Leishmanicidal potential of N-substituted morpholine derivatives: synthesis and structure-activity relationships.
A series of N-substituted morpholines 2-20 was synthesised by reacting various acid chlorides and alkyl halides with morpholine (1). All of the synthesised compounds 2-20 were screened for their leishmanicidal effects using amphotericin B (IC(50) = 0.24 microg L(-1)) and pentamidine (IC(50) = 2.56 microg mL(-1)) as standards and a structure-activity relationship (SAR) study was established. The compounds 2 (IC(50) = 48 microg mL(-1)), 3 (IC(50) = 30.0 microg mL(-1)), 10 (IC(50) = 41.0 microg mL(-1)), 15 (IC(50) = 33.0 microg mL(-1)), 16 (IC(50) = 35.0 microg mL(-1)) and 20 (IC(50) = 47.0 microg mL(-1)) showed weak leishmanicidal activities.
Khan
Khalid Mohammed
KM
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan. hassaan2@super.net.pk
Khan
Muhammad Zarrar
MZ
Taha
Muhammad
M
Maharvi
Ghulam Murtaza
GM
Saify
Zafar Saeed
ZS
Parveen
Shahnaz
S
Choudhary
Muhammad Iqbal
MI
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D018320:Leishmania major / Q000187:drug effects; D009025:Morpholines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism
D000981:Antiprotozoal Agents; D009025:Morpholines