59399-36-9Relevant academic research and scientific papers
The synthesis, characterization and catalytic application of manganese porphyrins bonded to novel modified SBA-15
Rayati, Saeed,Nafarieh, Parinaz,Amini, Mostafa M.
, p. 6464 - 6471 (2018/04/23)
In the presented research, a highly ordered mesoporous silica material (SBA-15) was functionalized with imidazole as a functionalizing reagent (SBA-TMSIm) and then characterized via FT-IR spectroscopy, thermogravimetric analysis (TGA), powder X-ray diffra
Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction
Serrao, Erik,Xu, Zhong-Liang,Debnath, Bikash,Christ, Frauke,Debyser, Zeger,Long, Ya-Qiu,Neamati, Nouri
, p. 5963 - 5972 (2013/09/23)
Though much progress has been made in the inhibition of HIV-1 integrase catalysis, clinical resistance mutations have limited the promise of long-term drug prescription. Consequently, allosteric inhibition of integrase activity has emerged as a promising approach to antiretroviral discovery and development. Specifically, inhibitors of the interaction between HIV-1 integrase and cellular cofactor LEDGF/p75 have been validated to diminish proviral integration in cells and deliver a potent reduction in viral replicative capacity. Here, we have contributed to the development of novel allosteric integrase inhibitors with a high-throughput AlphaScreen-based random screening approach, with which we have identified novel 5-carbonyl-1H-imidazole-4-carboxamides capable of inhibiting the HIV-1 integrase-LEDGF/p75 interaction in vitro. Following a structure-activity relationship analysis of the initial 1H-imidazole-4,5- dicarbonyl core, we optimized the compound's structure through an industrial database search, and we went further to synthesize a selective and non-cytotoxic panel of inhibitors with enhanced potency.
Ring-expanded ("fat") nucleoside and nucleotide analogues exhibit potent in vitro activity against Flaviviridae NTPases/helicases, including those of the West Nile virus, hepatitis C virus, and Japanese encephalitis virus
Zhang, Ning,Chen, Huan-Ming,Koch, Verena,Schmitz, Herbert,Liao, Ching-Len,Bretner, Maria,Bhadti, Vishweshwar S.,Fattom, Ali I.,Naso, Robert B.,Hosmane, Ramachandra S.,Borowski, Peter
, p. 4149 - 4164 (2007/10/03)
A series of ring-expanded ("fat") heterocycles, nucleoside and nucleotide analogues (RENs) containing the imidazo[4,5-e][1,3]diazepine ring system (9, 14, 15, 18, 24-26, 28, 31, and 33) and imidazo[4,5-e][1,2,4]triazepine ring systems (30b, 30c, 32, and 3
Ring-expanded nucleosides and nucleotides
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Example 2, (2008/06/13)
The present invention relates to compositions comprising analogues of purine nucleotides containing a ring-expanded ("fat") heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS) and hepatitis.
