- 6-Phenyl-3-(4-pyridyl)-1,2,4-triazolo-[3,4-b][1,3,4]thiadiazole
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The title compound, C14H9N5S, has been synthesized and characterized both spectroscopically and structurally. The triazolo-thiadiazole system, the pyridine ring and the phenyl ring are all planar. The plane of the triazolo
- Dincer, Muharrem,Oezdemir, Namik,Cetin, Ahmet,Cansiz, Ahmet,Bueyuekguengoer, Orhan
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- 6-Phenyl-3-(4-pyridyl)-1,2,4-triazolo-[3,4-b][1,3,4]thiadiazole: Synthesis, experimental, theoretical characterization and biological activities
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The molecular geometry, vibrational frequencies, and gauge including atomic orbital (GIAO) 1H and 13C NMR chemical shift values of the title compound in the ground state have been calculated using the Hartree-Fock (HF) and density fu
- Cansiz, Ahmet,Cetin, Ahmet,Orek, Cahit,Karatepe, Mustafa,Sarac, Kamiran,Kus, Alper,Koparir, Pelin
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- New CuII and CdII Metal-organic Coordination Polymers with 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole Ligands: Syntheses, Structures and Luminescent Properties
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Three new complexes {[Cu(L1)2(NO3)2]H2O}oo (1), {[Cu4(L2)2(OAc)8]-CH3CH2OH}oo (2) and [Cd2(L3/s
- Fan, Jian-Zhong,Li, Jin-Ping,Zhang, Li-Peng,Zhang, Liu-Gen,Wang, Duo-Zhi
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- 3. 6 - Disubstituted [1, 2, 4] triazolo [3, 4 - b] [1, 3, 4] thiadiazole compound and use thereof
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The invention discloses 3,6-disubstituted[1,2,4]triazolyl[3,4-b][1,3,4]thiadiazole compounds represented by general formula (I), and pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof. The compounds can be used as a transpeptidase SrtA inhibitor of Staphylococcus aureus, Bacillus pyogenes, Bacillus anthracis, Streptococcus pneumoniae and other Gram-positive bacteria, and can be used to prepare drugs for treating pathogen infection diseases with the transpeptidase SrtA of the Gram-positive bacteria, such as Staphylococcus aureus, Bacillus pyogenes, Bacillus anthracis and Streptococcus pneumoniae as target. The compounds avoid selection pressure induced drug resistance of pathogens to a certain degree, and mitigate threat of continuous drug-resistant pathogens to the health of human.
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Paragraph 0052; 0060; 0069
(2018/11/22)
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- Synthesis of novel 1,2,4-triazoles, triazolothiadiazines and triazolothiadiazoles as potential anticancer agents
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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).
- Kamel, Mona M.,Megally Abdo, Nadia Y.
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- 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
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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.
- Gilani, Sadaf Jamal,Khan, Suroor Ahmad,Alam, Ozair,Siddiqui, Nadeem
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p. 205 - 211
(2011/10/09)
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- Synthesis, anti-inflammatory, analgesic, and antibacterial activities of some triazole, triazolothiadiazole, and triazolothiadiazine derivatives
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This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4- thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)- 5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde
- Hussein, Mostafa A.,Shaker, Refaat M.,Ameen, Mohammed A.,Mohammed, Mohammed F.
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experimental part
p. 1239 - 1250
(2012/05/20)
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- Synthesis of some 1, 2, 4-triazole derivatives and investigation of their fungicidal activities
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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.
- Singh, Ram Janam,Singh, Dharmendra Kumar
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p. 235 - 239
(2011/10/08)
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- 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
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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.
- Gilani, Sadaf J.,Khan, Suroor A.,Siddiqui, Nadeem
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experimental part
p. 4762 - 4765
(2010/10/04)
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- Synthesis and biological activity of some triazolothiadiazoles
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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.
- Singh, Ram J.,Singh, Dharmendra K.
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experimental part
p. 105 - 108
(2010/09/04)
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- Synthesis and pharmacological properties of 6-substituted 3-(pyridine-4-yl)-1,2,4-triazole [3,4-b][1,3,4]thiadiazoles
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A number of new 6-substituted 3-(pyridine-4-yl) 1,2,4-triazole[3,4-b][1,3,4]thiadiazoles were synthesized and evaluated for their pharmacological activity. Some of them exhibited moderate MAO, antimalarial and in vitro antitumor activity.
- Invidiata,Grimaudo,Giammanco,Giammanco
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p. 1489 - 1495
(2007/10/02)
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