonggang Li; Yufang Xu; Xuhong Qian; Baoyuan Qu
Journal:  Bioorg Med Chem Lett       Date:  2003-10-20       Impact factor: 2.823

2.  Recent Developments in Leishmaniasis: Epidemiology, Diagnosis, and Treatment.

Authors:  Jonathan Berman
Journal:  Curr Infect Dis Rep       Date:  2005-01       Impact factor: 3.725

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Journal:  J Med Chem       Date:  1995-06-09       Impact factor: 7.446

Review 4.  Taxonomy of Leishmania. Use of isoenzymes. Suggestions for a new classification.

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Journal:  Ann Parasitol Hum Comp       Date:  1990

5.  Synthesis and antibacterial activity of some 5-guanylhydrazone/thiocyanato-6-arylimidazo[2,1-b]-1,3, 4-thiadiazole-2-sulfonamide derivatives.

Authors:  A K Gadad; C S Mahajanshetti; S Nimbalkar; A Raichurkar
Journal:  Eur J Med Chem       Date:  2000-09       Impact factor: 6.514

Review 6.  Leishmaniasis.

Authors:  B L Herwaldt
Journal:  Lancet       Date:  1999-10-02       Impact factor: 79.321

Review 7.  Recent advances in antileishmanial drug development.

Authors:  Antony J Davis; Lukasz Kedzierski
Journal:  Curr Opin Investig Drugs       Date:  2005-02

8.  Activity of megazol, a trypanocidal nitroimidazole, is associated with DNA damage.

Authors:  Bertin Enanga; Mark R Ariyanayagam; Mhairi L Stewart; Michael P Barrett
Journal:  Antimicrob Agents Chemother       Date:  2003-10       Impact factor: 5.191

9.  Synthesis and in vitro anti-leishmanial activity of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]- and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines.

Authors:  Mina Behrouzi-Fardmoghadam; Fatemeh Poorrajab; Sussan Kaboudanian Ardestani; Saeed Emami; Abbas Shafiee; Alireza Foroumadi
Journal:  Bioorg Med Chem       Date:  2008-02-20       Impact factor: 3.641

10.  Effect of megazol on Trypanosoma brucei brucei acute and subacute infections in Swiss mice.

Authors:  B Bouteille; A Marie-Daragon; G Chauvière; C de Albuquerque; B Enanga; M L Dardé; J M Vallat; J Périé; M Dumas
Journal:  Acta Trop       Date:  1995-10       Impact factor: 3.112

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  1 in total

Review 1.  Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review.

Authors:  Azar Tahghighi; Fateme Babalouei
Journal:  Iran J Basic Med Sci       Date:  2017-06       Impact factor: 2.699

  1 in total

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