Design, Synthesis, and in Vitro Gene Delivery Efficacies of Novel Cholesterol-Based Gemini Cationic Lipids and Their Serum Compatibility:  A Structure−Activity Investigation

2007 ◽  
Vol 50 (10) ◽  
pp. 2432-2442 ◽  
Author(s):  
Avinash Bajaj ◽  
Paturu Kondiah ◽  
Santanu Bhattacharya
Keyword(s):  
Gene Delivery ◽  
Cationic Lipids ◽  
Design Synthesis ◽  
Structure Activity

Synthesis and Evaluation of Cationic Lipids Bearing Cholesteryl Groups for Gene Delivery in vitro.

ChemInform ◽  
2003 ◽  
Vol 34 (7) ◽  
Author(s):  
Man-Zhou Zhu ◽  
Qi-Hua Wu ◽  
Guisheng Zhang ◽  
Tan Ren ◽  
Dexi Liu ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Cationic Lipids

scholarly journals Cationic lipids with a cyclen headgroup: synthesis and structure–activity relationship studies as non-viral gene vectors

RSC Advances ◽  
2017 ◽  
Vol 7 (30) ◽  
pp. 18681-18689 ◽  
Author(s):  
De-Chun Chang ◽  
Yi-Mei Zhang ◽  
Ji Zhang ◽  
Yan-Hong Liu ◽  
Xiao-Qi Yu
Keyword(s):  
Gene Delivery ◽  
Structure Activity Relationship ◽  
Cationic Lipids ◽  
Activity Relationship ◽  
Viral Gene ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Gene Delivery Vectors ◽  
Gene Vectors ◽  
Viral Gene Delivery

The structure–activity relationships of cyclen-based cationic lipids as non-viral gene delivery vectors were studied and clarified.

Synthesis and antimicrobial activity of aryldiazenyl/arylhydrazono pyrazoles

2021 ◽  
Vol 45 (11-12) ◽  
pp. 1093-1099
Author(s):  
Abdulrhman Alsayari ◽  
Yahya I Asiri ◽  
Abdullatif Bin Muhsinah ◽  
Mohd. Zaheen Hassan
Keyword(s):  
Active Site ◽  
Phenyl Ring ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Docking Studies ◽  
Considerable Effect ◽  
Design Synthesis ◽  
Structure Activity ◽  
Antimicrobial Evaluation

We report the design, synthesis, and in vitro antimicrobial evaluation of functionalized pyrazoles containing a hydrazono/diazenyl moiety. Among these newly synthesized derivatives, 4-[2-(4-chlorophenyl)hydrazono]-5-methyl-2-[2-(naphthalen-2-yloxy)acetyl]-2,4-dihydro-3 H-pyrazol-3-one is a promising antimicrobial agent against Staphylococcus aureus (minimum inhibitory concentration 0.19 μg mL−1). Structure–activity relationship studies reveal that the electronic environment on the distal phenyl ring has a considerable effect on the antimicrobial potential of the hybrid analogues. Molecular docking studies into the active site of S. aureus dihydrofolate reductase also prove the usefulness of hybridizing a pyrazole moiety with azo and hydrazo groups in the design of new antimicrobial agents.

α‐Tocopherol‐Conjugated, Open Chain Sugar‐Mimicking Cationic Lipids: Design, Synthesis and In–Vitro Gene Transfection Properties

2021 ◽  
Vol 6 (46) ◽  
pp. 13025-13033
Author(s):  
Venkatesh Ravula ◽  
Venkanna Muripiti ◽  
Shireesha Manthurthi ◽  
Srilakshmi V. Patri
Keyword(s):  
Gene Transfection ◽  
Cationic Lipids ◽  
Open Chain ◽  
Design Synthesis

Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents

2020 ◽  
Vol 44 (6) ◽  
pp. 2247-2255
Author(s):  
Qifan Zhou ◽  
Lina Jia ◽  
Fangyu Du ◽  
Xiaoyu Dong ◽  
Wanyu Sun ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Activity Assay ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Enhancer Of Zeste

A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with in vitro biological activity assay and docking results.

Synthesis and in Vitro Evaluation of Glutamide-Containing Cationic Lipids for Gene Delivery

2006 ◽  
Vol 17 (6) ◽  
pp. 1530-1536 ◽  
Author(s):  
Vijaya Gopal ◽  
Tekkatte K. Prasad ◽  
Nalam M. Rao ◽  
Makoto Takafuji ◽  
Mohammed M. Rahman ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Cationic Lipids ◽  
In Vitro Evaluation

Cyclen-based cationic lipids containing a pH-sensitive moiety as gene delivery vectors

2015 ◽  
Vol 13 (2) ◽  
pp. 620-630 ◽  
Author(s):  
Zheng Huang ◽  
Yan-Hong Liu ◽  
Yi-Mei Zhang ◽  
Ji Zhang ◽  
Qiang Liu ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Structure Activity Relationship ◽  
Ph Sensitive ◽  
Cationic Lipids ◽  
Activity Relationship ◽  
Structure Activity ◽  
Gene Delivery Vectors

Imidazole-functionalized cationic lipids with a cyclen headgroup were synthesized, and the structure–activity relationship in gene delivery mediated by these lipids was discussed.

Synthesis and in vitro evaluation of substituted aryl- and hetarylmethyl phosphonate and phosphate — UMP derivatives as potential glucosyltransferase inhibitors

2002 ◽  
Vol 80 (8) ◽  
pp. 973-982 ◽  
Author(s):  
Asish K Bhattacharya ◽  
Florian Stolz ◽  
Jürgen Kurzeck ◽  
Wolfgang Rüger ◽  
Richard R Schmidt
Keyword(s):  
Transition State ◽  
Enzyme Inhibitors ◽  
Future Generations ◽  
Arbuzov Reaction ◽  
Inhibition Kinetics ◽  
Design Synthesis ◽  
Double Stranded Dna ◽  
Structure Activity ◽  
Potential Inhibitors

The enzyme β (1[Formula: see text]4)-glucosyltransferase (BGT) catalyses the transfer of glucose from uridine diphosphoglucose (UDP-Glc) to 5-hydroxymethylcytosine (5-HMC) bases in double-stranded DNA. Potential inhibitors of BGT were developed by structure-based design and synthesized. The designed inhibitors 1–6 provide conformational mimicry of the transition state in glucosyltransfer reactions. The key synthetic steps involve a Michaelis–Arbuzov reaction followed by coupling with uridine-5'-morpholidophosphate as activated UMP derivative. The compounds were tested for in vitro inhibitory activity against BGT and the inhibition kinetics were examined. Three of the designed molecules were found to be potential inhibitors of BGT having IC50 values in the micromolar (µM) range. Useful structure–activity relationships were established which provide guidelines for the design of future generations of inhibitors of BGT.Key words: β-glucosyltransferase, transition state, enzyme inhibitors, structure-based design, synthesis.

scholarly journals Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3320 ◽  
Author(s):  
Kai-Yi Wang ◽  
Zhi-Wen Zhou ◽  
Heng-Yuan Zhang ◽  
Yu-Cheng Cao ◽  
Jin-Yi Xu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Triterpenoid Saponin ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Good Antibacterial Activity ◽  
Structure Activity ◽  
In Vitro Antibacterial Activity ◽  
Free Hydroxyl

Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.

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