MINI-REVIEWS IN MEDICINAL CHEMISTRY 的目的是发表关于药物化学和相关学科近期重要进展的简短评论。MINI-REVIEWS IN MEDICINAL CHEMISTRY 涵盖药物化学的所有领域，包括药物合理设计、合成化学、生物有机化学的发展, 高通量筛选, 组合化学, 药物靶点, 天然产物研究和构效关系研究。MINI-REVIEWS IN MEDICINAL CHEMISTRY 是每一位希望随时了解最新情况的药物和药物化学家的重要期刊。日期与最新和最重要的发展。

The purpose of Mini-Reviews in Medicinal Chemistry is to publish concise reviews on recent significant advances in medicinal chemistry and related disciplines. This journal covers all areas of medicinal chemistry, including rational drug design, synthetic chemistry, developments in bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, natural product research, and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for researchers who wish to stay updated on the latest and most important developments in the field.

《Mini-Reviews in Medicinal Chemistry》旨在发表关于药物化学及相关学科近期重要进展的简短评论。该期刊涵盖药物化学的各个领域，包括药物合理设计、合成化学、生物有机化学的发展、高通量筛选、组合化学、药物靶点、天然产物研究和构效关系研究。《Mini-Reviews in Medicinal Chemistry》是每位希望及时了解药物和药物化学最新进展的研究者的重要期刊。

Mini-Reviews in Medicinal Chemistry

Abstract: The small-molecular inhibitors targeted JAks (JAK inhibitors), could modulate the cytokines-mediated signaling via JAK-STAT pathway, which plays a important role in immune regulation and cell proliferation. The JAK inhibitors are previously designed and synthesized to treat diseases involved with hematologic and immune system. Increasing evidence shows that they are quite effective in atopic dermatitis (AD), alopecia areata (AA), psoriasis, vitiligo, and other autoimmune-induced dermatologic conditions. Currently, many JAK inhibitors possessing anti-vitiligo activity are being investigated in laboratory and clinically. In this view, we would like to summarize so we review the applications of these inhibitors with emphasis on profile of vitiligo, clinical efficacy, dosages, development of new candidates and adverse events through available literatures.

Chao Niu

Hunjun Xie

Haji Akber Aisa

Janus Kinase Inhibitors: A Review of Their Application in the Vitiligo

Janus激酶抑制剂：其在白癜风中的应用综述

Background: Acetylcholinesterase is a serine hydrolase that terminates the action of the neurotransmitter acetylcholine by hydrolyzing it into acetic acid and choline. Objective: The enzyme, containing an ellipsoidal structure, possesses three binding sites such as active site (with catalytic anionic and esteratic subsites), aromatic gorge and peripheral anionic site, where the inhibiting compounds interact. The acetylcholinesterase inhibitors bind to the enzyme and interfere with the breakdown of acetylcholine, leading to the deposition of acetylcholine in the nerve synapses and causing disrupted neurotransmission. Based on this principle of action, many therapeutic drugs for the treatment of different diseases, pesticides and chemical warfare agents have been synthesized targeting the actylcholinesterase. Conclusion: The present review summarizes the current knowledge about acetylcholinesterase, its structure, function and biosynthesis, its inhibitors, and mode of action of inhibitors on it. Besides, the review also presents an overview about the resistance mechanism that the organisms develop due to the over-application of acetylcholinesterase inhibitors. Keywords: Acetylcholine, acetylcholinesterase, neurotransmission, active sites, acetylcholinesterase inhibitors, insecticide resistance.

Sunita Thapa

Min Lv

Hui Xu

Acetylcholinesterase: A Primary Target for Drugs and Insecticides

乙酰胆碱酯酶：药物和杀虫剂的主要靶点

Matrine, a tetracyclo-quinolizidine alkaloid, is isolated from the industrial crop plant Sophora flavescens. Due to a wide range of pharmacological and agricultural properties, the research on the phytochemistry, pharmacology, toxicology, and mechanisms of action of matrine and its derivatives has received much attention. On the other hand, to improve their biological activities, the study on structural optimizations and structure-activity relationships of matrine and its derivatives has also attached more and more importance. In this review article, the updates regarding the advances in bioactivities, mechanisms of action, structural modifications, and structure-activity relationships of matrine and its derivatives from 2017 to 2020 are presented. We hope that this review will provide a reference for the development and application of matrine and its derivatives as drugs or pesticides in the future.

Jianwei Xu

MRMC

The Advances in Bioactivities, Mechanisms of Action and Structural Optimizations of Matrine and its Derivatives

苦参碱及其衍生物的生物活性、作用机制及结构优化进展

Coumarins are found in higher plants like Rutaceae and Umbelliferae and essential oils of
cinnamon bark, cassia leaf, and lavender oil. Coumarin compounds show different biological properties,
viz antimicrobial, antibacterial, antifungal, antioxidant, antitumor, anti-HIV, antihypertension, anticoagulant,
anticancer, antiviral, anti-inflammatory, analgesics, antidiabetic, anti-depressive, and other bioactive
properties. Coumarin and its derivatives possess anticancer activity against different types of cancers
such as prostate, renal, breast, laryngeal, lung, colon, CNS, leukemia, malignant melanoma. In this review,
current developments of coumarin-based anticancer agents viz simple coumarin, furanocoumarin,
pyranocoumarin, pyrone-substituted coumarin, and their important derivatives have been discussed. The
coumarin-triazole, coumarin-chalcone, coumarin-thiosemicarbazone derivatives, and coumarin-metal
complexes have been found more potent than coumarin. Hence, further study and structural improvement
on coumarin and its derivatives may lead to the design and development of more potent anticancer
agents.

