ChemInform Abstract: POTENTIAL BROAD SPECTRUM ANTHELMINTICS. PART 4: DESIGN, SYNTHESIS AND SPECTRAL STUDY OF IMIDAZO(2,1-B)-1,3,4-THIADIAZOLE DERIVATIVES

1979 ◽  
Vol 10 (28) ◽  
Author(s):  
M. A. ELDAWY ◽  
S. A. SHAMS EL-DINE ◽  
K. M. EL-BREMBALY
Keyword(s):  
Broad Spectrum ◽  
Spectral Study ◽  
Design Synthesis ◽  
Thiadiazole Derivatives

Design, Synthesis, and Biological Characterization of Bivalent 1-Methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole Derivatives as Selective Muscarinic Agonists

2001 ◽  
Vol 44 (26) ◽  
pp. 4563-4576 ◽  
Author(s):  
W. G. Rajeswaran ◽  
Yang Cao ◽  
Xi-Ping Huang ◽  
Mary Elizabeth Wroblewski ◽  
Tracy Colclough ◽  
...  
Keyword(s):  
Biological Characterization ◽  
Muscarinic Agonists ◽  
Design Synthesis ◽  
Thiadiazole Derivatives

scholarly journals Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2

2020 ◽  
Vol 11 (12) ◽  
pp. 1379-1385
Author(s):  
R. Kirk ◽  
A. Ratcliffe ◽  
G. Noonan ◽  
M. Uosis-Martin ◽  
D. Lyth ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Bacterial Infections ◽  
Rational Design ◽  
Topoisomerase Ii ◽  
Topoisomerase Inhibitors ◽  
Design Synthesis ◽  
Pharmacokinetic Properties ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

We disclose the discovery of REDX07965, a novel tricyclic topoisomerase inhibitor (NTTI) which has broad spectrum activity, favourable in vitro pharmacokinetic properties and selectivity versus human topoisomerase II.

Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents

2016 ◽  
Vol 71 (3) ◽  
pp. 205-210 ◽  
Author(s):  
Ali Almasirad ◽  
Loghman Firoozpour ◽  
Maliheh Nejati ◽  
Najmeh Edraki ◽  
Omidreza Firuzi ◽  
...  
Keyword(s):  
Human Tumor ◽  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Antitumor Activities ◽  
Design Synthesis ◽  
Ethidium Bromide Staining ◽  
Thiadiazole Derivatives ◽  
Synthesis And Biological Evaluation

AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

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