New Emivirine (MKC-442) Analogues Containing a Tetrahydronaphthalene at C-6 and Their anti-HIV Activity. -Synthesis and testing of the inhibitory activity concerning the HIV-1 replication are given. Only the emivirine analogues (VII) show moderate activity against wild-type HIV-1 and against the Y181C mutant whereas (XV) is devoid of activity against HIV. -(THERKELSEN, F.; JOERGENSEN, P. T.; NIELSEN, C.; PEDERSEN*, E. B.; Monatsh. Chem. 138 (2007) 5, 495-503; Dep. Chem., Univ. South. Den., DK-5230 Odense, Den.; Eng.) -H. Haber 35-196
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Synthesis of New MKC-442 Analogues Containing Alkenyl Chains orReactive Functionalities at C-5.-In an effort to obtain more insight into the interaction between HIV-1 reverse transcriptase (RT) and MKC-442 analogues, a series of new compounds is synthesized and evaluated for inhibition of HIV-1 replication. The modifications include bulky alkenyl substituents at the C-5 position of the uracil ring like in (III) or in the corresponding N-alkylated derivatives (V), (IX), and (XI). Uracils, e.g. (VI) and (XII) with reactive epoxy and aldehyde functionalities at C-5 are also synthesized. Antiviral activity and cytotoxicities of the new substances are tested. -(PETERSEN, LENE; HANSEN, THOMAS H.; KHALIFA, NAGY M.; JOERGENSEN, PER T.; PEDERSEN, ERIK B.; NIELSEN, CLAUS; Monatsh. Chem. 133 (2002) 7, 1031-1043; Dep. Chem., Univ. South. Den., DK-5230 Odense, Den.; EN)
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Synthesis. -Optimized syntheses of 4-isothiocyanatomethylpyridine (IX) and title ester (VI), side product in the original synthesis of (IX), are developed. Both compounds appear to be appropriate precursors for the preparation of thiourea derivative (VIII). -(SARHAN*, A. E.; JOERGENSEN, P. T.; PEDERSEN, E. B.; Synth. Commun. 35 (2005) 18, 2475-2480; Dep. Med.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.