21911-89-7Relevant academic research and scientific papers
Synthesis and antimicrobial activity of some 2,5-disubstituted 1,3,4-oxadiazoles
Honnalli,Ronad,Vijaybhasker,Hukkeri,Kumar, Rajiv
, p. 505 - 508 (2005)
4-Chloro aniline is condensed with methyl acrylate in presence of acetic acid to yield methyl-β-(4-chloro methyl aniline)-propionate, which was futher treated with hydrazine hydrate in presence of ethanol to obtain β -alanine-N-(4-chloro methyl-phenyl) hy
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA- methyltransferase, DNA mismatch repair, and p53
Pletsas, Dimitrios,Garelnabi, Elrashied A.E.,Li, Li,Phillips, Roger M.,Wheelhouse, Richard T.
, p. 7120 - 7132 (2013/10/01)
The antitumor prodrug temozolomide is compromised by its dependence for activity on DNA mismatch repair (MMR) and the repair of the chemosensitive DNA lesion, O6-methylguanine (O6-MeG), by O6-methylguanine-DNA-methyltransferase (E.C. 2.1.1.63, MGMT). Tumor response is also dependent on wild-type p53. Novel 3-(2-anilinoethyl)-substituted imidazotetrazines are reported that have activity independent of MGMT, MMR, and p53. This is achieved through a switch of mechanism so that bioactivity derives from imidazotetrazine-generated arylaziridinium ions that principally modify guanine-N7 sites on DNA. Mono- and bifunctional analogues are reported, and a quantitative structure-activity relationship (QSAR) study identified the p-tolyl-substituted bifunctional congener as optimized for potency, MGMT-independence, and MMR-independence. NCI60 data show the tumor cell response is distinct from other imidazotetrazines and DNA-guanine-N7 active agents such as nitrogen mustards and cisplatin. The new imidazotetrazine compounds are promising agents for further development, and their improved in vitro activity validates the principles on which they were designed.
Solvent free synthesis of some substituted 1,2,4-triazoles using zeolite nay as a reusable solid support and catalyst
Rawal, Manish K.,Sitha, Diwaker,Ameta, Rakshit,Chittora, Anil K.,Punjabi, Pinki B.
, p. 169 - 170 (2013/09/23)
NaY zeolite has been employed as a solid support and catalyst for the clean and solvent free synthesis of some substituted 1,2,4-triazoles under microwave irradiation. The compounds were characterized on the basis of their elemental analysis and spectral data.
AMINOALYL-IMIDAZOTETRAZINES FOR TREATMENT OF CANCER
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Page/Page column 32, (2009/12/02)
The present invention relates to imidazotetrazines of Formula (I) and their use in the treatment of cancer.
Synthesis of some 1,2,4-triazoles as potential antifungal agents
Siddiqui, Anees A.,Arora, Amit,Siddiqui,Misra, Amit
, p. 838 - 841 (2007/10/03)
Some new 3-(p-substituted anilinoethyl)-4-(p-substituted phenyl)-5-thioxo-1,2,4-triazoles 3a-p are synthesized and evaluated for antifungal activity against Candida albicans and Aspergillus niger.
