共查询到20条相似文献,搜索用时 0 毫秒
1.
2.
3.
4.
Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti‐Inflammatory and Anti‐Proliferative Agents
下载免费PDF全文
![点击此处可从《Archiv der Pharmazie》网站下载免费的PDF全文](/ch/ext_images/free.gif)
Alhamzah Dh. Hameed Syed Ovais Raed Yaseen Pooja Rathore Mohammed Samim Surender Singh Kalicharan Sharma Mymona Akhtar Kalim Javed 《Archiv der Pharmazie》2016,349(2):150-159
5.
6.
Nawar S. Hamad Nahed H. Al‐Haidery Iman A. Al‐Masoudi Mey Sabri Luma Sabri Najim A. Al‐Masoudi 《Archiv der Pharmazie》2010,343(7):397-403
A new series of 2‐(naphthalen‐2‐yloxy)‐N‐[(aryl‐5‐thioxo‐4,5‐dihydro‐1H‐1,2,4‐triazol‐3‐yl)methyl] acetamides 5a–f was synthesized from naphthalene‐derived glycine derivative 2 via the hydrazinoacetamide analogs 4a–f . Alternatively, treatment of 4a with H2SO4 afforded 2‐(naphthalen‐2‐yloxy)‐N‐((5‐(phenylamino)‐1,3,4‐thiadiazol‐2‐yl)methyl) acetamide 6a . Alkylation or sulphonylation of 5a afforded the S‐alkylated derivatives 7 and 8 , respectively. Interestingly, treatment of 3 with methoxide ion gave the triazine derivative 9 . The synthesized compounds have been screened for their inhibitory activity against HIV‐1 and HIV‐2 in MT‐4 cells. However, 7 was found to be the potent inhibitor in vitro for the replication of HIV‐1 (EC50 = 0.20 μg/mL), suggesting a new lead in the development of an antiviral agent. 相似文献
7.
8.
Ranju Bansal Gaurav Narang Carmen Calle Rosalia Carron Karen Pemberton Alan L. Harvey 《Drug development research》2013,74(1):50-61
Preclinical Research |
9.
Discovery of Novel 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole Derivatives as Potential Anti‐Inflammatory Agents
下载免费PDF全文
![点击此处可从《Chemical biology & drug design》网站下载免费的PDF全文](/ch/ext_images/free.gif)
Xinning Wang Yang Zong Leilei Zhao Junhao Xing Jinpei Zhou Huibin Zhang 《Chemical biology & drug design》2015,86(4):509-516
A novel 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole derivative 5 with good anti‐inflammatory activity was identified from our in‐house library. Based on hit compound 5 , two series of 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole derivative 6a – g and 7a – h were designed and synthesized as novel anti‐inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF‐α production in LPS‐stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm ) and TNF‐α (IC50 = 1.87 μm ) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti‐inflammatory activity than ibuprofen did on xylene‐induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF‐κB in LPS‐stimulated RAW 264.7 macrophages. 相似文献
10.
11.
Design and Synthesis of 2‐Phenoxynicotinic Acid Hydrazides as Anti‐inflammatory and Analgesic Agents
Alireza Moradi Latifeh Navidpour Mohsen Amini Hamid Sadeghian Hooman Shadnia Omidreza Firouzi Ramin Miri Seyed Esmaeil Sadat Ebrahimi Mohammad Abdollahi Mona Haddad Zahmatkesh Abbas Shafiee 《Archiv der Pharmazie》2010,343(9):509-518
A series of 2‐phenoxynicotinic acid hydrazides were synthesized and evaluated for their analgesic and anti‐inflammatory activities. Several compounds having an unsubstituted phenyl/4‐pyridyl or C‐4 methoxy substituent on the terminal phenyl ring showed moderate to high analgesic or anti‐inflammatory activity in comparison to mefenamic acid as the reference drug. The compounds with highest anti‐inflammatory activity were subjected to in vitro COX‐1/COX‐2 inhibition assays and showed moderate to good COX‐1 and weak COX‐2 inhibition activities. 相似文献
12.
Shafiya Yaseen Syed Ovais Rafia Bashir Pooja Rathore Mohammed Samim Surender Singh Vinod Nair Kalim Javed 《Archiv der Pharmazie》2013,346(6):491-498
Nine 4‐arylphthalazones bearing benzenesulfonamide (2a – i ) were synthesized by the condensation of the appropriate 2‐aroylbenzoic acid ( 1a – i ) and 4‐hydrazinobenzenesulfonamide in ethanol. The structures of these compounds were elucidated by elemental analysis, IR, 1H NMR, 13C NMR, and MS spectroscopy. Two compounds, 2b and 2i , showed significant anti‐inflammatory activity comparable to that of the standard drug celecoxib in the carrageenan‐induced rat paw edema model. These compounds ( 2b and 2i ) had selective inhibitory activity towards the COX‐2 enzyme. Compound 2b had a better selectivity ratio (COX‐1/COX‐2) compared to that of celecoxib and can be used as a novel template for the design of selective COX‐2 inhibitors. Compounds 2d and 2i were screened for their antiproliferative activity toward 60 human cancer cell lines by the National Cancer Institute (USA). The compounds 2d and 2i displayed mild activity toward the renal cancer cell line UO‐31. 相似文献
13.
