Base Information
- Chemical Name:1-(4-Cyanophenyl)guanidine nitrate
- CAS No.:5637-41-2
- Molecular Formula:C8H8N4.HNO3
- Molecular Weight:223.19
- Hs Code.:
- Mol file:5637-41-2.mol
Synonyms:
Synonyms:
98%min *data from raw suppliers
1-(4-Cyanophenyl)guanidine nitrate >95% *data from reagent suppliers
The research focuses on the development of novel nonnucleoside reverse transcriptase inhibitors (NNRTIs) that combine the structural features of diarylpyrimidines (DAPYs) and dihydro-alkoxy-benzyl-oxopyrimidines (DABOs) to create DAPY-DABO hybrids. These hybrids were designed to exhibit potent anti-HIV-1 activity at the (sub)nanomolar level. The study involved the synthesis of four series of compounds (1-4) characterized by the para-cyanoaniline group typical of DAPYs and the 2,6-difluorobenzyl group of DABOs, with variations at the C-4 pyrimidine ring position. The compounds were tested for cytotoxicity and their ability to inhibit HIV-induced cytopathic effect in MT-4 cells, as well as against clinically relevant HIV-1 mutant strains. 1-(4-cyanophenyl)guanidine nitrate was used in the condensation reaction with β-oxoesters to form 2-(4-cyanoanilino)-pyrimidin-4(3H)ones (1a–d). The experiments utilized the MTT method to assess viable cell numbers and recombinant WT HIV-1 RT to evaluate enzyme inhibition. The analyses included determining the effective concentration (EC50), cytotoxic concentration (CC50), and selectivity index (SI) for each compound, as well as inhibitory dose (ID50) against HIV-1 reverse transcriptase and its mutants. The results indicated that compounds with a free amino group at the C-4 position of the pyrimidine ring and double methyl substitution at the C-5/C-6 benzylic positions showed the highest inhibitory activity, with compounds 2d and 4d selected as lead candidates for further optimization due to their (sub)nanomolar inhibitory potency against both wild-type and mutant HIV-1 strains.
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