title: Inhibition of growth of Leishmania donovani promastigotes by newly synthesized 1,3,4-thiadiazole analogs.
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.
authors: Molecular Virology and Infectious Diseases Section, Department of Biological and Medical Research, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia.
authors: Ahmed
authors: A
authors: Al-Qahtani
authors: Yunus M
authors: YM
authors: Siddiqui
authors: Adnan A
authors: AA
authors: Bekhit
authors: Ola A
authors: OA
authors: El-Sayed
authors: Hassan Y
authors: HY
authors: Aboul-Enein
authors: Mohammed N
authors: MN
authors: Al-Ahdal
keywords: Antileishmanial; Antiparasite; Leishmania donovani; Thiadiazoles
references: East Mediterr Health J. 2003 Jul;9(4):837-43
references: 15748080
references: Eur J Med Chem. 2005 Dec;40(12):1346-50
references: 16095763
references: Bioorg Med Chem. 2008 Apr 15;16(8):4509-15
references: 18321711
references: Gene. 1998 Apr 14;210(2):325-33
references: 9573393
references: J Med Chem. 2001 Mar 1;44(5):749-62
references: 11262085
references: J Postgrad Med. 2003 Jan-Mar;49(1):39-49
references: 12865570
references: Mol Pharmacol. 2001 Jan;59(1):30-7
references: 11125021
references: Acta Trop. 1995 Oct;60(2):73-80
references: 8610542
references: Parasitol Today. 1999 May;15(5):182-7
references: 10322351
references: Curr Infect Dis Rep. 2005 Jan;7(1):33-38
references: 15610669
references: Farmaco. 1996 Oct;51(10):659-64
references: 8981756
references: Curr Opin Investig Drugs. 2005 Feb;6(2):163-9
references: 15751739
references: Antimicrob Agents Chemother. 1997 Apr;41(4):827-30
references: 9087498
references: Cancer Commun. 1991 Jul;3(7):207-12
references: 1867954
references: J Infect Chemother. 2004 Dec;10(6):307-15
references: 15614453
references: Exp Parasitol. 1991 May;72(4):411-7
references: 2026215
references: Clin Infect Dis. 2001 Dec 1;33(11):1847-51
references: 11692295
references: Mol Cell Biol. 1992 Jun;12(6):2855-65
references: 1350325
references: Eur J Med Chem. 2002 Dec;37(12):979-84
references: 12660023
references: Eur J Med Chem. 2009 Apr;44(4):1758-62
references: 18485538
references: Lancet. 1999 Oct 2;354(9185):1191-9
references: 10513726
references: Farmaco. 2002 Mar;57(3):253-7
references: 11989804
references: Ann Trop Med Parasitol. 2003 Oct;97 Suppl 1:47-56
references: 14678632
references: Adv Exp Med Biol. 1986;195 Pt B:547-51
references: 3020925
references: Bioorg Med Chem Lett. 2003 Oct 20;13(20):3513-5
references: 14505660
references: Parasitol Res. 2008 Jun;103(1):1-10
references: 18389282
references: Ann Parasitol Hum Comp. 1990;65(3):111-25
references: 2080829
references: Arch Pharm (Weinheim). 2005 Oct;338(10):484-7
references: 16211660
references: J Med Chem. 2005 Feb 24;48(4):1145-51
references: 15715480
references: Biochem Pharmacol. 2003 Mar 15;65(6):999-1006
references: 12623132
references: Eur J Med Chem. 2000 Sep;35(9):853-7
references: 11006486
references: Antimicrob Agents Chemother. 2003 Oct;47(10):3368-70
references: 14506061
references: J Med Chem. 1995 Jun 9;38(12):2038-40
references: 7540208
references: Bioorg Med Chem Lett. 2005 Apr 15;15(8):1983-5
references: 15808452