In Vitro Antiviral Characteristics of HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068
- B. Nowicka-Sans, Y. Gong, M. Krystal
- BiologyAntimicrobial Agents and Chemotherapy
- 30 April 2012
The results suggest that BMS-626529 should be active against the majority of HIV-1 viruses and support the continued clinical development of the compound.
Antimicrobial Evaluation of Nocathiacins, a Thiazole Peptide Class of Antibiotics
- M. Pucci, J. Bronson, Y. Ueda
- BiologyAntimicrobial Agents and Chemotherapy
- 1 October 2004
Nocathiacin-resistant compounds demonstrated potential for further development as a new class of antibacterial agents with activity against key antibiotic-resistant gram-positive bacterial pathogens.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor…
- J. Kadow, Y. Ueda, D. Grasela
- Chemistry, BiologyJournal of Medicinal Chemistry
- 22 February 2012
The data showed that prodrug 4 had excellent potential to significantly reduce dissolution rate-limited absorption following oral dosing in humans, and provided guidance for further efforts to obtain an effective HIV-1 attachment inhibitor.
Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.
The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs) that originated with 1 to deliver temsavir (3, BMS-626529) is described. The most beneficial increases in…
A simple method of preparing trimethylsilyl- and tert-butyldimethylsilyl-enol ethers of α-diazoacetoacetates and their use in the synthesis of a chiral precursor to thienamycin analogs
- Y. Ueda, G. Roberge, V. Vinet
- Chemistry
- 1 December 1984
Les enols ethers du titre (A) sont prepares par action des trifluoromethanesulfonates de trialkylsilyle sur des α-diazoacetylacetates; l'action de l'acetoxy-4 t-butyldimethylsiloxy-1' ethyl-3…
Envelope Conformational Changes Induced by Human Immunodeficiency Virus Type 1 Attachment Inhibitors Prevent CD4 Binding and Downstream Entry Events
Results indicate that obstruction of gp120-sCD4 interactions is the primary inhibition mechanism of this compound and that compound interaction with envelope must precede CD4 binding.
Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors.
- B. N. Naidu, M. Sorenson, M. A. Walker
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 1 February 2015
The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.
- B. N. Naidu, M. A. Walker, N. Meanwell
- ChemistryBioorganic & Medicinal Chemistry Letters
- 1 July 2018
Michael addition of amines and thiols to dehydroalanine amides: a remarkable rate acceleration in water.
- B. N. Naidu, M. Sorenson, T. Connolly, Y. Ueda
- Chemistry, BiologyJournal of Organic Chemistry
- 27 November 2003
In water, the rate of Michael addition of amines and thiols to dehydroalanine amides was greatly accelerated, leading to shorter reaction times and higher yields, providing an attractive route to the synthesis of natural and unnatural amino acid derivatives.
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