Narayan Bhattarai

Anupa A. Kumbhar

Yuba Raj Pokharel

Paras Nath Yadav

Anticancer Potential of Coumarin and its Derivatives

香豆素及其衍生物的抗癌潜力

Plants produce a vast variety of specialized metabolites which can be a rich source for lead compounds for the development of new drugs. Alkaloids are one the largest groups of plant specialized metabolites important for natural product based pharmaceuticals. Of these, lysine (Lys)-derived alkaloids exhibit a wide range of pharmacological properties which are beneficial for humans. For instance they have anticancer, anti-Alzheimer's disease, anti-inflammatory, hypocholesterolemic and antiarrhtymic effects. Lys-derived alkaloids are widely distributed throughout the plant kingdom: they can be found in various species from clubmosses to flowering plants. Lys is one of the most essential amino acids for humans and livestock and is synthesized in the plastids of land plants. Lys-derived alkaloids can be divided into four major groups including quinolizidine, lycopodium, piperidine, and indolizidine alkaloids. Despite the importance of these compounds, the biosynthetic pathways of Lys-derived alkaloids are not well understood. With the exception of indolizidine alkaloids, Lys decarboxylase (LDC) is the enzyme involved in the first committed step of the biosynthesis by catalyzing the transformation of L-Lys into cadaverine. Cadaverine is then oxidized by copper amine oxidase (CuAO) and spontaneously cyclized to Δ1-piperideine Schiff base which is a universal intermediate for the production of various Lys-derived alkaloids.In this review, we briefly summarize the recent understanding about the structures, occurrences, analytical procedures, biosyntheses, and potential health effects and medical applications of Lys-derived alkaloids with emphasis on quinolizidine alkaloids (QAs).

Somnuk Bunsupa

Mami Yamazaki

Kazuki Saito

Lysine-derived Alkaloids: Overview and Update on Biosynthesis and Medicinal Applications with Emphasis on Quinolizidine Alkaloids

赖氨酸衍生的生物碱：生物合成与药物应用综述及最新进展，重点介绍喹啉生物碱

Margot Paulino Zunini

Meet the Editorial Board Member

认识编辑委员会成员

Carbamate has been extensively used as a scaffold in the recent era of drug discovery and is a common structural motif of many approved drugs. The carbamate moiety's unique amide-ester hybrid (-O-CO-NH-) feature offers the designing of specific drug-target interactions. Despite the discovery of numerous carbamate derivatives that act on the endocannabinoid system (ECS), the development of clinically effective carbamates remains a challenge. In this review, we highlight the therapeutic potential of carbamate inhibitors of endocannabinoid degrading enzymes as a breakthrough in discovering neurotherapeutic drugs. We discuss the design strategies and medicinal chemistry aspects involved in developing carbamate-based molecular architectures that modulate the endocannabinoid signaling pathway by interfering with fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and α/β-Hydrolase domain-containing 6 (ABHD6). Additionally, we highlight the dual activity profile of carbamates against FAAH and MAGL, FAAH and cholinesterase, and FAAH and TRPV1 channels. Furthermore, we illustrate the pharmacophores of O-functionalized carbamates and N-cyclic carbamates that are crucial for FAAH and MAGL inhibitory activities, respectively.

Shivani Jaiswal

Senthil Raja Ayyannan

Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold

具有卡巴姆酯骨架的潜在内源性大麻素降解酶抑制剂

Tiziano Tuccinardi

Meet the Editor-in-Chief

认识主编

Davide Barreca

Preface

前言

Abstract: Sulfated glycosaminoglycans (SGAGs), such as heparin, are complex linear polysaccharides attached to core proteins via covalent bonds to form proteoglycans. SGAGs are crucial in assembling extracellular matrix, the regulation of cell signaling and cell behavior, hemostasis, development, and various diseases, including thrombosis, cancer, infectious diseases, and neurodegenerative disorders, through their binding with diverse proteins. Despite the abundant SGAG-protein interactions provided by nature, the development of small SGAG-like molecules remains underexplored. However, sulfonated penta-galloyl glucose (SPGG) represents a promising, easily synthesized, small-molecule mimetic of SGAGs, capable of harnessing these interactions. This minireview discusses the chemical synthesis and characterization of SPGG, along with its pharmacological effects derived from modulating the SGAG-protein interface.

Rami A. Al-Horani

Sulfonated Penta-Galloyl Glucose (SPGG): The Pharmacological Effects of Promiscuous Glycosaminoglycan Small Molecule Mimetic

磺化五没食子酰葡萄糖（SPGG）：杂乱糖胺聚糖小分子模拟物的药理作用

短名	MRMC
Journal Impact	3.32
国际分区	CHEMISTRY, MEDICINAL(Q2)
期刊索引	SCI Q2中科院 3 区

ISSN	1389-5575, 1875-5607
h-index	107
国内分区	医学(3区)医学药物化学(3区)

涉及主题	生物化学医学生物化学遗传学内科学有机化学药理学物理心理学病理内分泌学核磁共振基因免疫学精神科生物信息学立体化学
出版信息	出版商: Bentham Science Publishers，出版周期: Quarterly，期刊类型: journal，开源期刊: 否
基本数据	创刊年份: 2001，原创研究文献占比: 0.00%，自引率:0.00%， Gold OA占比: 0.00%
平均审稿周期	网友分享经验：平均6.0个月
平均录用比例	网友分享经验：约75%

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