50995-73-8Relevant academic research and scientific papers
Copper mediated one-pot synthesis of quinazolinones and exploration of piperazine linked quinazoline derivatives as anti-mycobacterial agents
Ahmad, Md. Naiyaz,Chopra, Sidharth,Dasgupta, Arunava,Gatadi, Srikanth,Gour, Jitendra,Kaul, Grace,Madhavi, Y. V.,Malasala, Satyaveni,Nanduri, Srinivas,Shukla, Manjulika
, p. 43533 - 43538 (2020/12/25)
A facile method was developed for the synthesis of quinazolinone derivatives in a one-pot condensation reaction via in situ amine generation using ammonia as the amine source and with the formation of four new C-N bonds in good to excellent yields. With the optimised method, we synthesized a library of piperazine linked quinazoline derivatives and the synthesized compounds were evaluated for their inhibitory activity against Mycobacterium tuberculosis. The compounds 8b, 8e, 8f, 8m, 8n and 8v showed potent anti-mycobacterial activity with MIC values of 2-16 μg mL-1. All the synthesized compounds follow Lipinski's rules for drug likeness. This journal is
Computer-aided design, synthesis and validation of 2-phenylquinazolinone fragments as CDK9 inhibitors with anti-HIV-1 tat-mediated transcription activity
Sancineto, Luca,Iraci, Nunzio,Massari, Serena,Attanasio, Vanessa,Corazza, Gianmarco,Barreca, Maria Letizia,Sabatini, Stefano,Manfroni, Giuseppe,Avanzi, Nilla Roberta,Cecchetti, Violetta,Pannecouque, Christophe,Marcello, Alessandro,Tabarrini, Oriana
, p. 1941 - 1953 (2014/01/06)
The activity of the cyclin-dependent kinase 9 (CDK9) is critical for HIV-1 Tat-mediated transcription and represents a promising target for antiviral therapy. Here we present computational studies that, along with preliminary synthetic efforts, allowed us
