934417-63-7Relevant academic research and scientific papers
Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis
De Luca, Laura,Ferro, Stefania,Buemi, Maria Rosa,Monforte, Anna-Maria,Gitto, Rosaria,Schirmeister, Tanja,Maes, Louis,Rescifina, Antonio,Micale, Nicola
, p. 1585 - 1596 (2018)
Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence,
Design and synthesis of N1-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors
Monforte, Anna-Maria,Ferro, Stefania,De Luca, Laura,Lo Surdo, Giuseppa,Morreale, Francesca,Pannecouque, Christophe,Balzarini, Jan,Chimirri, Alba
, p. 1459 - 1467 (2014/03/21)
A series of novel N1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies.
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Monforte, Anna-Maria,Logoteta, Patrizia,Luca, Laura De,Iraci, Nunzio,Ferro, Stefania,Maga, Giovanni,De Clercq, Erik,Pannecouque, Christophe,Chimirri, Alba
experimental part, p. 1702 - 1710 (2010/05/02)
A series of novel benzimidazolones and their analogues, characterized by the presence of one or more methyl groups or other bioisosteric moieties at different positions of the phenyl ring at N-1, were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Most of the new compounds proved to be highly effective in inhibiting both HIV-1 replication in MT4 cells with minimal cytotoxicity and RT enzyme at nanomolar concentrations. Some derivatives were also tested against RTs containing single amino acid mutations responsible for resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs). The different potencies displayed by the new compounds were studied using molecular modeling.
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents
Monforte, Anna-Maria,Logoteta, Patrizia,Ferro, Stefania,Luca, Laura De,Iraci, Nunzio,Maga, Giovanni,Clercq, Erik De,Pannecouque, Christophe,Chimirri, Alba
scheme or table, p. 5962 - 5967 (2009/12/24)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have become very important components in the antiretroviral combination therapies used to treat HIV. Recently, our group identified some 1,3-dihydrobenzimidazol-2-one derivatives and their sulfones as a potent and novel class of NNRTIs. We herein report the synthesis and biological evaluation of the new compounds in which different structural modifications have been introduced in order to investigate their effects on RT inhibition.
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors
Monforte, Anna-Maria,Rao, Angela,Logoteta, Patrizia,Ferro, Stefania,De Luca, Laura,Barreca, Maria Letizia,Iraci, Nunzio,Maga, Giovanni,De Clercq, Erik,Pannecouque, Christophe,Chimirri, Alba
, p. 7429 - 7435 (2008/12/23)
Several N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones were synthesized and evaluated as anti-HIV agents. Some of them proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentration as potent non-nucleoside HIV-1 RT
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains
Barreca, Maria Letizia,Rao, Angela,Luca, Laura De,Iraci, Nunzio,Monforte, Anna-Maria,Maga, Giovanni,Clercq, Erik De,Pannecouque, Christophe,Balzarini, Jan,Chimirri, Alba
, p. 1956 - 1960 (2008/02/04)
Molecular modeling studies led to the rational discovery of N1-arylsulfonyl-1,3-dihydro-2H-benzimidazol-2-one as a novel template for the design of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) that are active against wild-type a
