Design and Synthesis of Heterocyclic Conjugated Peptides as Novel Antimicrobial Agents

Design and synthesis of tryptophan containing peptides as potential analgesic and anti‐inflammatory agents

“…In this perspective, our next goal was to extend the length of the peptide chain. It was noticed that increasing the peptide chain length increased the pharmacological profile of the synthesized peptides [23,24]. This fact is substantiated by the evidence that the tetrapeptide GFGW (29) has exhibited 65% activity, whereas the hexapeptides have shown 71-73% activity.…”

“…Each peptide (8-19) (0.003 mol) was hydrolysed in methanol (10 ml/g of peptide) using cold solution of 1 N NaOH (15 ml) for 2 h. The completion of the reaction was monitored by TLC, solvent was evaporated, cooled, neutralized with cold 1 N HCl, extracted with CHCl 3 , washed with 1 N HCl followed by water and dried over anhydrous Na 2 SO 4 . The solvent was removed under pressure and triturated with ether, filtered, washed with ether and dried to obtain carboxyl free peptides as hygroscopic foam (20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30)(31).…”

“…From the results, it was observed that the test compounds revealed significant analgesic and anti-inflammatory properties. Among the N-Fmoc containing dipeptides such as Gly (20), Pro (21), Phe (22), Lys(Boc) (23) and His(Trt) (24), compound 24 has shown high activity, which could be due to aromaticity of His as well as trityl group, acid-base character and H-binding affinity of His. This is followed by Lys(Boc).…”

“…Led by the previous facts and coupled with our ongoing project aimed at investigating new bioactive molecules derived from amino acid/peptide conjugates [22][23][24][25][26], the present work involves the synthesis of a series of smaller peptides with Trp at the C-terminal as common entity and varying different protected amino acids/peptides at the N-terminal ( Figure 1). Laboratories Pvt.…”

Synthesis, characterization and antibacterial study of tripodal tris-(N-benzoylthioureido)ethylamine

“…It shows the presence of the hydrophilic groups such as hydroxyl plays an important role although the molecule is large. The increasing polarity of molecule would help the molecule to interact or penetrate more effectively through the cell membrane and thereby inactivating them [28]. Inclusions of the electron withdrawing group for example halogens into the thiourea system are expected to enhance the activity [29].…”