- Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors
-
A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus. Our efforts have resulted in a series of benzoic acid analogues that are potent inhibitors of HIV-1 replication against a panel of HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs). Furthermore, the combination of good antiviral potency, a broad spectrum of activity, and an excellent pharmacokinetic profile provides strong justification for the further development of compound 7 as a potential treatment for wild type and NNRT1-resistant HIV-1 infection.
- O'Meara, Jeff A.,Yoakim, Christiane,Bonneau, Pierre R.,B?s, Michael,Cordingley, Michael G.,Déziel, Robert,Doyon, Louise,Duan, Jianmin,Garneau, Michel,Guse, Ingrid,Landry, Serge,Malenfant, Eric,Naud, Julie,Ogilvie, William W.,Thavonekham, Bounkham,Simoneau, Bruno
-
-
Read Online
- Oxime ether derivative and preparation method and application thereof
-
The invention discloses oxime ether derivative and a preparation method and application thereof. The oxime ether derivative is shown as any one of 1) to 6), wherein the 1) is 5-bromine-1-naphthalene formaldehyde oxime ether, the 2) is 5-methoxy-1-naphthalene formaldehyde oxime ether, the 3) is 5-phenyl-1-naphthalene formaldehyde oxime ether, the 4) is 5-p-methoxyphenyl-1-naphthalene formaldehyde oxime ether, the 5) is 5-p-ethoxyphenyl-1-naphthalene formaldehyde oxime ether, and the 6) is 3-5-ethyl(E)-1-naphthalene formaldehyde oxime ether. According to the oxime ether derivative, 1-naphthoic acid is utilized as a raw material; the oxime ether derivative is synthesized by coupling reaction of Suzuki reaction, Heck reaction and the like, acylation reaction and oximation reaction. The compound disclosed by the invention has good antineoplastic activity and has a very good prospect in medicinal development.
- -
-
Paragraph 0075; 0078
(2018/08/03)
-
- DIHYDROIMIDAZOTHIAZOLE DERIVATIVES
-
Compounds of formula (I): or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.
- -
-
Page/Page column 51
(2008/06/13)
-
- Photogeneration of 1,5-naphthoquinone methides via excited-state (formal) intramolecular proton transfer (ESIPT) and photodehydration of 1-naphthol derivatives in aqueous solution
-
The photochemistry of naphthols 1, 2, 4, 5 and 9, and phenol 10 has been studied in aqueous solution with the primary aim of exploring the viability of such compounds for naphthoquinone and quinone methide photogeneration, along the lines already demonstr
- Lukeman, Matthew,Veale, Duane,Wan, Peter,Munasinghe, V. Ranjit N.,Corrie, John E.T.
-
p. 240 - 253
(2007/10/03)
-
- Asymmetric Additions to Chiral Naphthalenes. 4. An Asymmetric Synthesis of the AB-Ring of Aklavinone
-
The chiral 1-naphthyloxazoline (+)-6, prepared from known 1-iodo-5-methoxynaphthalene, was treated with vinyllithium to afford the dihydronaphthalene 8, after quenching and reductive removal of the chiral auxiliary.Introduction of the tertiary hydroxyl gr
- Meyers, A. I.,Higashiyama, Kimio
-
p. 4592 - 4597
(2007/10/02)
-