New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase

Bellarosa, Daniela; Antonelli, Guido; Bambacioni, Federica; Giannotti, Danilo; Viti, Giovanni; Nannicini, Rossano; Giachetti, Antonio; Dianzani, F.; Witvrouw, Myriam; Pauwels, Rudi; Desmyter, Jan; Clercq, Erik De

doi:10.1016/0166-3542(95)00906-x

Cited by 27 publications

(14 citation statements)

References 46 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The title compound may be used as a precursor for obtaining bioactive molecules with antitumor activity, see: Bellarosa et al (1996). For the biological activity of benzofuropyrimidine derivatives, see: Moneam et al (2004); Bodke & Sangapure (2003).…”

Section: Related Literaturementioning

confidence: 99%

3,3′-(1,4-Phenylene)bis[2-(propylamino)benzofuro[3,2-d]pyrimidin-4(3H)-one] ethanol disolvate

Gong

et al. 2012

Acta Cryst E

View full text Add to dashboard Cite

The title compound, C32H28N6O4·2C2H5OH, consists of two 2-(propylamino)benzofuro[3,2-d]pyrimidin-4(3H)-one units connected, via one of the pyrimidine N atoms, to a bridging benzene ring in the 1,4 positions. Two ethanol solvent molecules are also present. The main molecule lies on a center of symmetry located at the center of the benzene ring. The fused-ring system of the benzofuro[3,2-d]pyrimidine moiety is nearly planar (r.m.s. deviation = 0.016 Å) and forms a dihedral angle of 78.21 (7)° with the central benzene ring. The crystal structure features O—H⋯O and N—H⋯O interactions. The C atoms of the propylamino side chain in the main molecule and the ethyl group in the solvent molecule are disordered over two positions, with site-occupancy factors 0.34:0.66 and 0.42:0.58, respectively.

show abstract

Section: Related Literaturementioning

confidence: 99%

3,3′-(1,4-Phenylene)bis[2-(propylamino)benzofuro[3,2-d]pyrimidin-4(3H)-one] ethanol disolvate

Gong

et al. 2012

Acta Cryst E

View full text Add to dashboard Cite

show abstract

“…The title compound may be used as a precursor for obtaining bioactive molecules, see: Bellarosa et al (1996). For the biological activity of benzofuropyrimidine derivatives, see: Moneam et al (2004); Bodke et al (2003); Palacios et al (2007); Duval et al (2005); Teimouria et al (2006).…”

Section: Related Literaturementioning

confidence: 99%

Ethyl (2,5-dioxo-1-phenyl-2,3-dihydro-1H,5H-1-benzofuro[3,2-d]imidazo[1,2-a]pyrimidin-3-yl)acetate

Deng¹,

Cao²,

Cai³

et al. 2010

Acta Cryst E

View full text Add to dashboard Cite

In the title compound, C22H17N3O5, synthesized via the aza-Wittig reaction of ethyl 3-(phenyliminomethyleneamino)benzofuran-2-carboxylate, benzene isocyanate and diethyl 2-aminosuccinate, the imidazo[1,2-a]benzo[4,5]furo[2,3-d]pyrimidine ring system is essentially planar (r.m.s. deviation for all 16 non-H atoms = 0.020 Å). The phenyl ring is twisted with respect to this ring system, making a dihedral angle of 54.23 (4)°. The crystal packing is stabilized by weak intermolecular C—H⋯O interactions.

show abstract

“…Nevirapine (116), a dipyrido-1,4-diazepine compound (Fig. Bellorosa et al reported on arylpyridodiazepine (117) and it was found to inhibit human immunodeficiency virus type I [HIV-1(IIIB)] replication at a concentration of 0.003-0.04 M without being cytotoxic at a 3,000-15,000 fold higher concentration [159]. Bellorosa et al reported on arylpyridodiazepine (117) and it was found to inhibit human immunodeficiency virus type I [HIV-1(IIIB)] replication at a concentration of 0.003-0.04 M without being cytotoxic at a 3,000-15,000 fold higher concentration [159].…”

Section: Non-nucleoside Reverse Transcriptase Inhibitors (Nnrtis) Conmentioning

confidence: 99%

Current Scenario of 1,4-Diazepines as Potent Biomolecules-A Mini Review

Ramajayam¹,

Girdhar²,

Yadav

2007

MRMC

View full text Add to dashboard Cite

show abstract

New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase

Cited by 27 publications

References 46 publications

3,3′-(1,4-Phenylene)bis[2-(propylamino)benzofuro[3,2-d]pyrimidin-4(3H)-one] ethanol disolvate

3,3′-(1,4-Phenylene)bis[2-(propylamino)benzofuro[3,2-d]pyrimidin-4(3H)-one] ethanol disolvate

Ethyl (2,5-dioxo-1-phenyl-2,3-dihydro-1H,5H-1-benzofuro[3,2-d]imidazo[1,2-a]pyrimidin-3-yl)acetate

Current Scenario of 1,4-Diazepines as Potent Biomolecules-A Mini Review

Contact Info

Product

Resources

About