Total synthesis and biological evaluation of seven new anti-inflammatory oxacyclododecindione-type macrolactones

2020 ◽  
Vol 18 (30) ◽  
pp. 5906-5917
Author(s):  
Carina Weber ◽  
Nina Vierengel ◽  
Thorsten Walter ◽  
Torsten Behrendt ◽  
Tobias Lucas ◽  
...  

Seven new macrolactones of the oxacyclododecindione family have been synthesized and tested for their inhibitory activity on TGF-β-inducible Smad2/3- as well as IL-4-inducible STAT6-dependent signalling pathways.

2006 ◽  
Vol 16 (24) ◽  
pp. 6155-6160 ◽  
Author(s):  
Chung-Ren Su ◽  
Yuh-Chiang Shen ◽  
Ping-Chung Kuo ◽  
Yann-Lii Leu ◽  
Amooru G. Damu ◽  
...  

2019 ◽  
Vol 2019 (13) ◽  
pp. 2376-2381 ◽  
Author(s):  
Hanuman P. Kalmode ◽  
Suhag S. Patil ◽  
Kishor L. Handore ◽  
Paresh R. Athawale ◽  
Rambabu Dandela ◽  
...  

2017 ◽  
Vol 13 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Jelena Savic ◽  
Sanda Dilber ◽  
Marina Milenkovic ◽  
Jelena Kotur-Stevuljevic ◽  
Bojan Markovic ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3224
Author(s):  
Leander Geske ◽  
Ulrich Kauhl ◽  
Mohamed E. M. Saeed ◽  
Anja Schüffler ◽  
Eckhard Thines ◽  
...  

The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regioselective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.


2017 ◽  
Vol 33 (6) ◽  
pp. 890-894 ◽  
Author(s):  
Bohua Long ◽  
Jingzhao Zhang ◽  
Xueyan Wang ◽  
Xudong Tang ◽  
Zhengzhi Wu

2009 ◽  
Vol 131 (30) ◽  
pp. 10587-10597 ◽  
Author(s):  
K. C. Nicolaou ◽  
Xiao-Shui Peng ◽  
Ya-Ping Sun ◽  
Damien Polet ◽  
Bin Zou ◽  
...  

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.


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