Psoriasis and psoriatic arthritis are immune-mediated chronic inflammatory disorders which predominantly involve skin and joints. Around the world, it has affected nearly 38 million people worldwide. In 2014, Celgene Corporation’s (S)-apremilast was introduced to treat patients suffering from the different types of psoriasis. In this review, we discuss the different strategies for the synthesis of (S)-apremilast which will help further develop novel routes for its synthesis.

Utilizing the solid phase peptide synthesis protocol, we have designed and prepared a novel dipeptide library containing (S)‐5‐oxopyrrolidine‐2‐carboxylic acid moiety. All the newly synthesized dipeptides were characterized by spectroscopic techniques as well as elemental analysis. Furthermore, the in vitro antimicrobial activities of the synthesized dipeptide conjugates were evaluated. Two Gram‐positive (Streptococcus pyogenes and Staphylococcus aureus) and two Gram‐negative bacteria (Escherichia coli and Pseudomonas aeruginosa) were utilized to evaluate the antibacterial activity of the screened derivatives. In contrast to the standard drug Ampicillin, the targeted derivatives exhibited good antibacterial activity. Additionally, two fungi (Candida albicans and Aspergillus niger) were used to evaluate the antifungal activity of the target dipeptides. The targeted derivatives also exhibited good antifungal activity compared to the standard drug Nystatin. In continuous, the molecular docking study of the targeted derivatives was also carried out, which revealed that the dipeptide analogs showed encouraging binding interaction networks with Escherichia coli DNA gyrase B and lanosterol‐14 alpha demethylase resulting in antibacterial and antifungal activities, respectively. Such synthesis, biological evolution, and molecular docking study of peptide derivatives with oxopyrrolidine conjugates open the door for the future development of new therapeutics containing heterocycle and peptide hybrids with potency as antimicrobial agents.

Aims:The research is aimed at developing an economic and sustainable growth medium using abundantly available and highly nutritive agro-industrial waste soybean meal as the substrate for the production of violacein by Chromobacterium violaceum. Methods and Results:Violacein produced using soybean meal medium was compared with the commercial complex growth media. Upon utilization of 2% w/v soybean meal (SM 2 ) medium, 496 mg/L crude violacein was achieved after 48-hr incubation time, which was 1.62-fold higher than the crude violacein produced in Luria-Bertani (LB) broth. Additionally, supplementation of 100 mg/L L-tryptophan to 1% and 2% w/v soybean meal (SMT 1 and SMT 2 ) medium yielded 1217 mg/L (3.96fold higher as compared to LB) and 1198 mg/L (3.90-fold higher as compared to LB) crude violacein respectively. Optimization of culture conditions and concentration of L-tryptophan using Box-Behnken design (BBD) model produced as high as 1504.5 mg/L crude violacein. To the best of our knowledge, this is the highest crude violacein produced to date using agro-industrial-based waste as a substrate with minimal supplementation in a shake flask. Conclusions:The study signifies the potentiality of soybean meal as a cost-effective growth medium for the production of violacein. Optimization of the fermentation parameters clearly demonstrated a surge in violacein production. Significance and Impact of the Study: Utilization of soybean meal as an alternative to the expensive commercial media would surely promote the large-scale synthesis of this multifaceted compound.

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Epilepsy is a chronic neurological disorder in the brain, affecting individuals of all age groups. Nearly 1% of the world population is affected by seizure disorder, of which 80% of the patients are observed in underdeveloped and developing countries. The predominant treatment option for epilepsy includes an antiepileptic drug named brivaracetam. This drug emerged as an unusual success of rational drug discovery in clinical development by exhibiting magnificent affinity toward synaptic vesicle glycoprotein as compared to conventional drug levetiracetam and piracetam. Given its efficiency in limiting the progression of epilepsy, this drug has drawn considerable attention of researchers to devise novel routes of its synthesis. The present review encapsulates the reported literature on synthetic strategies for brivaracetam, which will assist medicinal chemists in the further progress of its synthesis.