Abstract:A new series of 2-[(chlorobenzyl)thio]-5-(5-nitro-2-furyl)-1,3,4-thiadiazoles (6a-h) were synthesized and evaluated by the disc diffusion method against Helicobacter pylori. Four compounds which exhibited strong anti-H. pylori activity at concentration of 8-32 lg/disc (average of inhibition zone[20 mm) were further tested against 20 clinical isolates of H. pylori at lower concentrations. The averages of inhibition zone diameters indicated that all selected compounds exhibit better anti-H. pylori activity profi… Show more
“…tested eight compounds in a series of 2‐[(chlorobenzyl)thio]‐5‐(5‐nitro‐2‐furyl)‐1,3,4‐thiadiazoles for possible anti‐ H. pylori activity. Of eight, four derivatives showed strong anti‐ H. pylori activity at concentration of 8–32 μg/disk and compound 57 containing the 3‐chlorobenzylthio moiety was found to exhibit the most potent and selective inhibitory activity against H. pylori with an inhibition zone of more than 20 mm at a concentration of 8 μg/disk .…”
The 1,3,4-thiadiazole nucleus is one of the most important and well-known heterocyclic nuclei, which is a common and integral feature of a variety of natural products and medicinal agents. Thiadiazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, and antitubercular agents. The broad and potent activity of thiadiazole and their derivatives has established them as pharmacologically significant scaffolds. In this study, an attempt has been made with recent research findings on this nucleus, to review the structural modifications on different thiadiazole derivatives for various pharmacological activities.
“…tested eight compounds in a series of 2‐[(chlorobenzyl)thio]‐5‐(5‐nitro‐2‐furyl)‐1,3,4‐thiadiazoles for possible anti‐ H. pylori activity. Of eight, four derivatives showed strong anti‐ H. pylori activity at concentration of 8–32 μg/disk and compound 57 containing the 3‐chlorobenzylthio moiety was found to exhibit the most potent and selective inhibitory activity against H. pylori with an inhibition zone of more than 20 mm at a concentration of 8 μg/disk .…”
The 1,3,4-thiadiazole nucleus is one of the most important and well-known heterocyclic nuclei, which is a common and integral feature of a variety of natural products and medicinal agents. Thiadiazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, and antitubercular agents. The broad and potent activity of thiadiazole and their derivatives has established them as pharmacologically significant scaffolds. In this study, an attempt has been made with recent research findings on this nucleus, to review the structural modifications on different thiadiazole derivatives for various pharmacological activities.
“…Nowadays, for developing new potential anti-H. pylori candidates, scientists in the medicinal chemistry field are also equally concerned with the creation of new synthetic drug compounds (Foroumadi et al, 2008a(Foroumadi et al, ,b, 2009aLetafat et al, 2008;Mohammadhosseini et al, 2008Mohammadhosseini et al, , 2009Moshafi et al, 2011;Tafti et al, 2011). Complementary and alternative modes of treatment, particularly non-toxic, natural, and inexpensive products are attractive.…”
Context: Helicobacter pylori is a small, spiral, Gram-negative bacillus that plays a role in the pathogenesis of a number of diseases ranging from asymptomatic gastritis to gastric cancer. Schedule compliance, antibiotic drug resistance, and side-effects of triple or quadruple therapy have led to research for novel candidates from plants.Objective: The purpose of this paper is to review the most potent medicinal plants of recently published literature with anti-H. pylori activity. For centuries, herbals have been used by traditional healers around the world to treat various gastrointestinal tract disorders such as dyspepsia, gastritis, and peptic ulcer disease. The mechanism of action by which these botanicals exert their therapeutic properties has not been completely and clearly elucidated. Anti-H. pylori properties may be one of the possible mechanisms by which gastroprotective herbs treat gastrointestinal tract disorders. Materials and methods: Electronic databases such as PubMed, Google scholar, EBSCO, and local databases were explored for medicinal plants with anti-H. pylori properties between 1984 and 2013 using key words ''medicinal plants'' and ''Helicobacter pylori'' or ''anti-Helicobacter pylori''. Results: A total of 43 medicinal plant species belonging to 27 families including Amaryllidaceae,
“…In particular, the highest antiproliferative activity was found for 2-(2,4-dichlorophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole (876), with an ID 50 two times lower (human cell lines SW707 and T47D) than cisplatin studied comparatively as the control compound [373]. It is also used as bactericidal; compounds 877 and 878 are active against Helicobacter pylori [374]. Moreover many 1,3,4-thiadiazole derivatives have also been patented in the agricultural field as pesticides, herbicides, insecticides, fungicides, and so on.…”
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