مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Information Journal Paper

Title

ANTI-HELICOBACTER PYLORI ACTIVITY AND STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF 2-ALKYLTHIO-5- (NITROARYL) -1, 3, 4-THIADIAZOLE DERIVATIVES

Pages

  281-287

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 mg/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 a-methylbenzylthio side chain at C-2 position of thiadiazole ring, showed strong inhibitory response against metronidazole resistant H. pylori isolates at 12.5 mg/disk (the inhibition zone diameter at all evaluated concentrations (12.5- 100 mg/disk) is > 50 mm). Novel 5- (5-nitroaryl) -1, 3, 4-THIADIAZOLE scaffold bearing different C-2 attached thiopendant 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.

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    • Cite

    APA: Copy

    ASADIPOUR, ALI, EDRAKI, NAJMEH, NAKHJIRI, MARYAM, YAHYA MEYMANDI, AZADEH, ALIPOUR, ESKANDAR, SANIEE, PARASTOO, SIAVOSHI, FARIDEH, SHAFIEE, ABBAS, & FOROUMADI, ALIREZA. (2013). ANTI-HELICOBACTER PYLORI ACTIVITY AND STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF 2-ALKYLTHIO-5- (NITROARYL) -1, 3, 4-THIADIAZOLE DERIVATIVES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 12(3), 281-287. SID. https://sid.ir/paper/288106/en

    Vancouver: Copy

    ASADIPOUR ALI, EDRAKI NAJMEH, NAKHJIRI MARYAM, YAHYA MEYMANDI AZADEH, ALIPOUR ESKANDAR, SANIEE PARASTOO, SIAVOSHI FARIDEH, SHAFIEE ABBAS, FOROUMADI ALIREZA. ANTI-HELICOBACTER PYLORI ACTIVITY AND STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF 2-ALKYLTHIO-5- (NITROARYL) -1, 3, 4-THIADIAZOLE DERIVATIVES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2013;12(3):281-287. Available from: https://sid.ir/paper/288106/en

    IEEE: Copy

    ALI ASADIPOUR, NAJMEH EDRAKI, MARYAM NAKHJIRI, AZADEH YAHYA MEYMANDI, ESKANDAR ALIPOUR, PARASTOO SANIEE, FARIDEH SIAVOSHI, ABBAS SHAFIEE, and ALIREZA FOROUMADI, “ANTI-HELICOBACTER PYLORI ACTIVITY AND STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF 2-ALKYLTHIO-5- (NITROARYL) -1, 3, 4-THIADIAZOLE DERIVATIVES,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 12, no. 3, pp. 281–287, 2013, [Online]. Available: https://sid.ir/paper/288106/en

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