5-(4-aminophenyl)-2-thiol-1,3,4-oxadiazole 2 has been prepared through cyclization of 4-aminobenzoyl hydrazide 1 with carbon disulfide in the existence of (KOH) in ethyl alcohol. Oxadiazole derivative 2 has been transformed to analogous diazonium salt that was straightaway treated with salicylaldehyde as coupling reagent to yield the initiator aldehyde 3. Condensation of aldehyde 3 with anilines consisting (p-bromoaniline, p-chloroaniline, p-nitroaniline, m-nitroaniline, p-methoxyaniline and p-hydroxyaniline) using microwave irradiation technique in ethyl alcohol to give six imines 4af. Treatment of the resulting imines 4af with tyrosine in microwave oven produced six imidazolidin-4-ones 5af consisting 1,3,4-oxadiazole unit. Investigation of antibacterial activity for the target compounds has been taken place on bacteria, Staphylococcus aurous and Escherichia coli. Outputs evinced that the synthesized imidazolidin-4-one (compound 5e) exhibited better activity to gentamycin athwart positive bacteria. Meanwhile, the imidazolidin-4-ones (5a, 5d, 5e and 5f) expressed greater verve athwart negative bacteria in comparison with that of the reference antibiotic (Gentamycin).

1.
J.
Yamaguchi
.,
E
Shibuta
and,
Y.
Oishi
,
International Journal of Organic Chemistry
,
2014
,
4
,
286
291
.
2.
M.
Caterina
,
M.
Corona
,
C.
de los Santos
and,
M.
Abasolo
,
Arkivoc
,
2014
,
iv
,
228
241
.
3.
H.K.
Ibrahim
,
Egyptian Journal of Chemistry
,
2006
,
45
,
225
240
.
4.
M.
Boca
, p
Baran
,
R Boca
,
Fuess
H.
,
G.
Kickelbick
,
W.
Linert
,
F. Renz
and
,
I.
Svoboda
,
Inorganic Chemistry
,
2000
,
39
,
3205
3212
.
5.
Da Silva Guerra
,
A.S.H.
,
D.J. Do Nascimento
Malta
,
L.P. Morais
Laranjeira
,
M.B. Souza
Maia
,
N. Cavalcanti
Colaco
.,
M. Do Carmo
Alves De Lima
,
S.L.
Galdino
,
I. Da Rocha
Pitta
, and
T.
Goncalves-Silva
,
International Immunopharmacology
,
2011
,
11
,
1816
1822
.
6.
Y.
Brouillette
,
V.
Lisowski
,
J.
Guillon
,
S
Massip
and
Martinez
,
J.
,
Tetrahedron
,
2007
,
63
,
7538
7544
.
7.
J.F.C.
Albuquerque
,
J.A.R.
Filho
,
S.S.F.
Brandao
,
M.C.A.
Lima
, and et al,
Farmaco
,
1999
,
54
,
77
82
.
8.
M.
Arrowsmith
,
M.S Hill
and
,
G.
Kociok-kohn
,
Chemistry - A European Journal
,
2015
,
21
,
10548
10557
.
9.
G.
Baccolini
,
C.
Boga
,
C.
Delpivo
,
G.
Micheletti
,
Tetrahedron Letters
,
2011
,
52
,
1713
1717
.
10.
R
Badru
. and,
B.
Singh
,
RSC Advances
,
2014
,
4
,
38978
38985
.
11.
M.
Kratky
,
J.
Mandikova
,
F.
Trejtnar
,
V.
Buchta
,
J.
Stolarikova
and
J.
Vinsova
,
Chemical Papers
,
2015
,
69
,
1108
1117
.
12.
R.S.
Kumar
,
A.
Idhayadhulla
,
A.J.A
Nasser
and
J.
,
Selvin
,
Oriental Journal of Chemistry
,
2010
,
26
,
1425
1430
.
13.
M.J.
Lee
and
Sun
,
C.M.
,
Tetrahedron Letters
,
2004
,
45
,
437
440
.
