Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2′ groups

Synthesis of2H‐benzo[g]furo/thieno/pyrrolo[2,3‐e]indazolesviaIntramolecular Dehydrogenation Photocyclization

“…Indazole derivatives have been recognized as important pharmacophores in the development of antitumor, antimicrobial, anti‐inflammatory and anti‐HIV agents. [ 1‐4 ] The structurally diverse indazole moiety has a variety of biological properties, especially in benzoindazoles. Biological evaluation of those pharmacophores revealed that benzoindazoles was an effective CK2 inhibitors.…”

2-Allyl-7-nitro-2H-indazole

“…Data collection: APEX2 (Bruker, 2009); cell refinement: SAINT (Bruker, 2009); data reduction: SAINT; program(s) used to solve structure: SHELXS97 (Sheldrick, 2008); program(s) used to refine structure: SHELXL97 (Sheldrick, 2008); molecular graphics: ORTEP-3 for Windows (Farrugia, 2012); software used to prepare material for publication: PLATON (Spek, 2009) and publCIF (Westrip, 2010). The indazole subunit in organic molecules is an important structure in many drug substances with a wide range of pharmacological effects: e.g., anti-tumor, anti-microbial, anti-platelet, anti-HIV, and anti-inflammatory (Baraldi et al, 2001;Li et al, 2003;Lee et al, 2001;Rodgers et al, 1996;Schmidt et al, 2008). The present work is a continuation of the investigation of the indazole derivatives published recently by our team (El Brahmi et al, 2012;Chicha et al, 2013).…”

Citric acid Mediated One-pot Regioselective Synthesis of N-Alkylated Indazoles: An Efficient Green Strategy

“…Heterocyclic ring systems are frequently found in numerous naturally occurring compounds and they compose the core structures of many biologically active motifs as well as some industrial compounds [1]. Among them, indazoles represent an important class of nitrogen containing heterocycles and this nucleus (Figure 1) [2,3] is of great current interest as partial structure in many synthetic drugs or drug candidates with a broad range of pharmacological activities including anti-HIV [4], anti-inflammatory [5], anti-tumor [6,7], anti-depressant [8], analgesic and antipyretic [9], anti-leukemia [10], anti-convulsant activity [11], anti-cancer [12], anti-arthritic [13], anthelmintic [14] and anti-diabetes [15]. Indazole moiety is present only in three natural products such as Nigellicine, Nigeglanine and Nigellidine indicates their rare presence in nature [16,17].…”