Synthetic and medicinal chemistry of phthalazines: Recent developments, opportunities and challenges

S Zaib, I Khan - Bioorganic Chemistry, 2020 - Elsevier
Fused diaza-heterocycles constitute the core structure of numerous bioactive natural
products and effective therapeutic drugs. Among them, phthalazines have been recognized …

Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro …

AA Al-Karmalawy, MS Nafie, MA Shaldam… - Journal of Medicinal …, 2022 - ACS Publications
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-
nucleoside selective telomerase inhibitor; however, it experiences ineligible …

The long and winding road of designing phosphodiesterase inhibitors for the treatment of heart failure

NF Nadur, LL de Azevedo, L Caruso… - European journal of …, 2021 - Elsevier
Cyclic nucleotide phosphodiesterases (PDEs) are a superfamily of enzymes known to play a
critical role in the indirect regulation of several intracellular metabolism pathways through …

Discovery of novel pyridazine-tethered sulfonamides as carbonic anhydrase II inhibitors for the management of glaucoma

HO Tawfik, MM Saleh, A Ammara… - Journal of Medicinal …, 2024 - ACS Publications
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left
untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective …

Muti-target rationale design of novel substituted N-phenyl-2-((6-phenylpyridazin-3-yl) thio) acetamide candidates as telomerase/JAK1/STAT3/TLR4 inhibitors: In vitro …

MA Shaldam, MHA Mousa, HO Tawfik… - Bioorganic …, 2024 - Elsevier
In this work, additional effort was applied to design new BIBR1532-based analogues with
potential inhibitory activity against telomerase and acting as multitarget antitumor candidates …

Bromination of indazoles enhanced by organic-dye, visible-light photoredox catalysis

LF Hornbrook, CD Reed, AA Lamar - Tetrahedron, 2023 - Elsevier
A variety of functionalized indazoles are brominated in moderate to excellent yields using N-
bromosuccinimide (NBS) under visible-light activated conditions. A screening of organic dye …

[HTML][HTML] Scaffold repurposing reveals new nanomolar phosphodiesterase type 5 (pde5) inhibitors based on pyridopyrazinone scaffold: Investigation of in vitro and in …

KM Amin, OM El-Badry, DE Abdel Rahman… - Pharmaceutics, 2022 - mdpi.com
Inhibition of PDE5 results in elevation of cGMP leading to vascular relaxation and reduction
in the systemic blood pressure. Therefore, PDE5 inhibitors are used as antihypertensive and …

Ex-vivo antioxidant, enzyme inhibitory properties and computational analysis unveil the molecular mechanism of cardiac and penile phosphodiesterase-5 inhibition by …

HA Oyewusi, OO Oladipo, HF Muritala… - International Journal of …, 2024 - Elsevier
The study uses in-vitro antioxidant, ex-vivo enzyme kinetics and in-silico approach using
standard protocols to understand their inhibitory mechanism better. The study revealed that …

Antiallodynic action of phosphodiesterase inhibitors in a mouse model of peripheral nerve injury

S Megat, S Hugel, SH Journée, Y Bohren, A Lacaud… - …, 2022 - Elsevier
Neuropathic pain arises as a consequence of a lesion or disease affecting the
somatosensory nervous system. It is accompanied by neuronal and non-neuronal …

Diverse pharmacological potential of pyridazine analogs against various diseases

AA Alsaiari, MM Almehmadi, M Asif - Medicinal Chemistry, 2024 - benthamdirect.com
Pyridazinone analogs possess diverse types of pharmacological activities, such as
anticancer, antimicrobial, anticonvulsant, analgesic, anti-inflammatory, antioxidant …