New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

Molecules, Journal Year: 2022, Volume and Issue: 27(5), P. 1643 - 1643

Published: March 2, 2022

This review describes the recent Food and Drug Administration (FDA)-approved drugs (in year 2021) containing at least one halogen atom (covalently bound). The structures proposed throughout this work are grouped according to their therapeutical use. Their synthesis is presented as well. number of halogenated molecules that reaching market regularly preserved, 14 50 approved by FDA in last contain halogens. underlines emergent role halogens and, particular, fluorine chlorine preparation for treatment several diseases such viral infections, types cancer, cardiovascular disease, multiple sclerosis, migraine inflammatory vasculitis.

Language: Английский

---

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

Chemical Society Reviews, Journal Year: 2024, Volume and Issue: 53(4), P. 2099 - 2210

Published: Jan. 1, 2024

Recent tactical applications of prodrugs as effective tools in drug discovery and development to resolve issues associated with delivery lead candidates are reviewed a reflection the approval 53 during 2012–2022.

Language: Английский

---

The importance of binding kinetics and drug–target residence time in pharmacology

British Journal of Pharmacology, Journal Year: 2023, Volume and Issue: 181(21), P. 4103 - 4116

Published: May 10, 2023

A dominant assumption in pharmacology throughout the 20th century has been that vivo target occupancy—and attendant pharmacodynamics—depends on systemic concentration of drug relative to equilibrium dissociation constant for drug–target complex. In turn, duration pharmacodynamics is temporally linked pharmacokinetics drug. Yet, there are many examples drugs which pharmacodynamic effect endures long after a waned (equilibrium) insignificant levels. To reconcile such data, residence time model was formulated, positing it lifetime (or time) binary complex, and not its affinity per se, determines extent pharmacodynamics. Here, we review this model, evolution over time, applications natural ligand‐macromolecule biology synthetic pharmacology.

Language: Английский

---

A Review of FDA-Approved Anti-HIV-1 Drugs, Anti-Gag Compounds, and Potential Strategies for HIV-1 Eradication

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(7), P. 3659 - 3659

Published: March 25, 2024

Acquired immunodeficiency syndrome (AIDS) is an enormous global health threat stemming from human virus (HIV-1) infection. Up to now, the tremendous advances in combination antiretroviral therapy (cART) have shifted HIV-1 infection a fatal illness into manageable chronic disorder. However, presence of latent reservoirs, multifaceted nature HIV-1, drug resistance, severe off-target effects, poor adherence, and high cost restrict efficacy current cART targeting distinct stages life cycle. Therefore, there unmet need for discovery new therapeutics that not only bypass limitations but also protect body’s at same time. The main goal complete eradication purging latently infected cells patients’ bodies. A potential strategy called “lock-in apoptosis” targets budding phase cycle leads susceptibility apoptosis elimination reservoirs and, ultimately, eradication. work intends present advantages disadvantages United States Food Drug Administration (FDA)-approved anti-HIV-1 drugs as well plausible strategies design development more compounds with better potency, favorable pharmacokinetic profiles, improved safety issues.

Language: Английский

---

DrugFlow: An AI-Driven One-Stop Platform for Innovative Drug Discovery

Journal of Chemical Information and Modeling, Journal Year: 2024, Volume and Issue: 64(14), P. 5381 - 5391

Published: June 26, 2024

Artificial intelligence (AI)-aided drug design has demonstrated unprecedented effects on modern discovery, but there is still an urgent need for user-friendly interfaces that bridge the gap between these sophisticated tools and scientists, particularly those who are less computer savvy. Herein, we present DrugFlow, AI-driven one-stop platform offers a clean, convenient, cloud-based interface to streamline early discovery workflows. By seamlessly integrating range of innovative AI algorithms, covering molecular docking, quantitative structure-activity relationship modeling, generation, ADMET (absorption, distribution, metabolism, excretion toxicity) prediction, virtual screening, DrugFlow can offer effective solutions almost all crucial stages in including hit identification hit/lead optimization. We hope provide sufficiently valuable guidance aid real-word discovery. The available at https://drugflow.com.

Language: Английский

---

Fluorine in the pharmaceutical industry: Synthetic approaches and application of clinically approved fluorine-enriched anti-infectious medications

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 271, P. 116446 - 116446

Published: April 26, 2024

Language: Английский

---

Discovery of Noncovalent Diaminopyrimidine-based Inhibitors for Glioblastoma via a Dual FAK/DNA Targeting Strategy

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 286, P. 117288 - 117288

Published: Jan. 16, 2025

Language: Английский

---

Quinolines and isoquinolines as HIV-1 inhibitors: Chemical structures, action targets, and biological activities

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 136, P. 106549 - 106549

Published: April 20, 2023

Language: Английский

---

Fluorine in anti-HIV drugs approved by FDA from 1981 to 2023

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 258, P. 115586 - 115586

Published: June 28, 2023

Language: Английский

---

A Review on FDA Approved Anti-HIV-1 Drugs, Anti-Gag Compounds and Potential Strategies for HIV-1 Eradication

Published: Jan. 18, 2024

Acquired immunodeficiency syndrome (AIDS) is an enormous global health threat stemming from human virus (HIV-1) infection. Up to now, the tremendous advances in combination antiretroviral therapy (cART) have shifted HIV-1 infection a fatal illness into manageable chronic disorder. However, presence of latent reservoirs, multifaceted nature HIV-1, drug resistance, severe off-target effects, poor adherence, and high cost restrict efficacy current cART targeting distinct stages life cycle. Therefore, there unmet need for discovery new therapeutics that not only bypass limitations but also protect body at same time. The main goal complete eradication purging latently infected cells patients’ bodies. A potential strategy called “lock-in apoptosis” budding phase cycle leading susceptibility apoptosis elimination reservoirs ultimately eradication. work intends present advantages disadvantages United States Food Drug Administration (FDA) approved anti-HIV-1 drugs as well plausible strategies design development more compounds with better potency, favorable pharmacokinetic profiles, improved safety issues.

Language: Английский

---