Literature DB >> 9934481

Tricyclic ureas: a new class of HIV-1 protease inhibitors.

W Han1, J C Pelletier, C N Hodge.   

Abstract

A new class of tricyclic ureas containing a conformationally constrained proline was designed with the aid of molecular modeling. Efficient stereoselective intermolecular pinacol coupling represented the highlight of the synthesis. These rigid cyclic ureas are active towards HIV-1 protease, with 9 being the most potent compound (Ki = 9 nM) despite interacting with only three side chain binding pockets of HIV protease.

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Year:  1998        PMID: 9934481     DOI: 10.1016/s0960-894x(98)00659-3

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


  5 in total

1.  Synthesis of fused indazole ring systems and application to nigeglanine hydrobromide.

Authors:  Aaron C Sather; Orion B Berryman; Julius Rebek
Journal:  Org Lett       Date:  2012-03-02       Impact factor: 6.005

2.  Late-stage ortho-C-H alkenylation of 2-arylindazoles in aqueous medium by Manganese(i)-catalysis.

Authors:  Krishna Kanta Das; Asim Kumar Ghosh; Alakananda Hajra
Journal:  RSC Adv       Date:  2022-07-04       Impact factor: 4.036

3.  A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.

Authors:  Khalid Boujdi; Nabil El Brahmi; Jérôme Graton; Didier Dubreuil; Sylvain Collet; Monique Mathé-Allainmat; Mohamed Akssira; Jacques Lebreton; Saïd El Kazzouli
Journal:  RSC Adv       Date:  2021-02-10       Impact factor: 3.361

4.  Metal-free, regioselective, visible light activation of 4CzIPN for the arylation of 2H-indazole derivatives.

Authors:  Rajendhiran Saritha; Sesuraj Babiola Annes; Subburethinam Ramesh
Journal:  RSC Adv       Date:  2021-04-15       Impact factor: 3.361

5.  Oxidative cross-dehydrogenative coupling (CDC) via C(sp2)-H bond functionalization: tert-butyl peroxybenzoate (TBPB)-promoted regioselective direct C-3 acylation/benzoylation of 2H-indazoles with aldehydes/benzyl alcohols/styrenes.

Authors:  Richa Sharma; Lalit Yadav; Ravi Kant Yadav; Sandeep Chaudhary
Journal:  RSC Adv       Date:  2021-04-15       Impact factor: 3.361

  5 in total

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