Efficient synthesis and utilization of phenyl-substituted heteroaromatic carboxylic acids as aryl diketo acid isosteres in the design of novel HIV-1 integrase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 16, 2008, Pages 4521-4524

  Zeng, Li Fan ^a   Zhang, Hu Shan ^a   Wang, Yun Hua ^b   Sanchez, Tino ^c   Zheng, Yong Tang ^b   Neamati, Nouri ^c   Long, Ya Qiu ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b KUNMING INSTITUTE OF ZOOLOGY   (China)

^c UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

Author keywords

1H Pyrazole; Antiviral effect; Bioavailability; Bioisostere; Heteroaromatic carboxylic acid; HIV 1 integrase inhibitor; Isothiazole; Isoxazole

Indexed keywords

1 [5 (4 FLUOROBENZYL) 2 FURYL] 3 (1,2,4 TRIAZOL 3 YL) 1,3 PROPANEDIONE; 3 [3 (BENZYLOXY)PHENYL]ISOXAZOLE 5 CARBOXYLIC ACID; 5 (4 NITROPHENYL) 1H PYRAZOLE 3 CARBOXYLIC ACID; 5 [3 (BENZYLOXY)PHENYL] N HYDROXYISOXAZOLE 3 CARBOXAMIDE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; BENZALDEHYDE; ELVITEGRAVIR; ESTER DERIVATIVE; INTEGRASE; ISOTHIAZOLE DERIVATIVE; ISOXAZOLE; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; PYRAZOLE DERIVATIVE; RALTEGRAVIR; UNCLASSIFIED DRUG;

AMIDATION; ANTIVIRAL ACTIVITY; ARTICLE; CYCLOADDITION; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; PHYSICAL CHEMISTRY; SUBSTITUTION REACTION;

AMINO ACID MOTIFS; ANTI-HIV AGENTS; BIOLOGICAL AVAILABILITY; CARBOXYLIC ACIDS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; HIV INFECTIONS; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; INHIBITORY CONCENTRATION 50; KETO ACIDS; MODELS, CHEMICAL; THIAZOLES;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 48749113136     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.07.047     Document Type: Article

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