Bilal Ahmad Rather Tilak Raj Aravind Reddy Mohan Paul S. Ishar Samitha Sivakumar Perumal Paneerselvam 《Archiv der Pharmazie》2010,343(2):108-113
A novel series of 2‐substituted‐quinazolin‐4(3H)‐ones were synthesized by reacting 3,5‐disubstituted‐anthranilic acid with acetic anhydride/benzoyl chloride, which were further reacted with different primary amines to obtain 2,6,8‐substituted‐quinazolin‐4(3H)‐ones 6a–f , 7 , 8 . All the synthesized compounds were characterized and screened for analgesic and anti‐inflammatory activities. Compounds 6,8‐dibromo‐2‐phenyl‐3‐(4′‐carboxyl phenyl)quinazolin‐4(3H)‐one 7 and 6,8‐dibromo‐2‐phenyl‐3‐(2′‐phenylethanoic acid)quinazolin‐4(3H)‐one 8 displayed good analgesic and anti‐inflammatory activity in comparison to the reference standards acetyl salicylic acid and indomethacin, respectively. 相似文献
14.
Synthesis and Evaluation of 2‐Alkylthio‐4‐(N‐substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti‐myeloma Agents
下载免费PDF全文
![点击此处可从《Chemical biology & drug design》网站下载免费的PDF全文](/ch/ext_images/free.gif)
Jinbao Xiang Crystal Leung Zhuoqi Zhang Cassie Hu Chao Geng Lili Liu Lang Yi Zhiwei Li James Berenson Xu Bai 《Chemical biology & drug design》2016,87(3):472-477
A series of pyrimidine hydroxamic acids with a sulfide substituent at the second position and a sulfonamide substituent at the fourth position have been synthesized and evaluated for their activity against human myeloma cell line RPMI 8226. Several compounds exhibited significant anti‐cancer potency. It was found that representative compound 6a selectively killed cancerous but not normal cells. Moreover, compound 6a was effective in causing apoptosis in RPMI 8226 cells and exhibited promising HDAC‐inhibitory activities. 相似文献
15.
Cristina Nastasă Brînduşa Tiperciuc Alina Pârvu Mihaela Duma Ioana Ionuţ Ovidiu Oniga 《Archiv der Pharmazie》2013,346(6):481-490
A novel series of 5‐arylidene ‐ 2,4‐thiazolidinediones (TZDs) 2a – p was synthesized from the condensation of 3‐((2‐phenylthiazol‐4‐yl)methyl)thiazolidine‐2,4‐dione with different benzaldehyde derivatives. All the structures were confirmed by their spectral (IR, 1H NMR, 13C NMR and mass) and elemental analytical data. The new molecules were evaluated in vivo as anti‐inflammatory agents in an acute experimental inflammation, evaluating the acute phase bone marrow response and phagocyte activity. All compounds, excepting one, reduced the absolute leukocytes count due to the lower neutrophil percentage. Phagocytary index was decreased by the same molecules, while only half of them reduced the phagocytary activity. The effect was superior to meloxicam, the reference anti‐inflammatory drug, for the majority of the TZD derivatives. The new molecules were also investigated for their antimicrobial properties on Gram‐positive and Gram‐negative bacteria and one fungal strain. Two compounds ( 2e and 2n ) manifested growth inhibition capacity on all the tested strains. 相似文献
16.
17.
18.
V. Alagarsamy V. Raja Solomon R. V. Sheorey R. Jayakumar 《Chemical biology & drug design》2009,73(4):471-479
A new series of 3‐(3‐ethylphenyl)‐2‐substituted hydrazino‐3H‐quinazolin‐4‐ones were synthesized by reacting the amino group of 2‐hydrazino‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one with a variety of aldehydes and ketones. The title compounds were investigated for analgesic, anti‐inflammatory and ulcerogenic index behavior. The compound 2‐(N′‐3‐pentylidene‐hydrazino)‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one ( AS2 ) emerged as the most active compound in exhibiting analgesic activity and the compound 2‐(N′‐2‐pentylidene‐hydrazino)‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one ( AS3 ) emerged as the most active compound in exhibiting anti‐inflammatory activity; and these compounds are moderately potent when compared with the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared with aspirin. 相似文献
19.
20.
Rahul P. Modh Amit C. Patel Dharmesh H. Mahajan Christophe Pannecouque Erik De Clercq Kishor H. Chikhalia 《Archiv der Pharmazie》2012,345(12):964-972
In an attempt to afford possible antibacterial and anti‐human immunodeficiency virus (HIV) agents, a series of 22 novel styryl quinazoline‐based heterocyclic entities were designed and synthesized. Various substituted aryl urea and thiourea cores were incorporated at position 4 of quinazoline, followed by styrylation of position 2, aiming at an augmented biological potential. The synthesized compounds were well characterized through IR, 1H NMR, 13C NMR and elemental analyses. All compounds were screened for their in vitro anti‐HIV activity against the HIV‐1 (IIIB) and HIV‐2 (ROD) strains. The antibacterial activity was also evaluated against various pathogenic Gram‐positive and Gram‐negative bacterial strains. 相似文献