Dihydrofolate reductase inhibitors: Patent landscape and phases of clinical development (2001–2021)
Introduction Dihydrofolate reductase (DHFR) plays an important role in the biosynthesis of
amino acid and folic acid. It participates by reducing dihydrofolate to tetrahydrofolate, in the …
amino acid and folic acid. It participates by reducing dihydrofolate to tetrahydrofolate, in the …
A review on multipurpose potential of bioactive heterocycle quinoxaline
In last few decades, nitrogen‐containing heterocycles have maintained their status as an
important core of FDA‐approved drugs and medicinally active compounds. Quinoxaline is …
important core of FDA‐approved drugs and medicinally active compounds. Quinoxaline is …
From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity
MH El-Shershaby, A Ghiaty, AH Bayoumi… - Bioorganic & Medicinal …, 2021 - Elsevier
Inhibition of PCAF bromodomain has been validated as a promising strategy for the
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …
The antimicrobial potential and pharmacokinetic profiles of novel quinoline-based scaffolds: synthesis and in silico mechanistic studies as dual DNA gyrase and …
MH El-Shershaby, KM El-Gamal, AH Bayoumi… - New Journal of …, 2021 - pubs.rsc.org
The resistance of pathogenic microbes to currently available antimicrobial agents has been
considered a global alarming concern. Hence, close attention should be paid to the …
considered a global alarming concern. Hence, close attention should be paid to the …
Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives
MH El‐Shershaby, KM El‐Gamal… - Archiv der …, 2021 - Wiley Online Library
Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline
derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed …
derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed …
New Pyrazole-Clubbed Pyrimidine or Pyrazoline Hybrids as Anti-Methicillin-Resistant Staphylococcus aureus Agents: Design, Synthesis, In Vitro and In Vivo …
Two hybrid series of pyrazole-clubbed pyrimidines 5a–c and pyrazole-clubbed pyrazoline
compounds 6a, b and 7 were designed as attractive scaffolds to be investigated in vitro and …
compounds 6a, b and 7 were designed as attractive scaffolds to be investigated in vitro and …
Design, Synthesis, antimicrobial screening and molecular modeling of novel 6, 7 dimethylquinoxalin-2 (1H)-one and thiazole derivatives targeting DNA gyrase …
RM Alqurashi, TA Farghaly, R Sabour… - Bioorganic …, 2023 - Elsevier
Abstract New 6, 7-dimethylquinoxalin-2 (1H)-one and hydrazineylidene thiazol-4-one
derivatives were synthesized, and evaluated for their in vitro antimicrobial activity. The …
derivatives were synthesized, and evaluated for their in vitro antimicrobial activity. The …
Introducing of novel class of pyrano[2,3-c]pyrazole-5-carbonitrile analogs with potent antimicrobial activity, DNA gyrase inhibition, and prominent pharmacokinetic …
Microbiological DNA gyrase is recognized as an exceptional microbial target for the
innovative development of low-resistant and more effective antimicrobial drugs. Hence, we …
innovative development of low-resistant and more effective antimicrobial drugs. Hence, we …
An insight into synthetic strategies and recent developments of dihydrofolate reductase inhibitors
The dihydrofolate reductase (DHFR) is a significant target in cancer, microbial infection,
fungal infection, malaria, leishmaniasis, and tuberculosis, among other diseases. The DHFR …
fungal infection, malaria, leishmaniasis, and tuberculosis, among other diseases. The DHFR …
Structure based design and synthesis of 3-(7-nitro-3-oxo-3, 4-dihydroquinoxalin-2-yl) propanehydrazide derivatives as novel bacterial DNA-gyrase inhibitors: In-vitro …
Antimicrobial resistance (AMR) is one of the critical challenges that have been encountered
over the past years. On the other hand, bacterial DNA gyrase is regarded as one of the most …
over the past years. On the other hand, bacterial DNA gyrase is regarded as one of the most …