Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 3 de 3
Filter
Add filters








Language
Year range
1.
IJPR-Iranian Journal of Pharmaceutical Research. 2013; 12 (3): 281-287
in English | IMEMR | ID: emr-138284

ABSTRACT

Nitro-containing heteroaromatic derivatives structurally related to nitroimidazole [Metronidazole] are being extensively evaluated against Helicobacter pylori isolates. On the other hand, 1,3,4-thiadiazole derivatives have also demonstrated promising antibacterial potential. In present study, we evaluated anti-H. pylori activity of novel hybrid molecules bearing nitroaryl and 1,3,4-thiadiazole moieties. Anti-H. pylori activity of novel 5-[5-nitroaryl]-1,3,4-thiadiazole derivatives bearing different bulky alkylthio side chains at C-2 position of thiadiazole ring, were assessed against three different metronidazole resistant H. pylori isolates by paper disk diffusion method. Most of the compounds demonstrated moderate to strong inhibitory response especially at 25 micro g/disk. The structure-activity relationship study of the compounds demonstrated that introduction of different alkylthio moieties at C-2 position of thiadiazole ring alter the inhibitory activity which is mainly dependent on the type of C-5 attached nitrohetercyclic ring. The promising compound of this scaffold, bearing 1-methyl-5-nitroimidazole moiety at C-5 and alpha -methylbenzylthio side chain at C-2 position of thiadiazole ring, showed strong inhibitory response against metronidazole resistant H. pyloriisolates at 12.5 micro g/disk [the inhibition zone diameter at all evaluated concentrations [12.5-100 micro g/disk] is > 50 mm]. Novel 5-[5-nitroaryl]-1,3,4-thiadiazole scaffold bearing different C-2 attached thio-pendant moieties with promising anti-H. pylori potential were identified. Among different nitroheterocycles, 5-nitrofuran and 5-nitroimidazole moieties were preferable for the substitution at C-5 position of 1,3,4-thiadiazole ring. Introduction of different alkylthio side chains at C-2 position of central ring alter the inhibitory activity which is mainly dependent on the type of C-5 attached nitrohetercyclic ring


Subject(s)
Heterocyclic Compounds/chemical synthesis , Helicobacter pylori/growth & development , Structure-Activity Relationship
2.
DARU-Journal of Faculty of Pharmacy Tehran University of Medical Sciences. 2005; 13 (4): 160-164
in English | IMEMR | ID: emr-70335

ABSTRACT

Centaurea aucheri [DC.] Wagenitz is one of the species of Asteraceae that has not been the subject of many investigations. Different species of this genus have been used in traditional medicine. In this investigation C. aucheri was collected from Khanesorkh of Kerman and the essential oil of the aerial parts of plant was extracted by Clevenger apparatus and analyzed by GC-MS. Identification of the components of oils were based on their retention indices and mass spectra data in comparison with those reported in literatures. The amount of essential oil was 0.16% and 22 substances consisting 80.03% of the composition of the essential oil were identified. The main compounds were caryophyllene oxide [19.44%], beta-caryophyllene [14%], Geremacrene-D [13.38%]. The essential oil was rich in sesquiterpene oil


Subject(s)
Oils, Volatile , Gas Chromatography-Mass Spectrometry
3.
DARU-Journal of Faculty of Pharmacy Tehran University of Medical Sciences. 2004; 12 (3): 98-100
in English | IMEMR | ID: emr-65648

ABSTRACT

The essential oil from flowering aerial parts of Nepeta depauperata Benth., an endemic Iranian plant, obtained by steam distillation was analyzed by GC/MS. The constituents were identified by their mass spectra and Kovats' indices. Thirty-three compounds consisting 82.52% of the total components were identified from the oil obtained with a yield of 0.3%v/w. Among them, spathulenol [31.84%], beta caryophyllene [12.93%] and caryophyllene oxide [10.27%] were the major components of the oil


Subject(s)
Plant Structures , Plant Oils/isolation & purification , Gas Chromatography-Mass Spectrometry
SELECTION OF CITATIONS
SEARCH DETAIL