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Titolo:
Designs and syntheses of oxathiin carboxanilide analogues and their antiviral activities
Autore:
Hahn, HC; Rhee, HK; Lee, CK; Whang, KJ;
Indirizzi:
Korea Adv Inst Sci & Technol, Sunkbuk Ku, Seoul, South Korea Korea Adv Inst Sci & Technol Seoul South Korea k Ku, Seoul, South Korea Korea Res Inst Chem Technol, Yusong Ku, Taejon 305343, South Korea Korea Res Inst Chem Technol Taejon South Korea 305343 05343, South Korea Sookmyung Womens Univ, YongsanKu, Seoul, South Korea Sookmyung Womens Univ Seoul South Korea , YongsanKu, Seoul, South Korea
Titolo Testata:
ARCHIVES OF PHARMACAL RESEARCH
fascicolo: 4, volume: 23, anno: 2000,
pagine: 315 - 323
SICI:
0253-6269(200008)23:4<315:DASOOC>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
REVERSE-TRANSCRIPTASE INHIBITORS; DERIVATIVES; INVITRO; REARRANGEMENT; INFECTIVITY; MECHANISMS; POTENT; NNRTIS;
Keywords:
heterocyclic carboxanilide; oxathiins; thiazines; dithiins; thiocarboxanilides; antiviral activities;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Hahn, HC Korea Adv Inst Sci & Technol, Sunkbuk Ku, 39-1 Hawolkok Dong, Seoul, SouthKorea Korea Adv Inst Sci & Technol 39-1 Hawolkok Dong Seoul SouthKorea
Citazione:
H.C. Hahn et al., "Designs and syntheses of oxathiin carboxanilide analogues and their antiviral activities", ARCH PH RES, 23(4), 2000, pp. 315-323

Abstract

Syntheses of new analogues of oxathiin carboxanilide (UC84) and their antiviral activities were described. The heterocyclic carboxylic acids including oxathiins (4), thiazines (9) and dithiins (13) in which the methyl was replaced either by lipophilic trifluoromethyl- or bulky phenyl-group were synthesized starting from beta-keto esters (5). Reaction of 4, 9 and 13 with thionyl chloride followed by treatment of the substituted aniline 22 gave the corresponding carboxanilides (24a similar to 24f). The carboxanilides were subjected to Laweson's reagent the corresponding thiocarboxanilides (24g similar to 24k). The antiviral activities of the synthesized compounds against human immunodeficiency virus type 1 (HIV-1), poliovirus type 1 (PV-1), coxsackie B virus type 3 (CoxB-3), vesicular stomatitis virus (VSV) and herpes simplex virus type 1 (HSV-1) were presented. The antiviral activity against HIV-1 of dithiin carboxanilide (24e) was similar with that of UC84 (24a). The corresponding thiocarboxanilides (24g similar to 24k) showed higherinhibitory activity against HIV-1 than the carboxanilides (24a, 24b, 24d, 24e). The compounds in which ether the lipophilic trifluoromethyl substituents (24d, 24f, 24i, 24k) or bulky phenyl substituent is present in the heterocyclic compounds showed lower inhibitory activity than that of the methylsubstituents is present in the compounds against the HIV-1. But the trifluoromethylated dithiin (24f) showed higher inhibitory activity against PV-1 and CoxB-3 virus than commercial antiviral agents, ribavirin (RV).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/09/20 alle ore 09:00:19