478362-75-3Relevant academic research and scientific papers
Synthesis of novel 1,2,4-triazoles, triazolothiadiazines and triazolothiadiazoles as potential anticancer agents
Kamel, Mona M.,Megally Abdo, Nadia Y.
, p. 75 - 80 (2014/11/07)
A series of new N-substituted-3-mercapto-1,2,4-triazoles (3a,b and 7a-d), triazolo[1,3,4]thiadiazines (5a,b) and triazolo[1,3,4]thiadiazoles (4a-d, 6 and 8a-d) have been synthesized starting from isonicotinic acid hydrazide. The structure of the newly synthesized compounds was confirmed on the basis of their spectral data and elemental analyses. All the compounds were screened for their in vitro anticancer activity against 6 human cancer cell lines and normal fibroblasts. Seven of the tested compounds (3a,b, 4c, 5a and 8b-d) exhibited significant cytotoxicity against most cell lines. Among these derivatives compound 4c exhibited equivalent cytotoxic effect to the standard CHS 828 against gastric cancer cell line (IC50 = 25 nM). Normal fibroblast cells (WI38) were affected to a much lesser extent (IC50 > 10,000 nM).
Synthesis and in vitro antimicrobial evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid
Gilani, Sadaf Jamal,Khan, Suroor Ahmad,Alam, Ozair,Siddiqui, Nadeem
, p. 205 - 211 (2011/10/09)
A series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g, 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their in vitro antimicrobial activity. All the synthesized compounds were in good agreement with elemental and spectral data. A majority of the tested compounds showed good to moderate antimicrobial activity against all tested pathogenic bacterial and fungal strains.
Synthesis of some 1, 2, 4-triazole derivatives and investigation of their fungicidal activities
Singh, Ram Janam,Singh, Dharmendra Kumar
, p. 235 - 239 (2011/10/08)
The synthesis of a series of 3-pyridyl-6-aryl-s-triazolo (3. 4-b) (1, 3. 4) - thiadiazoles are described, synthesis of 3-pyndyl-6-aryl-s-triazolo (3. 4-b) (1, 3, 4) - thiadiazoles (3a-m) have been achieved by the condensation of potassium dithiocarbazinate (1) with hydrazine hydrate and water. was under reflux 8 hours to yield 4-amino-3-pyridyl-5-mercapto-s-triazole (2). followed bv treatment with aromatic acid The compounds (3a-m) were characterized by spectral and elemental analyses. All thirteen compounds have been assayed for their fungicidal activity against P. oryzae. B. cinerea, A. nigar, C. albicans and T. rubrum. Compounds containing aryl substituents at position six and the 1. 2, 4-triazole moiety at position one or two showed reasonable fungicidal activity.
Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid
Gilani, Sadaf J.,Khan, Suroor A.,Siddiqui, Nadeem
experimental part, p. 4762 - 4765 (2010/10/04)
The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g and 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models.
Synthesis and biological activity of some triazolothiadiazoles
Singh, Ram J.,Singh, Dharmendra K.
experimental part, p. 105 - 108 (2010/09/04)
The synthesis of a series of novel 3-pyridyl-6-aryl-s-triazolo[3,4-b]-[1,3, 4]-thiadiazoles is described. Fourteen new compounds were synthesized and characterized by spectral and elemental analyses. Some compounds were screened for antibacterial activity against S. aureus, E. coli, B. subtilis and P. aeruginosa. Compounds containing aryl substituents at position 6 and the 1,2,4-triazole moiety at position 1 or 2 showed reasonable antibacterial activity.
