HIV-1 integrase inhibitors

Satoh M, Motomura T, Matsuda T, Kondo K, Ando K, Matsuda K, Miyake S, Uehara H (2005) 4-Oxoquinohne compounds and utilization thereof as HIV integrase inhibitors, PCT Int, Appl, WO 2005113508... 

HIV Integrase Inhibitor Raitegravir Table 6.2 Optimization of stereoselective amidoxime addition to DMAD. 

HIV Integrase Inhibitor Raltegravir Table 6.3 Direct methylation of hydroxypyrimidinone 3. 

V.M., Reamer, R.A., Stanik, M., Weissman, S., and Wright, T.). Development of a 2nd Generation, Highly Effident Manufacturing Route for the HIV Integrase Inhibitor Rakegravir Potassium , submitted. 

Improving free fraction continues to be a goal in the anti-infective area, particularly in areas where animal efficacy models are not readily available. The importance of adequate free fraction was noted in publications describing a series of HIV integrase inhibitors [52], the HCV protease inhibitor VX-950 [53], a series of cyclosporine derivatives active against HCV [54], and a series of antibacterial MurB inhibitors [55]. 

The investigation of HIV integrase inhibitors has been largely restricted to testing available compounds that inhibit other enzymes with similar substrates or... 

Several compounds and their derivatives that do not contain adjacent hydroxy groups on a phenyl ring have recently been identified as HIV integrase inhibitors. These include suramin (X), curcumin (XI), phenanthroline-Cu+ complexes (XII), and 3 -azido-3 -deoxythymidylate (AZT) monophosphate (XIII). 

In the context of a medical chemistry project, Hazuda and coworkers proved the necessity for large-scale production of an HIV integrase inhibitor in order to be able to carry out several clinical tests [61]. The required precursor presented in Scheme 10 was prepared by a team from Merck in... 

Scheme 10 Microwave-mediated process for the synthesis of an HIV integrase inhibitor precursor...

HIV Integrase Inhibitor Interactions with Active-Site Metal Ions Fact or Fiction ... 

In the third paper [53], a new structural class of noncatechol-containing integrase inhibitors, bisaroylhydrazines, was identified by modification of hits obtained in the previously presented studies. These compounds may provide valuable avenues for the development of HIV integrase inhibitors. Finally, also natural products, i.e., lichen acids containing depsides and depsidones, and their synthetic derivatives were identified from 3D database search as novel HIV-1 integrase inhibitors with IC50 values below 50 pM [54],... 

Raghavan, K. Boulamwini, J.K. Fesen, M.R. Pommier, Y. Kohn, J.W. Weinstein, J.N. Three Dimensional Quantitative Structure-Activity Relationship (QSAR) of HIV Integrase Inhibitors A Comparative Molecular Field Analysis (CoMFA) Study. J. Med. Chem. 1995, 38, 890-897. 

S/GSK1349S72 In an open study in healthy subjects the HIV integrase inhibitor S/GSK1349572 had no effect on the steady-state pharmacokinetics of tenofovir in 15 healthy subjects [87=]. 

Song I, Min SS, Borland J, Lou Y, Chen S, Patel P, Ishibashi T, Piscitelli SC. The effect of lopinavir/ritonavir and daruna-vir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants. J Clin Pharmacol 2011 51(2) 237 2. 

Temesgen Z, Siraj DS. Raltegravir first in class HIV integrase inhibitor. Ther Clin Risk Manag 2008 4 493-500. 

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