Pyrazole Derivatives as Photosynthetic Electron Transport Inhibitors:  New Leads and Structure−Activity Relationship

2005 ◽  
Vol 53 (10) ◽  
pp. 3848-3855 ◽  
Author(s):  
Chiara B. Vicentini ◽  
Salvatore Guccione ◽  
Laura Giurato ◽  
Rebecca Ciaccio ◽  
Donatella Mares ◽  
...  
Keyword(s):  
Electron Transport ◽  
Photosynthetic Electron Transport ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Pyrazole Derivatives ◽  
Structure Activity ◽  
Transport Inhibitors

Quantitative Structure Activity Relationship of Diphenylamines as Inhibitors of Photosynthetic Electron Transport and Photophosphorylation

1979 ◽  
Vol 34 (11) ◽  
pp. 1024-1027 ◽  
Author(s):  
Walter Oettmeier
Keyword(s):  
Electron Transport ◽  
Electron Flow ◽  
Photosynthetic Electron Transport ◽  
Quantitative Structure Activity Relationship ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Quantitative Structure ◽  
Structure Activity ◽  
Cyclic Photophosphorylation ◽  
Relationship Of

Abstract A number of 16 substituted diphenylamines have been tested for their inhibitory activity on photosynthetic NADP reduction and photophosphorylation. The most active compounds exhibited pI50 values of 6.0 in photosynthetic electron transport and 6.8 in cyclic photophosphorylation, respectively. The inhibition site in electron flow of the diphenylamines is located between the two photosystems. Necessary for high activity is the substitution of the phenyl moieties by several strongly electron withdrawing substituents. A quantitative structure activity relationship according to a parabolic Hansch approach could be accomplished by using the Hammett electronic parameter as the only variable.

Synthesis of Pyrazole Derivatives and Their Evaluation as Photosynthetic Electron Transport Inhibitors

2004 ◽  
Vol 52 (7) ◽  
pp. 1898-1906 ◽  
Author(s):  
Chiara B. Vicentini ◽  
Donatella Mares ◽  
Alfredo Tartari ◽  
Maurizio Manfrini ◽  
Giuseppe Forlani
Keyword(s):  
Electron Transport ◽  
Photosynthetic Electron Transport ◽  
Pyrazole Derivatives ◽  
Transport Inhibitors

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 17-27 ◽  
Author(s):  
Elda Meta ◽  
Chiara Brullo ◽  
Michele Tonelli ◽  
Scott G. Franzblau ◽  
Yuehong Wang ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Pyrazole Derivatives ◽  
Antitubercular Agents ◽  
Active Compounds ◽  
Protein Targets ◽  
Preliminary Screening ◽  
New Class ◽  
Structure Activity ◽  
Starting Point

Background: We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, on their novelty with respect to the pipeline drugs. </P><P> Methods: In order to increase the potency and obtain more information about structure-activity relationship (SAR), we designed and synthesized three new series of compounds (2a–e, 3a–e, and 4a–l). Conclusion: Performed tests confirmed that both new pyrazoles and imidazo-pyrazoles could represent a new starting point to obtain more potent compounds and further work is now underway to identify the protein targets of this new class of anti-TB agents.

Structure-Activity Relationships and Physiological Aspects of New Photosynthetic Electron Transport Inhibitors, 3-Alkylaminoalkyliden-2H-pyran-2,4(3H)-diones (APs)

1988 ◽  
Vol 43 (11-12) ◽  
pp. 857-861 ◽  
Author(s):  
Tadao Asami ◽  
Hiroyuki Koike ◽  
Yorinao Inoue ◽  
Nobutaka Takahashi ◽  
Shigeo Yoshida
Keyword(s):  
Electron Transport ◽  
Photosynthetic Electron Transport ◽  
Structural Requirement ◽  
Structure Activity Relationships ◽  
New Class ◽  
Structure Activity ◽  
Transport Inhibition ◽  
Transport Inhibitors

3-Aminoalkylidene-2H-pyran-2,4(3H)-diones (APs), possessing a conjugated enamino moiety which is common to cyanoacrylates and 2-aminoalkylidenecyclohexane-1,3-diones (ACs), were found as a new class of photosynthetic electron transport inhibitors. Although the structural requirement of APs for photosynthetic electron transport inhibition was very similar to that of cyanoacrylates and ACs, thermoluminescence measurements indicated that the binding manner of APs to D 1 protein was totally different from that of other inhibitors.

Structure–Activity Relationship and Pharmacology of γ‐Aminobutyric Acid (GABA) Transport Inhibitors

2006 ◽  
pp. 265-284 ◽  
Author(s):  
Rasmus Prætorius Clausen ◽  
Karsten Madsen ◽  
Orla Miller Larsson ◽  
Bente Frølund ◽  
Povl Krogsgaard‐Larsen ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Aminobutyric Acid ◽  
Activity Relationship ◽  
Gaba Transport ◽  
Structure Activity ◽  
Transport Inhibitors
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