Peptide-based drug discovery: Current status and recent advances

K Sharma, KK Sharma, A Sharma, R Jain - Drug Discovery Today, 2023‏ - Elsevier
Highlights•A comprehensive compilation and analysis of FDA approved and under clinical
trials peptide-based therapeutics.•Clinical trial peptides pipeline analysis reveals emerging …

Design, synthesis, and applications of ring‐functionalized histidines in peptide‐based medicinal chemistry and drug discovery

K Sharma, KK Sharma, A Mahindra… - Medicinal Research …, 2023‏ - Wiley Online Library
Modified and synthetic α‐amino acids are known to show diverse applications. Histidine,
which possesses numerous applications when subjected to synthetic modifications, is one …

Modified histidine containing amphipathic ultrashort antifungal peptide, His [2-p-(n-butyl) phenyl]-Trp-Arg-OMe exhibits potent anticryptococcal activity

KK Sharma, R Ravi, IK Maurya, A Kapadia… - European Journal of …, 2021‏ - Elsevier
In pursuit of ultrashort peptide-based antifungals, a new structural class, His (2-aryl)-Trp-Arg
is reported. Structural changes were investigated on His-Trp-Arg scaffold to demonstrate the …

Functionalization of superparamagnetic Fe3O4@ SiO2 nanoparticles with a Cu (II) binuclear Schiff base complex as an efficient and reusable nanomagnetic catalyst …

AR Sardarian, M Kazemnejadi… - Applied …, 2021‏ - Wiley Online Library
Fe3O4@ SiO2 nanoparticles was functionalized with a binuclear Schiff base Cu (II)‐complex
(Fe3O4@ SiO2/Schiff base‐Cu (II) NPs) and used as an effective magnetic hetereogeneous …

Palladium-catalyzed aminocarbonylation of (hetero) aryl iodides with α-amino acid esters as nucleophiles

GK Rathod, R Jain - The Journal of Organic Chemistry, 2022‏ - ACS Publications
We report palladium-catalyzed aminocarbonylation of (hetero) aryl iodides with α-amino
acid esters as nucleophiles. The synthesized N-capped α-amino acids are biologically …

Synthetic amino acids-derived peptides target Cryptococcus neoformans by inducing cell membrane disruption

K Sharma, S Aaghaz, IK Maurya, KK Sharma… - Bioorganic …, 2023‏ - Elsevier
We investigated synthetic amino acid-based approach to design short peptide-based
antibiotics. Tautomerically restricted, amphiphilic 1-aryl-l-histidines along with hydrophobic …

Discovery of a Membrane-Active, Ring-Modified Histidine Containing Ultrashort Amphiphilic Peptide That Exhibits Potent Inhibition of Cryptococcus neoformans

KK Sharma, IK Maurya, SI Khan… - Journal of medicinal …, 2017‏ - ACS Publications
The new structural classes of ultrashort peptides that exhibit potent microbicidal action have
potential as future drugs. Herein, we report that C-2 arylated histidines containing tripeptides …

Recent developments in selective N-arylation of azoles

P Halder, T Roy, P Das - Chemical Communications, 2021‏ - pubs.rsc.org
Transition-metal based carbon–heteroatom (C–X) bond formation has attracted the attention
of synthetic chemists over the past few years because the resultant aryl/heteroaryl motifs are …

Ultrasound-promoted synthesis of novel N-arylamino-3, 5′-biquinoline derivatives: their applications in live-cell imaging and in vitro anticancer activity evaluation

A Alizadeh, A Rostampoor, M Alipour… - New Journal of …, 2023‏ - pubs.rsc.org
A novel strategy for the construction of functionalized N-arylamino-3, 5′-biquinoline has
been developed. The reaction involves base-mediated Knoevenagel condensation between …

Advances in microwave-assisted synthesis and the impact of novel drug discovery

E Berrino, CT Supuran - Expert opinion on drug discovery, 2018‏ - Taylor & Francis
ABSTRACT Introduction: Microwave (MW)-assisted synthesis of biologically active
compounds has received a lot of attention in the last decades due to the advantages that …