636992-53-5Relevant academic research and scientific papers
HCV PROTEASE INHIBITORS
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Paragraph 0054; 0055, (2014/06/24)
The present invention discloses a compound of general formula (I); A is O, S, CH, NH or NR', when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C-Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or -Y1-Rm; A1 is NH or CH2; R1' is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalky etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
HCV Protease Inhibitors
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Paragraph 0135-0138, (2014/06/24)
A compound of general formula (I); A is O, S, CH, NH or NR′, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1′ is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
Synthesis and biological evaluation of some novel benzofuranpyridine derivatives
Channamma,Basawaraj, Raga
, p. 183 - 188 (2019/01/21)
5-Bromo-3-amino-2-acetyl benzofuran 3 was prepared by the reaction of 5- bromosalicylonitrile 2 with chloroacetone in dry acetone in presence of anhydrous potassium carbonate to maintain basic condition. The Claisen-Schmidt condensation of compound 3 with various substituted aromatic aldehydes in presence of strong base in absolute ethanol gave 5-bromo-3-amino-2-arylidine acetyl benzofuran 4a-f in good yields. The compounds 4a-f upon treatment with orthophosphoric acid in acetic acid underwent cyclisation and resulted in the formation of above titled compounds 5a-f. All synthesized compounds were characterized on the basis of its physical constant, analytical and spectral studies. Further these compounds were evaluated for their antibacterial and antifungal activities.
Synthesis and antiinflammatory activity of 1H-pyrazolines bearing 5-bromo-3-amino benzofuran
Durgad, Siddanna,Kumbhar, Mahesh,Basawaraj, Raga,Susan Srujana,Barbole, Pruthviraj
, p. 167 - 172 (2013/09/24)
5-Bromo-3-amino-2-acetyl banzofuran 3 was prepared by the interaction of 5-bromosalicylonitrile and chloroacetone in presence of anhyd potassium carbonate in dry acetone. The compound 3 was treated with different substituted aromatic aldehydes in ethanol in presence of strong alkali to give 5-bromo-3-amino-2-arylidene acetylbenzofurans (4a-e). 5-(3-Amino-5- bromobenzofuran)-3-aryl-2-pyrazolines (5ae) were synthesized by the reaction of 5-bromo-3-amino-2-arylidene acetylbenzofurans (4a-e) with hydrazine hydrate. The reaction of compounds (5a-e) with chloroacetyl chloride in presence of triethylamine in dry toluene furnished 5-aryl-3-[5'-bromo-3'-(chloroacetyl)- aminobenzofuran-2-yl]-1H-pyrazolines (6a-e). All synthesized compounds were screened for their antimicrobial activities and some selected benzofuran pyrazoline derivatives were screened for antiinflammatory activities.
Syntheses of 3-acetoacetylaminobenzo[b]furan derivatives having cysteinyl leukotriene 2 receptor antagonistic activity
Ando, Kumiko,Tsuji, Eriko,Ando, Yuko,Kuwata, Noriko,Kunitomo, Jun-Ichi,Yamashita, Masayuki,Ohta, Shunsaku,Kohno, Shigekatsu,Ohishi, Yoshitaka
, p. 625 - 635 (2007/10/03)
Novel 3-acetoacetylaminobenzo[b]furan derivatives having a modified triene system at the 3-position were synthesized starting with 3-aminobenzo[b]furans. The enol isomers, 3-[(3-hydroxybul-2-enonyl)amino]benzo[b]furans (1), of the 3-acetoacetylaminobenzo[b]furans were obtained as stable isomers owing to formation of a hydrogen bonding between the enol hydroxyl group and the amidocarbonyl group. The planarity of the C-2 substituent through the C-3 side chain suggested the existence of a modified conjugational triene system in the enol compound. Cysteinyl leukotriene 1 and 2 receptor antagonistic activities for these compounds were evaluated. 2-(4-Cyanobenzoyl or ethoxycarbonyl)-3-[(2-cyano-3-hydroxybut-2-enonyl)amino]benzo[e]furans (15g, 15o, 15u) were moderately active.
Preparation of 3-acetoacetylaminobenzo[b]furan derivatives with cysteinyl leukotriene receptor 2 antagonistic activity.
Tsuji, Eriko,Ando, Kumiko,Kunitomo, Jun-ichi,Yamashita, Masayuki,Ohta, Shunsaku,Kohno, Shigekatsu,Ohishi, Yoshitaka
, p. 3139 - 3141 (2007/10/03)
Novel 3-acetoacetylaminobenzo[b]furan derivatives with a modified triene system at the 3-position were prepared through acylation of the 3-aminobenzo[b]furans with 5-methylisoxazole-4-carboxylic acid chloride followed by basic cleavage of the isoxazole ring and several of these compounds showed moderate cysteinyl leukotriene receptor 2 antagonistic activity.
