Design, synthesis and evaluation of small molecule CD4-mimics as entry inhibitors possessing broad spectrum anti-HIV-1 activity

Bioorganic and Medicinal Chemistry

Volumn 24, Issue 22, 2016, Pages 5988-6003

  Curreli, Francesca ^a   Belov, Dmitry S ^b   Ramesh, Ranjith R ^a   Patel, Naisargi ^a   Altieri, Andrea ^b   Kurkin, Alexander V ^b   Debnath, Asim K ^a  

^a NEW YORK BLOOD CENTER   (United States)

^b MOSCOW STATE UNIVERSITY   (Russian Federation)

Author keywords

Broad spectrum; ENV pseudovirus; HIV 1; Structure activity relationship; Virus entry antagonist

Indexed keywords

5 (3 FLUORO 4 METHYLPHENYL) N [[5 (2 HYDROXYETHYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (3 FLUORO 4 METHYLPHENYL) N [[5 (3 HYDROXYPROPYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (3 FLUORO 4 METHYLPHENYL) N [[5 (HYDROXYMETHYL) 4 METHYL 1H IMIDAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (3 FLUORO 4 METHYLPHENYL) N [[5 (HYDROXYMETHYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLORO 3 FLUOROPHENYL) N [[5 (2 HYDROXYETHYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLORO 3 FLUOROPHENYL) N [[5 (3 HYDROXYPROPYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLORO 3 FLUOROPHENYL) N [[5 (HYDROXYMETHYL) 4 METHYL 1H IMIDAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLORO 3 FLUOROPHENYL) N [[5 (HYDROXYMETHYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLOROPHENYL) N [[5 (2 HYDROXYETHYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLOROPHENYL) N [[5 (3 HYDROXYPROPYL) 4 METHYLTHIAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; 5 (4 CHLOROPHENYL) N [[5 (HYDROXYMETHYL) 4 METHYL 1H IMIDAZOL 2 YL](PIPERIDIN 2 YL)METHYL] 1H PYRROLE 2 CARBOXAMIDE; CD4 ANTIGEN; HUMAN IMMUNODEFICIENCY VIRUS FUSION INHIBITOR; N [2 AMINO 1 [5 (HYDROXYMETHYL) 4 METHYLTHIAZOL 2 YL]ETHYL] 5 (3 FLUORO 4 METHYLPHENYL) 1H PYRROLE 2 CARBOXAMIDE; N [2 AMINO 1 [5 (HYDROXYMETHYL) 4 METHYLTHIAZOL 2 YL]ETHYL] 5 (4 CHLORO 3 FLUOROPHENYL) 1H PYRROLE 2 CARBOXAMIDE; N [2 AMINO 1 [5 (HYDROXYMETHYL) 4 METHYLTHIAZOL 2 YL]ETHYL] 5 (4 CHLOROPHENYL) 1H PYRROLE 2 CARBOXAMIDE; NBD 11021; UNCLASSIFIED DRUG; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; MOLECULAR LIBRARY; NBD-11021; PYRROLE DERIVATIVE; THIAZOLE DERIVATIVE;

ARTICLE; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IC50; NONHUMAN; STRUCTURE ACTIVITY RELATION; VIRUS CELL INTERACTION; VIRUS INFECTIVITY; CELL LINE; CELL SURVIVAL; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; METABOLISM; MICROBIAL SENSITIVITY TEST; MOLECULAR LIBRARY; PHARMACOLOGY; SYNTHESIS;

ANTI-HIV AGENTS; CELL LINE; CELL SURVIVAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HIV-1; HUMANS; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; PYRROLES; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

EID: 84992203479     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2016.09.057     Document Type: Article

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