39181-55-0Relevant academic research and scientific papers
Synthesis and anticancer activity of thiadiazole containing thiourea, benzothiazole and imidazo[2,1-b][1,3,4]thiadiazole scaffolds
Avvaru, Stephen Paul,Noolvi, Malleshappa N.,More, Uttam A.,Chakraborty, Sudipta,Dash, Ashutosh,Aminabhavi, Tejraj M.,Narayan, Kumar P.,Sutariya, Vishnu
, p. 750 - 765 (2021/04/02)
Background: A great array of nitrogen-containing heterocyclic rings were being extensively explored for their functional versatility in the field of medicine, especially in anticancer research. 1,3,4-thiadiazole is one of such heterocyclic rings with prom
Synthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells
An, Ran,Guo, Chun,Li, Qing,Li, Yan,Wang, Renxiao,Xu, Yaochun,Zhou, Mi
supporting information, (2020/03/25)
A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an in-house cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1–5 μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry analysis of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50 μM on HEK-293T cells. Although the molecular targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.
Gamma-glutamyl transpeptidase inhibitors and methods of use
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Page/Page column 4; 27, (2017/01/31)
Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.
THIADIAZOLE AND OXADIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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, (2013/03/26)
The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine
Badiger, Naveen P.,Khan, Ashraf,Kalashetti,Khazi
, p. 1544 - 1549 (2012/11/07)
Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model. Springer Science+Business Media, LLC 2011.
Divergent effects of compounds on the hydrolysis and transpeptidation reactions of γ-glutamyl transpeptidase
Wickham, Stephanie,Regan, Nicholas,West, Matthew B.,Kumar, Vidya Prasanna,Thai, Justin,Li, Pui Kai,Cook, Paul F.,Hanigan, Marie H.
experimental part, p. 476 - 489 (2012/09/22)
A novel class of inhibitors of the enzyme γ-glutamyl transpeptidase (GGT) were evaluated. The analog OU749 was shown previously to be an uncompetitive inhibitor of the GGT transpeptidation reaction. The data in this study show that it is an equally potent uncompetitive inhibitor of the hydrolysis reaction, the primary reaction catalyzed by GGT in vivo. A series of structural analogs of OU749 were evaluated. For many of the analogs, the potency of the inhibition differed between the hydrolysis and transpeptidation reactions, providing insight into the malleability of the active site of the enzyme. Analogs with electron withdrawing groups on the benzosulfonamide ring, accelerated the hydrolysis reaction, but inhibited the transpeptidation reaction by competing with a dipeptide acceptor. Several of the OU749 analogs inhibited the transpeptidation reaction by slow onset kinetics, similar to acivicin. Further development of inhibitors of the GGT hydrolysis reaction is necessary to provide new therapeutic compounds.
Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6- (4′-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents
Karki, Subhas S.,Panjamurthy, Kuppusamy,Kumar, Sujeet,Nambiar, Mridula,Ramareddy, Sureshbabu A.,Chiruvella, Kishore K.,Raghavan, Sathees C.
experimental part, p. 2109 - 2116 (2011/06/21)
Levamisole, the imidazo[2,1-b]thiazole derivative has been reported as a potential antitumor agent. In the present study, we synthesized, characterized and evaluated biological activity of its novel analogues with substitution in the aralkyl group and on
THIADIAZOLE DERIVATIVES, INHIBITORS OF STEAROYL-COA DESATURASE
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Page/Page column 57, (2008/12/07)
The present invention relates to substituted thiadiazole compounds of the formula (I) and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.
2-Amino-5-(substituted or unsubstituted phenylalkyl)-thiadiazoles
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, (2008/06/13)
2-amino-5-(substituted or unsubstituted phenylalkyl)-thiadiazoles, e.g., 2-amino-5-(4-[phenylbutyl])-thiadiazole, prepared, e.g., by ring closure, of corresponding 1-(substituted or unsubstituted phenylalkanoyl)-thiosemicarbazide in a strong acid medium.
