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D Hazuda

Explore the profile of D Hazuda including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 22
Citations 591
Followers 0
Related Specialties
Biochemistry
Microbiology
Molecular Biology
Top 10 Co-Authors
J Kessler
M Miller
M S Springer
S L Gould
A Carella
E A Emini
K Holmes
W A Schleif
R Danzeisen
G Carver
Published In
Bioorg Med Chem Lett
J Virol
J Biol Chem
Drug Des Discov
Proc Natl Acad Sci U S A
Affiliations
Soon will be listed here.
Recent Articles
1.
Long-acting formulations for the treatment of latent tuberculous infection: opportunities and challenges
Swindells S, Siccardi M, Barrett S, Olsen D, Grobler J, Podany A, et al.
Int J Tuberc Lung Dis . 2018 Mar; 22(2):125-132. PMID: 29506608
Long-acting/extended-release drug formulations have proved very successful in diverse areas of medicine, including contraception, psychiatry and, most recently, human immunodeficiency virus (HIV) disease. Though challenging, application of this technology to...
2.
Combinatorial synthesis of CCR5 antagonists
Willoughby C, Berk S, Rosauer K, Degrado S, Chapman K, Gould S, et al.
Bioorg Med Chem Lett . 2001 Nov; 11(24):3137-41. PMID: 11720860
Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort....
3.
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection
Kim D, Wang L, CALDWELL C, Chen P, Finke P, Oates B, et al.
Bioorg Med Chem Lett . 2001 Nov; 11(24):3103-6. PMID: 11720852
Replacement of the large hydantoin-indole moiety from our previous work with a variety of smaller heterocyclic analogues gave rise to potent CCR5 antagonists having binding affinity comparable to the hydantoin...
4.
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection
Kim D, Wang L, CALDWELL C, Chen P, Finke P, Oates B, et al.
Bioorg Med Chem Lett . 2001 Nov; 11(24):3099-102. PMID: 11720851
A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are...
5.
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity
Hale J, Budhu R, Holson E, Finke P, Oates B, Mills S, et al.
Bioorg Med Chem Lett . 2001 Oct; 11(20):2741-5. PMID: 11591514
Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro.
6.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
Finke P, Oates B, Mills S, MacCoss M, Malkowitz L, Springer M, et al.
Bioorg Med Chem Lett . 2001 Sep; 11(18):2475-9. PMID: 11549450
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50=10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of...
7.
The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I
Singh S, Jayasuriya H, Salituro G, ZINK D, Shafiee A, Heimbuch B, et al.
J Nat Prod . 2001 Jul; 64(7):874-82. PMID: 11473415
From the screening of a microbial extract library, isocomplestatin (1), a new axial-chiral isomer of complestatin (2) which is a known rigid bicyclic hexapeptide, was identified as a potent natural...
8.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes
Finke P, Meurer L, Oates B, Mills S, MacCoss M, Malkowitz L, et al.
Bioorg Med Chem Lett . 2001 Feb; 11(2):265-70. PMID: 11206474
(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement...
9.
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes
Dorn C, Finke P, Oates B, Budhu R, Mills S, MacCoss M, et al.
Bioorg Med Chem Lett . 2001 Feb; 11(2):259-64. PMID: 11206473
Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded (2S)-2-(3,4-dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (4) as a potent lead structure having an IC50 binding affinity of 35 nM. Herein,...
10.
X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform
Chen Z, Yan Y, Munshi S, Li Y, Xu B, Witmer M, et al.
J Mol Biol . 2000 Feb; 296(2):521-33. PMID: 10669606
The crystal structure of simian immunodeficiency virus (SIV) integrase that contains in a single polypeptide the core and the C-terminal deoxyoligonucleotide binding domain has been determined at 3 A resolution...