1,721,089 research outputs found
Indolyl aryl Sulfones (IASs): Development of highly potent NNRTIs active against wt-HIV-1 and clinically relevant drug resistant mutants
No full textIndolyl aryl sulfones (IASs) are a potent class of NNRTIs developed from L-737,126, a lead agent discovered by Merck AG. IAS derivatives are endowed with inhibitory activities against wt HIV-1 in the low nanomolar concentration range. Introduction of two methyl groups at positions 3 and 5 of the phenyl ring of the aryl sulfonyl moiety furnished IAS derivatives such as 5-chloro- or 5-bromo-3-[(3,5-dimethylphenyl)sulfonyl]indole-2-carboxyamide, which showed very potent and selective anti-HIV-1 activity against some mutants carrying NNRTI resistant mutations at positions 103 and 181 of the reverse transcriptase. IAS derivatives bearing 2-hydroxyethylcarboxyamide or 2- hydroxyethylcarboxyhydrazide groups at position 2 of the indole nucleus were more active than L-737,126 against the K103N-Y181C double mutant. A great improvement of antiviral activity against wt HIV-1 and resistant mutants was obtained by coupling 1-3 simple amino acids, such as glycine and alanine, in sequence, with the 3-[(3,5- dimethylphenyl)sulfonyl]-1H-indole-2-carbonyl moiety. The transformation of the chain terminus into amide or hydrazide, produced short peptides with high selectivity and potent activity against wt HIV-1, and the viral mutants Y181C, K103N-Y181C and EFVR. IAS having two halogen atoms at the indole showed potent inhibitory activity against the Y181C and the EFVR resistant mutant strains. In particular, the introduction of a fluorine atom at position 4 of the indole ring notably contributed to improve the antiviral activities against both wt and the related resistant mutants. 5- Nitro-IASs were highly active against wt HIV-1 and exhibited low cytotoxicity. Experimental data highlighted the class IAS derivatives as promising candidates for clinical trials
THE USE OF COPPER-(II) BROMIDE AND N-BROMOSUCCINIMIDE IN THE BROMINATION OF 1-(1-METHYL-1H-PYRROL-2-YL)-2-PHENYLETHANONE
No full text(chlorothienyl)[(dihydrooxazolyl)phenoxy]butanone or [(carboxyphenoxy)oxopentyl]methyl-1H-pyrrolecarboxaldehyde and analogs, methods for their preparation and their use for the inhibition of rhinovirus infections
No full textCompds. for the treatment of rhinovirus infections are claimed.; such compds. are e.g. 1-(2-chloro-5-thienyl)-4-[4-(4,5-dihydro-2-oxazolyl)phenoxy]-1-butanone (I) or 4-[5-[4-(carboxyphenoxy)]-1-oxopentyl]-1-methyl-1H-pyrrole-2-carboxaldehyde (II). Condensation of 2-chloro-5-(5-chloropentanoyl)thiophene with 2-(4-hydroxyphenyl)-4,5-dihydrooxazole gave I (97% yield). I inhibited HRV-14 selectively. [on SciFinder(R)
Preparation of substituted 6-benzyl-4-oxopyrimidines for prevention and treatment of HIV infection
No full textThe invention concerns novel substituted 6-benzyl-4-oxopyrimidines of general formula (A). These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV) or pharmaceutically acceptable salts thereof, and find their application in the prevention and treatment of HIV infection and the treatment of the resulting acquired immune deficiency syndrome (AIDS). Pharmaceutical compositions containing the compounds and a method of use of the present compounds and other agents for the treatment of AIDS and viral infection by HIV are also envisaged
Synthetic approaches to difluoroindolecarboxylic acid ethyl esters.
No full textSynthetic approaches to ethyl 4,5-difluoroindole-2-carboxylate and ethyl 5,6-difluoroindole-2-carboxylate by Fischer indole synthesis and by the reaction of lithiated N-BOC-3,4-difluoro-2-methylaniline with diethyl oxalate or ethyl bromopyruvate were investigated. A simple and direct preparation of ethyl 4,5-difluoroindole-3-carboxylate from lithiated N-BOC-3,4-difluoroaniline and ethyl bromopyruvate was found
Preparation of 6-benzyl-4-oxopyrimidines as antiviral agents
No full textSubstituted 6-benzyl-4-oxopyrimidines having formula (I) are described, wherein: X is selected from the group consisting of O and S; R is selected from the group consisting of C1-4 alkyl and C5-6 cycloalkyl; R', R" and Z, equal or different among them mean H or C1-4 alkyl considering that, when X = O, R and R' cannot be both equal to H; their pharmaceutically acceptable salts and their soluble derivatives; one of their preparation processes and their use for the preparation of pharmaceutical compositions useful for the treatment of viral infections
Research on antibacterial and antifungal agents. 16. Synthesis and antifungal activities of 1-[α-(1-naphthyl)benzyl]imidazole derivatives and related 2-naphthyl isomers
No full textSome 1-arylmethylimidazoles bearing a naphthyl group at the α position of benzyl moiety have been synthesized and tested as antifungal agents against Candida albicans and Candida spp. Such derivatives resemble bifonazole and naftifine, two important antimycotic agents of clinical use. Various compounds were found highly active when tested against Candida strains in comparison with bifonazole, miconazole, clotrimazole and ketoconazole
Antimycobacterial Pyrroles: Synthesis, Anti-Mycobacterium tuberculosis Activity and QSAR Studies.
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