mail
editor@ajptr.com
whatsapp
9409046853
logo

American Journal of PharmTech Research

Muniraj Krishnaveni Yuvapriya*1.Periasamy Selvakumar1. Chandrasekar Balachandran

Author Profile
1
Publications
1
Years Active
0
Collaborators
43
Citations

Publications by Muniraj Krishnaveni Yuvapriya*1.Periasamy Selvakumar1. Chandrasekar Balachandran

1 publication found • Active 2017-2017

2017

1 publication

Novel Synthetic Unnatural β3 aminoacids via acid hydrolysis of diazepinones as Synthons for Antibiotics

2/1/2017

A convenient two-step method for the preparation of β3-amino acids is described.  This paper describes an efficient and straightforward two-step synthetic sequence leading in excellent yields to a relatively inaccessible lipophilic β3-amino acids with antimicrobial potential  from easily available starting materials. Schmidt reaction of substituted piperidin-4-ones with HN3 generated in situ afforded the corresponding diazapinones. Acid hydrolysis of chosen diazapinones yielded β3-amino acids. Selective cleavage of only the lactam bond is achieved using 4N HCl-MeOH (1:1) mixture   leading to the formation of N-alkyl β3-amino acids in quantitative yields. synthesized  aminoacids are subjected to antimicrobial activity for gram positive, gram negative bacteria, fungi. compounds  3e & 3h  possess excellent antimicrobial and antifungal activity comparable to standard streptomycin and ketoconazole. Therefore obtained β3-amino acids serves as a scaffold for  synthetic  antibiotics  as they have desired structural moieties necessary for antibiotic action. Further refinement of  the β3-amino acids  using  either conjugation or structural modification or incorporation of these aminoacids into synthetic peptides would bring about excellent antimicrobial activity.

Author Statistics
Total Publications:1
Years Active:1
First Publication:2017
Latest Publication:2017
Collaborators:0
Citations:43
Whatsapp