Bioorganic and medicinal chemistry letters p. 6611 - 6615,5 (2012)
Update date:2022-09-26
Topics:
Keche, Ashish P.
Hatnapure, Girish D.
Kamble, Vandana M.
Tale, Rajesh H.
Rodge, Atish H.
A series of novel 1-acetyl-3-(3,4-dimethoxypheny)-5-(4-(3-(arylureido/ arylthioureido/arylsulfonamido) phenyl)-4,5-dihydropyrazole derivatives of biological interest have been prepared by sequential cyclization of 1-(4-nitrophenyl)-3-(3,4-dimethoxyphenyl)-pro-2-ene-1 with hydrazine hydrate, reduction followed by reaction of resulting amine with different arylisocyanates or arylisothiocyanates or arylsulfonyl chlorides. All the synthesized compounds (1-32) have been screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological evaluation study showed, the compounds 4, 5, 9, 11, 14 and 16 found to have promising anti-inflammatory activity (up to 61-85% TNF-α and 76-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (76% TNF-α and 86% IL-6 inhibitory activity at 1 μM). Compounds 24, 26, 27, 28 and 29 exhibited promising antimicrobial activity at MIC values ranging from 70 to 10 μg/mL against all the selected pathogenic bacteria and fungi.
View MoreQida Chemical Co., Ltd.(expird)
Contact:+86-25-8776 0031
Address:3-2001 Jiaye Int'l Town, 158 Lushan Road,Nanjing, 210019, China
ShanDong XinDa Chemical CO.,LTD(expird)
Contact:086-0311-87580543
Address:No.168, High Technology Development Zone Jinan Shandong China
Golden Union Agrochemical Import and Export Co., Ltd.
Contact:86-755-23910527
Address:Room 1106, Tower 3A, Excellence Century Center, Futian District, Shenzhen, China
Wuhan Kemi-Works Chemical Co., Ltd
website:http://www.kemiworks.com
Contact:86-27-85736489
Address:Rm. 1503, No. 164, Jianghan North Rd., Wuhan, 430022 China
Hubei Lingsheng Pharmaceuticals Co., Ltd.
Contact:+86-0710-3538058
Address:Xiangyang City Xiangcheng Economic Development Zone, Hubei Province
Doi:10.1002/hlca.19910740804
(1991)Doi:10.1016/j.cattod.2012.03.039
(2012)Doi:10.1021/acs.joc.0c02869
(2021)Doi:10.1016/j.molstruc.2012.07.054
(2013)Doi:10.1248/cpb.c12-00292
(2012)Doi:10.1039/c2cc36839k
(2013)