Additions and Corrections - Structure-Activity Relationship Studies with Symmetric Naphthalenesulfonic Acid Derivatives. Synthesis and Influence of Spacer and Naphthalenesulfonic Acid Moiety on Anti-HIV-1 Activity.

1993 ◽  
Vol 36 (25) ◽  
pp. 4130-4130 ◽  
Author(s):  
Prem Mohan ◽  
Man Fai Wong ◽  
Sandeep Verma ◽  
Peggy Huang ◽  
Anura Wickramasinghe ◽  
...  
1996 ◽  
Vol 31 (1-2) ◽  
pp. 87-94 ◽  
Author(s):  
Katsushi Ijichi ◽  
Masatoshi Fujiwara ◽  
Hideki Nagano ◽  
Yukiharu Matsumoto ◽  
Yasuaki Hanasaki ◽  
...  

2000 ◽  
Vol 11 (2) ◽  
pp. 117-133 ◽  
Author(s):  
Roberta Costi ◽  
Roberto Di Santo ◽  
Marino Artico ◽  
Silvio Massa ◽  
Antonio Lavecchia ◽  
...  

Using 2,6-dichloro-4-aminopyrimidine, a number of uracil and cytosine derivatives with both arylthio and alkoxy moieties were prepared. These novel pyrimidines share chemical similarities with DABOs and HEPTs, two classes of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors (NNRTIs), which have been widely studied of late. All new derivatives were tested in MT-4 cells to explore their potential in vivo anti-HIV activity. Like other NNRTIs, they selectively inhibit HIV-1 but not HIV- 2. The majority of test derivatives were found to have low potency and were sometimes more cytotoxic than zidovudine and emivirine (formerly MKC-442), used here as reference drugs. Uracil and cytosine derivatives bearing a sec-butoxy chain and a methyl-substituted benzenesulphonyl moiety were the most potent. Enzyme assays proved that these derivatives target RT. Structure-activity relationship studies established a correlation between the anti-HIV-1 activity and the meta substitution on the phenyl ring; furthermore, oxidation of sulphide to sulphone significantly increased the potency of certain derivatives.


RSC Advances ◽  
2016 ◽  
Vol 6 (97) ◽  
pp. 95177-95188 ◽  
Author(s):  
Tazeem Tazeem ◽  
Xin Han ◽  
Qingjun Zhou ◽  
Jingchen Wei ◽  
Po Tien ◽  
...  

A series of adamantine substituted imidazo[1,2-a]pyridine derivatives were developed through a one-pot multi-component Groebke–Blackburn–Bienaymé reaction, among them several compounds were identified to be the potent inhibitors against HIV-1 cells.


2001 ◽  
Vol 12 (1) ◽  
pp. 37-50 ◽  
Author(s):  
Gianluca Sbardella ◽  
Antonello Mai ◽  
Marino Artico ◽  
Paola Chimenti ◽  
Silvio Massa ◽  
...  

MedChemComm ◽  
2013 ◽  
Vol 4 (1) ◽  
pp. 252-259 ◽  
Author(s):  
Ronen Gabizon ◽  
Ofrah Faust ◽  
Hadar Benyamini ◽  
Sivan Nir ◽  
Abraham Loyter ◽  
...  

We used peptide arrays to perform structure–activity relationship studies on anti-HIV peptides derived from HIV-1 integrase.


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