Design of a novel tryptophan-rich membrane-active antimicrobial peptide from the membrane-proximal region of the HIV glycoprotein, gp41

• Evan F. Haney,
• Leonard T. Nguyen,
• David J. Schibli and
• Hans J. Vogel

Beilstein J. Org. Chem. 2012, 8, 1172–1184, doi:10.3762/bjoc.8.130

• that does not possess intrinsic antimicrobial activity. Peptides derived from the envelope HIV-1 glycoproteins, gp120 and gp41, have previously been examined for their antimicrobial activity [10] and we chose to use the membrane-proximal region of gp41 as our starting peptide scaffold. This region of

• has four additional positive charges and is also antimicrobially inactive. The lack of antimicrobial activity may be related to the fact that the gp41w peptide appears to oligomerize in solution. When found in the HIV-1 Env glycoprotein complex, gp41 is known to exist as a trimer [26], and previous

Marilones A–C, phthalides from the sponge-derived fungus Stachylidium sp.

• Celso Almeida,
• Stefan Kehraus,
• Miguel Prudêncio and
• Gabriele M. König

Beilstein J. Org. Chem. 2011, 7, 1636–1642, doi:10.3762/bjoc.7.192

• liver stages as described by Ploemen et al. [24]. Inhibition of the viral HIV-1- and HIV-2-induced cytopathogenic effect in MT-4 cells assays was performed according to Pannecouque et al. [25] and Zhan et al. [26]. Severe Acute Respiratory Syndrome coronavirus (SARS) assays were performed according to

• Phosphorylation & Disease, CNRS, Roscoff, France) for performing the protein kinases assays and Dr. C. Pannecouque (Rega Institute for Medical Research, Leuven, Belgium) for performing the HIV-1 and HIV-2 antiviral assays; we also kindly thank Indra Bergval (KIT Biomedical Research, Royal Tropical Institute

Multicomponent synthesis of artificial nucleases and their RNase and DNase activity

• Anton V. Gulevich,
• Lyudmila S. Koroleva,
• Olga V. Morozova,
• Valentina N. Bakhvalova,
• Vladimir N. Silnikov and
• Valentine G. Nenajdenko

Beilstein J. Org. Chem. 2011, 7, 1135–1140, doi:10.3762/bjoc.7.131

• oligoribonucleotides and an HIV-1 recombinant RNA fragment 96 nucleotides long [17]. Previously, compounds 1 and 2 have been synthesized from the corresponding diamines by condensation with protected natural amino acids and subsequent deprotection [18]. This approach is significantly limited by using available natural

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

Approaches towards the synthesis of 5-aminopyrazoles

• Ranjana Aggarwal,
• Vinod Kumar,
• Rajiv Kumar and
• Shiv P. Singh

Beilstein J. Org. Chem. 2011, 7, 179–197, doi:10.3762/bjoc.7.25

• = SCH3), respectively. These compounds were further treated with nitrous acid and coupled with different secondary amines to yield the triazenopyrazoles 78. Compounds 78 were tested for biological activity against HIV-1 and herpes simplex viruses, and showed moderate activity against HIV-1 virus (Scheme

Dipyridodiazepinone derivatives; synthesis and anti HIV-1 activity

• Nisachon Khunnawutmanotham,
• Nitirat Chimnoi,
• Arunee Thitithanyanont,
• Patchreenart Saparpakorn,
• Kiattawee Choowongkomon,
• Pornpan Pungpo,
• Supa Hannongbua and
• Supanna Techasakul

Beilstein J. Org. Chem. 2009, 5, No. 36, doi:10.3762/bjoc.5.36

• , Ubonratchathani 34190, Thailand 10.3762/bjoc.5.36 Abstract Ten dipyridodiazepinone derivatives were synthesized and evaluated for their anti HIV-1 reverse transcriptase activity against wild-type and mutant type enzymes, K103N and Y181C. Two of them were found to be promising inhibitors for HIV-1 RT. Keywords

• : AIDS; anti HIV-1 RT; dipyridodiazepinone; nevirapine; synthesis; Introduction Dipyridodiazepinone nevirapine (1) [1] (Figure 1) is a potent non-nucleoside inhibitor of human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and is approved as a therapeutic agent for the treatment of AIDS

• ][5][6][7][8]. On the basis of molecular modeling analysis on the wild-type (WT) and Y181C HIV-1 RT, it was found that the dipyridodiazepinone derivatives containing an unsubstituted lactam nitrogen and a 2-chloro-8-arylthiomethyl moiety, when compared with 9 [4] (Figure 2) as reference, are effective

N-1 regioselective Michael- type addition of 5-substituted uracils to (2-hydroxyethyl) acrylate

• Sławomir Boncel,
• Dominika Osyda and
• Krzysztof Z. Walczak

Beilstein J. Org. Chem. 2007, 3, No. 40, doi:10.1186/1860-5397-3-40

• -isopropyl-6-benzyluracyl) are in the third stage of clinical testing for their inhibition of HIV-1 reverse transcriptase.[3] Others, like acyclovir or gancyclovir are in clinical use.[4] Cidofovir, (S)-3-hydroxy-2-phosphonomethoxypropyl cytosine, is an acyclonucleoside that possesses broad-spectrum activity

One-pot synthesis of novel 1H-pyrimido[4,5-c][1,2]diazepines and pyrazolo[3,4-d]pyrimidines

• Dipak Prajapati,
• Partha P. Baruah,
• Baikuntha J. Gogoi and
• Jagir S. Sandhu

Beilstein J. Org. Chem. 2006, 2, No. 5, doi:10.1186/1860-5397-2-5

• -c]pyridazine-5,7-dione), inhibits the growth of Pseudomonas 568 and also binds to herring sperm DNA.[7] However, until the emergence of HEPT[8] as a potent and selective inhibitor of HIV-1, no attention was given to the synthetic manipulation at the 6-position of uracils. Also the synthetic

• compounds of biological importance including anti-tumor antibiotics and inhibitors of HIV-1 transcriptase.[30] New methods continue to appear in the literature describing the synthesis of novel benzodiazepine analogues[31], and emphasis is placed on the alteration and replacement of benzene ring with a