Mannich reaction

The novel series of 2-mercaptobenzimodazole derivative were synthesized by using secondary amine i.e. diethyl amine and aromatic aldehyde. In Mannish reaction instead of formaldehyde other aromatic aldehyde was used. This was main aim of present study. Same derivatives were synthesized by using Microwave technique & reaction time, practice yield were compared. The purity of synthesized compounds was checked by Melting point and TLC and their structure was established by various analytical techniques such as IR,1HNMR, Mass spectral studies. These Compounds were screened for their  Anticonvulsant activity.  Anticonvulsant activity was evaluated by PTZ induced model. Keyword- Mannich reaction, 2-Mercapto Benzimidazole, Aromatic aldehyde.

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.