Literature DB >> 11720852

Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.

D Kim1, L Wang, C G Caldwell, P Chen, P E Finke, B Oates, M MacCoss, S G Mills, L Malkowitz, S L Gould, J A DeMartino, M S Springer, D Hazuda, M Miller, J Kessler, R Danzeisen, G Carver, A Carella, K Holmes, J Lineberger, W A Schleif, E A Emini.   

Abstract

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 analogues. The synthesis, SAR, and biological profiles of this class of antagonists are described.

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Year:  2001        PMID: 11720852     DOI: 10.1016/s0960-894x(01)00655-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Intramolecular arylation of benzimidazoles via Pd(II)/Cu(I) catalyzed cross-dehydrogenative coupling.

Authors:  Kyle C Pereira; Ashley L Porter; Brenton Deboef
Journal:  Tetrahedron Lett       Date:  2014-03-05       Impact factor: 2.415

2.  Facile syntheses of novel benzo-1,3-dioxolo-, benzothiazolo-, pyrido-, and quinolino-fused 5H-benzo[d]-pyrazolo[5,1-b][1,3]-oxazines and 1H-pyrazoles.

Authors:  Belem Avila; Danielle M Solano; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2011-02-04       Impact factor: 6.005

3.  Davis-Beirut Reaction: A Photochemical Brønsted Acid Catalyzed Route to N-Aryl 2H-Indazoles.

Authors:  Niklas Kraemer; Clarabella J Li; Jie S Zhu; Julio M Larach; Ka Yi Tsui; Dean J Tantillo; Makhluf J Haddadin; Mark J Kurth
Journal:  Org Lett       Date:  2019-07-24       Impact factor: 6.005

4.  3D-QSAR studies of substituted 1-(3, 3-diphenylpropyl)-piperidinyl amides and ureas as CCR5 receptor antagonists.

Authors:  Yogesh D Aher; Avantika Agrawal; Prasad V Bharatam; Prabha Garg
Journal:  J Mol Model       Date:  2007-02-16       Impact factor: 1.810

5.  Discovery of Novel CCR5 Ligands as Anticolorectal Cancer Agents by Sequential Virtual Screening.

Authors:  Mariam A El-Zohairy; Darius P Zlotos; Martin R Berger; Hassan H Adwan; Yasmine M Mandour
Journal:  ACS Omega       Date:  2021-04-16

6.  Synthesis and in vitro activity of platinum(II) complexes of two fluorenylspirohydantoins against a human tumour cell line.

Authors:  Petja Marinova; Marin Marinov; Maria Kazakova; Yana Feodorova; Plamen Penchev; Victoria Sarafian; Neyko Stoyanov
Journal:  Biotechnol Biotechnol Equip       Date:  2014-07-10       Impact factor: 1.632

  6 in total

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