2015
DOI: 10.1248/cpb.c15-00059
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Synthesis and Anticancer Evaluation of 1,3,4-Oxadiazoles, 1,3,4-Thiadiazoles, 1,2,4-Triazoles and Mannich Bases

Abstract: A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydrazide. Aminoalkylation of compounds 5a-d with formaldehyde and various secondary amines furnished the Mannich bases 6a-p. The structures of the newly synthesized compounds were confirmed on the ba… Show more

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Cited by 39 publications
(13 citation statements)
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“…Investigations of 1,3,4-thiadiazole compounds, in particular their di-substituted derivatives, represent a majority in the available literature, probably due to their pharmacological effects. Literature presents the entire thiadiazol family as compounds with anticancer [ 2 , 4 6 ], antifungal [ 7 ], antibacterial [ 7 ], anticonvulsant [ 8 ], anti-inflammatory [ 9 , 10 ], antihypertensive [ 9 ], antiviral [ 7 ], radioprotective [ 7 ], antidepressant and antioxidant [ 11 ], or insecticidal [ 9 ] activity.…”
Section: Introductionmentioning
confidence: 99%
“…Investigations of 1,3,4-thiadiazole compounds, in particular their di-substituted derivatives, represent a majority in the available literature, probably due to their pharmacological effects. Literature presents the entire thiadiazol family as compounds with anticancer [ 2 , 4 6 ], antifungal [ 7 ], antibacterial [ 7 ], anticonvulsant [ 8 ], anti-inflammatory [ 9 , 10 ], antihypertensive [ 9 ], antiviral [ 7 ], radioprotective [ 7 ], antidepressant and antioxidant [ 11 ], or insecticidal [ 9 ] activity.…”
Section: Introductionmentioning
confidence: 99%
“…Piperidine-bearing compounds are known to have significant anti-cancer potential, as proved in the literature [79]. From the previous data, it is evident that the electronegativity of the substituents at the heterocyclic ring steer the magnitude of activity [80], as in the case of SF9 with an electronegative bromine atom in it. The method is not specific to anti-tumor activity.…”
Section: Cytotoxicity Against Raw Macrophages and Cancer Cell Lines (mentioning
confidence: 86%
“…Cancer is one of the most dreaded disease, characterised by metastasis, invasion, and uncontrolled cell growth (Megally Abdo and Kamel, 2015 ). Chemotherapy, radiation, and surgery are the major techniques among many, contemporarily applied for cancer treatment.…”
Section: The Triazoles As Agents Against Microorganismsmentioning
confidence: 99%