Combinatorial chemistry in drug discovery

R Liu, X Li, KS Lam - Current opinion in chemical biology, 2017 - Elsevier
Several combinatorial methods have been developed to create focused or diverse chemical
libraries with a wide range of linear or macrocyclic chemical molecules: peptides, non …

An overview of biochemically characterized drug targets in metabolic pathways of Leishmania parasite

S Raj, S Sasidharan, SN Balaji, P Saudagar - Parasitology Research, 2020 - Springer
Leishmaniasis is a neglected tropical disease with no effective vaccines to date. Globally, it
affects around 14 million people living in undeveloped and developing countries …

Development of novel anti-leishmanials: the case for structure-based approaches

M Soni, JV Pratap - Pathogens, 2022 - mdpi.com
The neglected tropical disease (NTD) leishmaniasis is the collective name given to a diverse
group of illnesses caused by~ 20 species belonging to the genus Leishmania, a majority of …

Recent advances in chemotherapeutics for leishmaniasis: Importance of the cellular biochemistry of the parasite and its molecular interaction with the host

R Singh, M Kashif, P Srivastava, PP Manna - Pathogens, 2023 - mdpi.com
Leishmaniasis, a category 1 neglected protozoan disease caused by a kinetoplastid
pathogen called Leishmania, is transmitted through dipteran insect vectors (phlebotomine …

Design, synthesis and biological evaluation of dual Topo II/HDAC inhibitors bearing pyrimido [5, 4-b] indole and pyrazolo [3, 4-d] pyrimidine motifs

M Zhao, K Yang, X Zhu, T Gao, W Yu, H Liu… - European Journal of …, 2023 - Elsevier
Abstract Both topoisomerase II (Topo II) and histone deacetylase (HDAC) are important
therapeutic targets for cancer. In this study, two series of novel compounds containing …

Design, synthesis, and fungicidal evaluation of novel pyrazole-furan and pyrazole-pyrrole carboxamide as succinate dehydrogenase inhibitors

TT Yao, DX Xiao, ZS Li, JL Cheng… - Journal of agricultural …, 2017 - ACS Publications
The identification of novel succinate dehydrogenase (SDH) inhibitors represents one of the
most attractive directions in the field of fungicide research and development. During our …

Molecular-level strategic goals and repressors in Leishmaniasis–Integrated data to accelerate target-based heterocyclic scaffolds

M Abirami, BK Kumar, S Dey, S Johri… - European Journal of …, 2023 - Elsevier
Leishmaniasis is a complex of neglected tropical diseases caused by various species of
leishmanial parasites that primarily affect the world's poorest people. A limited number of …

Topoisomerase 1B poisons: Over a half‐century of drug leads, clinical candidates, and serendipitous discoveries

MA Cinelli - Medicinal Research Reviews, 2019 - Wiley Online Library
Topoisomerases are DNA processing enzymes that relieve supercoiling (torsional strain) in
DNA, are necessary for normal cellular division, and act by nicking (and then religating) …

In vitro anti-Leishmania activity and molecular docking of spiro-acridine compounds as potential multitarget agents against Leishmania infantum

FS Almeida, GLS Sousa, JC Rocha, FF Ribeiro… - Bioorganic & Medicinal …, 2021 - Elsevier
Leishmaniasis is an infectious disease with several limitations regarding treatment schemes.
This work reports the anti-Leishmania activity of spiroacridine compounds against the …

[HTML][HTML] The ultimate fate determinants of drug induced cell-death mechanisms in Trypanosomatids

P Das, S Saha, S BoseDasgupta - International Journal for Parasitology …, 2021 - Elsevier
Chemotherapy constitutes a major part of modern-day therapy for infectious and chronic
diseases. A drug is said to be effective if it can inhibit its target, induce stress, and thereby …