Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/13261
Title: Nitroguanidines and guanidino-containing hetereocycles as potential nitric oxide synthase inhibitors
Authors: KOK HWA JIUAN
Keywords: Nitric Oxide Synthase; Selective inhibition.
Issue Date: 22-May-2008
Source: KOK HWA JIUAN (2008-05-22). Nitroguanidines and guanidino-containing hetereocycles as potential nitric oxide synthase inhibitors. ScholarBank@NUS Repository.
Abstract: A series of amines were synthesized with yields of 71 to 99% for coupling with S-methyl-N-nitroisothiourea (SMNNITU) to form library MK-I and MK-II compounds. The yields obtained for library MK-I and MK-II compounds ranged from 48 to 75% and 37 to 47% respectively. Library MK-I and MK-II compounds were screened for their inhibitory activities against the three isoforms of NOS at 100uM. MK-I-09 had a thiophene group which may be able to fit into the active site pocket thereby causing a strong inhibiton of 120% with respect to the positive control (100%), L-NG-nitro-arginine (L-NNA).Another library of guanidino-containing hetereocycles was screened for their inhibitory activities against the nNOS at 100uM. Compound X gave the highest inhibition of 44% among the guanidino-containing hetereocycles screened. This could be due to stronger interactions (e.g. hydrogen bonding) of the sulphur with the active site.
URI: http://scholarbank.nus.edu.sg/handle/10635/13261
Appears in Collections:Master's Theses (Open)

Show full item record
Files in This Item:
File Description SizeFormatAccess SettingsVersion 
KOKHJ.pdf601.22 kBAdobe PDF

OPEN

NoneView/Download

Page view(s)

227
checked on Dec 11, 2017

Download(s)

268
checked on Dec 11, 2017

Google ScholarTM

Check


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.