“…A series of 2‐(bis(1,3,4‐thiadiazolyl) methylthio)methylene)malononitriles were synthesized and evaluated in vitro against S. aureus , Bacillus subtilis , E. coli and Klebsiealla pneumonia . Among the synthesized compounds, 2‐(bis((5‐(4‐chlorophenyl)‐1,3,4‐thiadiazol‐2‐yl)methylthio) methylene) malononitrile ( 13 ) showed significant activity against S. aureus with zone of inhibition of 35 mm at a concentration of 200 μg/mL .…”
Section: Methodsmentioning
confidence: 99%
“…Antibacterial activity in a series of 3-(1,3,4-thiadiazole-2-yl) quinolines was found to be depended strongly on substitution at C5 and C2 of thiadiazole. From the findings, Bhat et al [9] revealed that thiadiazole derivatives substituted with N-(o-tolyl)acetamide (10) and N-(p-tolyl)acetamide (11) groups at C2 and 2,8-dichloroquinoline and 2-chloroquinoline at C5 showed better activity against S. aureus and S. pyogenes, respectively. He et al [10] carried out synthesis of 5-(1-aryl-1H-tetrazol-5-ylsulfanylmethyl)-N-xylopyranosyl-1,3,4-thiadiazole-2amine derivatives and investigated in vitro antibacterial activity against S. aureus.…”
Section: Biological Activity Of 4-thiazolidinonesmentioning
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.
“…A series of 2‐(bis(1,3,4‐thiadiazolyl) methylthio)methylene)malononitriles were synthesized and evaluated in vitro against S. aureus , Bacillus subtilis , E. coli and Klebsiealla pneumonia . Among the synthesized compounds, 2‐(bis((5‐(4‐chlorophenyl)‐1,3,4‐thiadiazol‐2‐yl)methylthio) methylene) malononitrile ( 13 ) showed significant activity against S. aureus with zone of inhibition of 35 mm at a concentration of 200 μg/mL .…”
Section: Methodsmentioning
confidence: 99%
“…Antibacterial activity in a series of 3-(1,3,4-thiadiazole-2-yl) quinolines was found to be depended strongly on substitution at C5 and C2 of thiadiazole. From the findings, Bhat et al [9] revealed that thiadiazole derivatives substituted with N-(o-tolyl)acetamide (10) and N-(p-tolyl)acetamide (11) groups at C2 and 2,8-dichloroquinoline and 2-chloroquinoline at C5 showed better activity against S. aureus and S. pyogenes, respectively. He et al [10] carried out synthesis of 5-(1-aryl-1H-tetrazol-5-ylsulfanylmethyl)-N-xylopyranosyl-1,3,4-thiadiazole-2amine derivatives and investigated in vitro antibacterial activity against S. aureus.…”
Section: Biological Activity Of 4-thiazolidinonesmentioning
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.
“…Although chemotherapy is the mainstay of cancer therapy, the use of available chemotherapeutics is often limited mainly due to undesirable side effects and a limited choice of available anticancer drugs (Goutham Vemana et al 2014). 2-Aminothiophenes exhibit several pharmacological activities and have therefore attracted considerable attention from medicinal and synthetic organic chemists (Behbehani et al, 2012;Du et al, 2013;Padmavathi et al, 2011;Wang et al, 2013;Titchenell et al, 2013;Aurelio et al, 2011;Perspicace et al, 2013;Duval et al, 2005). They have been described to present anti-inflammatory (Madhusudana et al, 2012), insecticidal (Campaigne, 1984), antibacterial (Dewal et al, 2012), antifungal (Stephens et al, 2001), antiviral (Goncales et al, 2005), and antinociceptive activities (Crouse et al, 2004).…”
The reaction of 2-amino-3-cyano-4,5,6,7-tetrahydrobenzo [b]thiophene with chloroacetyl chloride gave the 2-chloroacetamido derivative 3. The latter reacted with hydrazine hydrate to give the hydrazine derivative 5 which was used to form the hydrazone derivatives 7a, b and 9a, b via its reaction with some carbonyl compounds. Moreover, it produced the pyrazole derivatives 11a, b through its reaction with either acetylacetone or ethyl acetoacetate. On the other hand, compounds 5 and 3 were used to form some thiazole, pyridine, and fused derivatives. The cytotoxicity of the newly obtained products was evaluated against some of the human cancer and normal cell lines where the results showed that compounds 3, 11b, 13, 18c, 18d, 21, 23, and 24 exhibited optimal cytotoxic effect against cancer cell lines, with IC 50 's in the nM range.
“…The compounds containing 1,3,4‐thiadiazole moiety show interesting pharmacological activities as well as properties useful from the technological and agricultural point of view . Their antibacterial, antiviral, anticancer, antiparasitic, anti‐inflammatory, anticholinergic and antihistamine activities have been widely studied. Some compounds belonging to this class are potent radioprotective agents .…”
The (1) H, (13) C and (15) N spectra of aryl-substituted 1,3,4-thiadiazoles were recorded. The results obtained were correlated with Hammett coefficients. The experimental results were compared with DFT-calculated chemical shifts. The results obtained were compared with those for 1,3,4-oxadiazoles and 1,3,4-selenadiazoles.
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