Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

“…19 The identical LDHA potency values of 4 and 5 presented an opportunity to further explore the 6-position SAR of the dihydropyrone core. The initial dihydropyrone analogs were synthesized using a previously described route 20 in which a benzaldehyde (13) was reacted with…”

In search of therapeutic candidates for HIV/AIDS: rational approaches, design strategies, structure–activity relationship and mechanistic insights

“…[105][106][107] Some natural quinolines such as, g-fagarine 108 and haplopine 109 were extracted from the roots and barks of the Zanthoxylum ailanthoides plant and found to exert their anti-HIV actions through the inhibition of HIV replication. 108 Various quinoline derivatives (110)(111)(112)(113)(114)(115)(116) have been synthesized with amide and styryl linkers and evaluated for inhibition of HIV-1 together with the positive control azidothymidine (AZT), as depicted in Fig. 13.…”

Modification and biological evaluation of novel 4-hydroxy-pyrone derivatives as non-peptidic HIV-1 protease inhibitors

“…As a result, compound 1 (Fig. 1) was identified to be a potent HIV PR inhibitor with a very low IC 50 value of 1.1 nM (Vara Prasad et al, 1999). But it showed poor antiviral activity (EC 50 = 15 lM).…”

“…Different research groups have synthesized series of 4-hydroxy-pyran-2-one derivatives as HIV-1 PR inhibitors (Romines and Chrusciel, 1995;Vara Prasad et al, 1999;Tummino et al, 1996;Thaisrivongs et al, 1996;Lunney et al, 1994;Skulnick et al, 1995;Tait et al, 1997;Sun et al, 2005). The pyran-2-one group, 4-hydroxyl group, and substitution at the 3-position were all necessary for the HIV-1 PR inhibitory activity.…”