14 / 29
Page 75
conferenceseries
.com
Volume 8
Medicinal Chemistry
ISSN: 2161-0444
Medicinal Chemistry 2018
June 14-15, 2018
June 14-15, 2018 | Barcelona, Spain
10
th
World Congress on
Medicinal Chemistry and Drug Design
Novel dihalo-substituted thiocarbamides as standalone agents to combat deadly tuberculosis: Design
synthesis and bioevaluation
Abdulmohsen H Al-Rohaimi
Shaqra University, Saudi Arabia
S
tudies carried out in the field of TB biochemistry have revealed that M. tuberculosis is unique among most bacteria,
therefore, several drugs require activation
in situ
to produce the inhibitory effect. Impelled by the fact, it was envisaged
to develop and screen newer dihalo-substituted thiocarbamide derivatives as an analog of ethionamide against strains of
Mycobacterium tuberculosis
(Mtb). The chemical modification approach was chosen in the hope that it may provide information
in the identification of some new targets. There are several known targets which are involved in the synthesis of some specific
protein or mycolic acid for which InhA is the key enzyme. Various thiocarbamide drugs (ETH, TAC, ISO and C26) act via
different final targets upon metabolic activation by the EthA protein inhibiting the biosynthesis of mycolic acid. Some novel
dihalo-substituted thiocarbamide derivatives were synthesized and structures of these derivatives were established on the
basis of IR, 1H and 13C-NMR and mass spectral data. All the dihalo-substituted thiocarbamide derivatives were tested
in-
vitro
for antimycobacterial activity against
Mycobacterium tuberculosis
(ATCC-25177) by well diffusion method and MIC
by serial dilution method. Results of the antitubercular screening disclosed that some of the derivatives showed moderate
to good antitubercular potential. Among all the tested derivatives, two viz., 1-(3,4-Dichlorophenyl)-1-(furan-2-ylmethyl)-
3-phenylthiourea and 1-(3,4-Dichlorophenyl)-3-phenyl-1-(1-(thiophen-2-yl)ethyl)thiourea displayed MIC values of 25μg/
mL and one compound 1-(3-Chloro-4-fluorophenyl)-3-phenyl-1-(1-(thiophen-2-yl)ethyl)thiourea exhibited MIC value of
12.5μg/ml against
Mycobacterium tuberculosis
(ATCC-25177).
alrohaimi@hotmail.comMed chem (Los Angeles) 2018, Volume 8
DOI: 10.4172/2161-0444-C1-040