14.
A.
Ahmedova
,
P.
Marinova
,
K.
Paradowska
,
M.
Marinov
,
I.
Wawer
and
M.
Mitewa
,
Polyhedron
,
2010
,
29
,
1639
1645
.
15.
M.C.P.A.
Albuquerque
,
T.G.
Silva
,
M.G.R.
Pitta
,
A.C.A.
Silva
,
E.
Malagueno
,
J. V.
Santana
,
A.G.
Wanderley
,
M.C.A.
Lima
,
S.L.
Galdino
,
J.
Barbe
,
I.R.
Pitta
,
Pharmazie
,
2005
,
60
,
13
17
.
16.
M.M.
Ghanbari
,
J.
Safari
and
Z.
Roohi
,
Open Access Library Journal
,
2014
,
1
,
1
5
.
17.
E.K.
Beloglazkina
,
A.G
Majoouga
,
A.V.
Mironov
,
A.V.
Yudina
,
O.Y.
Kuznetsova
and
N.V.
Zyk
,
Polyhedron
,
2014
,
76
,
45
50
.
18.
A.
Czopek
,
H.
Byrtus
,
M.
MKolaczkowsk
,
Pawlowski
,
M.
Dybala
,
G.N.
Owak
,
E.
Tatarczynska
,
A.
Wesolowska
, and
E.
Chojnacka-Wojcik
,
European Journal of Medicinal Chemistry
,
2010
,
45
,
1295
1303
.
19.
A
Czopek
,
M.
,
Kolaczkowski
,
A.
Bucki
,
H.
Byrtus
,
M.
Pawlowski
,
G.
Kazek
,
A.J.
Bojarski
,
Piaskowska
,
A.
,
J.
Kalinowska-Tuscik
,
A.
Partyka
, and
A.
Wesolowska
,
Bioorganic and Medicinal Chemistry
,
2015
,
23
,
3436
3447
.
20.
S
Sanchit
and
S.
Pandeya
.,
International Journal of Research in Ayurveda & Pharmacy
,
2011
,
2
,
459
468
.
21.
B.
Mukesh
,
S. Vandana
and
,
K.
Rekesh
.,
International Journal of Pharmacy
,
2011
,
2
,
84
89
.
22.
N.
Hebert;
h,
A.L.
Hanna
and n,
S.C.
Sutto
,
Tetrahedron Letters
,
1999
,
40
,
8547
8550
.
23.
R.
Dass
,
G.S.
Ashthana
,
K.A.
Suri
,
D.K.
Metha
and
A.
Asthana
,
Journal of Pharmaceutical Science and Research
,
2015
,
7
,
806
811
.
24.
B.
Nimavat
.,
S.
Mohan
,
J.
Saravanan
,
S.
Deka
,
A
Talukdar
,
B. J.
Sahariah
,
B.K.
Dey
,
R.K.
Sarma
,
International Journal of Research in Pharmacy and Chemistry
,
2012
,
2
,
594
602
.
25.
R.R.
Somani
,
A.G.
Agrawal
,
P.P.
Kalantri
,
P.S Gavarkar
and
,
E.D.
Clercq
,
International Journal of Drug Design and Discovery
,
2011
,
2
,
353
360
.
26.
B
Sadek
.,
K.
Mustafa
and,
S.
Fahelelbom
,
Molecules
,
2011
,
4339
4347
.
27.
R.W.
Yong
, and
K. H.
Wood
,
Journal American Chemistry Society.
,
1955
,
77
,
400
403
.
28.
Acton
,
Q.A.
,
Azo Compounds: Advances in Research and Application
,
Scholarly Paper Edition
,
Atlanta
,
2011
.
29.
Z.H
Abood
.,
H.A.
Qabel
and,
H.R.
Ali
,
Journal of Physics: Conf. Series
,
1032
(
2018
)
012058
.
30.
N.S.
Egorove
,
Antibiotics Scientific Approach, Mir
.
Publishers
,
Moscow
,
1985
.
This content is only available via PDF.