substituted

Substituted piperidines-1 can promote the release of growth hormone in humans and animals.

SD-254 is a deuterium analog of Effexor, with fewer side effects and a longer half-life.

SU16f (3-substituted indolin-2-one 16f) is a potent and selective PDGFRβ inhibitor (IC50s: 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively). Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs conditioned medium in gastric cancer cell proliferation and migration.

Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2).

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

RV01 is a novel quinoline-substituted analogue of resveratrol that inhibits DNA damage, reduces ethanol-induced acetaldehyde dehydrogenase (ALDH2) mRNA expression, and has hydroxyl radical scavenging activity. rV01 reduces iNOS expression and has anti-neuroinflammatory effects. rV01 reduces tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion. RV01 reduced tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion, inhibited lps-induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation, decreased toll-like receptor 4 (TLR4) protein expression, and inhibited lps-induced activation of mitogen-activated protein kinase (MAPK) and nuclear transcription factor-кB (NF-кB) signaling pathways.

2-Chloronaphthoquinone (2-Chloro-1,4-naphthoquinone) is a substituted naphthoquinone which is used as an insecticide and acaricide.

Clanfenur belongs to a new group of substituted benzoylphenylureas. The drug shows both in vitro and in vivo antitumour activity.

Verofylline (Verofyllinum) is an orally available, long-acting, multiacting, methylxanthine-substituted bronchodilator with inhibitory effects on PDE4 for the treatment of asthma disease research obesity.

1-Ethyl-6-aminouracil (6-AMINO-1-ETHYL-1H-PYRIMIDINE-2,4-DIONE) is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosine A2B receptors.

Ensaculin (Anseculin), a novel benzopyrone partially substituted with piperazine, showed memory-enhancing effects in passive and conditioned avoidance paradigms in normal and artificially amnesic rodents. It showed neuroprotective activity in a model of NMDA toxicity and neurotrophic effects in primary cultured rat brain cells.Ensaculin can be used for the treatment of dementia.

I-37 free base is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.

I-49 free base (Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-6-(tetrahydro-2H-pyran-4-yl)-) is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.

Antidepressant agent 5 is a 7-substituted tetrahydroisoquinoline derivative with antidepressant activity.Antidepressant agent 5 acts similarly to magnoflorine in the study of depression and can be used for the prevention and treatment of depressive disorders.

4-(9H-fluoren-9-ylmethoxycarbonylamino)-piperidine-1,4-dicarboxylic acid mono-tert-butyl ester is a substituted piperidine derivative widely used in organic synthesis as a linker to form peptide and peptidomimetic molecules, and is widely used in peptide synthesis and peptide mimicry, as well as in the synthesis of pharmaceuticals, biopolymers and other organic molecules.

R 61837 is a novel rhinovirus inhibitor, a substituted phenylpyridazinamine, with antiviral activity.

(±)-Lisofylline is an enantiomer-specific, alkyl-substituted methylxanthine, which has specific and potent activity in down-regulating leukocyte activation. (±)-Lisofylline is an anti-inflammatory agent.

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene used topically as an antiseptic for the treatment of minor skin infections.

Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.

Midecamycin (Medecamycin A1), an acetoxy-substituted macrolide antibiotic, has effective on gram-positive and gram-negative bacteria acts by inhibiting bacterial protein synthesis.

COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis.

(R)-Lansoprazole (T 168390) is the R-isomer of lansoprazole and a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity.Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

2,3,4,5-Tetrachlorophenol is a metabolite of the insecticide γ-lindane.1It is toxic to fathead minnows and rainbow trout (LC50s = 0.496 and 0.304 mg/L, respectively, in tank water).2 1.Chadwick, R.W., and Freal, J.J.The identification of five unreported lindane metabolites recovered from rat urineBull. Environ. Contam. Toxicol.7(2)137-146(1972) 2.Holcombe, G.W., Phipps, G.L., Knuth, L., et al.The acute toxicity of selected substituted phenols, benzenes and benzoic acid esters to fathead minnows Pimephales promelasEnviron. Pollut.35(4)367-381(1984)

A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma. Of these, the unsubstituted or meta-substituted aromatic derivatives are the most potent FP receptor agonists. 17-trifluoromethylphenyl trinor PGF2α bears an aromatic ring which is reminiscent of the trifluoromethyl-phenoxy ring of travoprost ((+)-fluprostenol isopropyl ester). As an ocular hypotensive agent, it would be expected that 17-trifluoromethylphenyl trinor PGF2α would act very much like the free acid of travoprost. 17-phenyl trinor PGF2α is a potent luteolytic and abortifacient, with a potency equal to or greater than fluprostenol and cloprostenol.

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

2,3-Indolobetulinic glycine amide is a pentacyclic triterpene and derivative of betulinic acid .1It has been used in the synthesis of betulinic acid derivatives with anticancer activity. 1.Kumar, V., Rani, N., Aggarwal, P., et al.Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivativesBioorg. Med. Chem. Lett.18(18)5058-5062(2008)

KSD 2405 (3-Hydroxybenzyl alcohol) is a hydroxybenzyl alcohol that is phenol substituted at position C-3 by a hydroxymethyl group. It is a pink or beige to brown crystalline powder, soluble in water.

3-Amino-4-methylpentanoic acid (DL-Homovaline) is a beta-amino acid that is pentanoic acid substituted at positions 3 and 4 by amino and methyl groups respectively. It has a role as a human metabolite.

Aureothin is a natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities. It is a non-competitive inhibitor of NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC50s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

Bromacil, a substituted uracil herbicide used worldwide, is not readily biodegradable and therefore has consequences to the environment.

Diethyl oxalpropionate (HYL 2-METHYL-3-OXOSUCCINATE), also known as methyloxalacetic acid diethyl ester or diethyl methyloxalacetate, is a member of the class of compounds known as beta-keto acids and derivatives. These compounds are organic compounds containing an aldehyde substituted with a keto group on the C3 carbon atom. Diethyl oxalpropionate is slightly soluble (in water) and a very weakly acidic compound (based on its pKa). Within the cell, diethyl oxalpropionate is primarily located in the cytoplasm.

The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 μM compared to 20 μM by resveratrol.

rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)

Compound 10w, a substituted pyrazolo[1,5-a]pyrimidinamide compound, is a ZSTK474 analog that shows anticancer activity against HeLa cells.

SP-346 nonapeptide is a pipecolic acid substituted nonapeptide.

Methyl 3-aminopyrazine-2-carboxylate is a pyrazine that is substituted by a methoxycarbonyl group at position 2 and an amino group at position 3. It is a member of pyrazines, a methyl ester and an aromatic amine. Methyl 3-aminopyrazine-2-carboxylate could

Lenacil (634 Hexilure) is an agent of herbicide.Lenacil can inhibit photosynthesis.

N-(4-Chlorophenyl)-3-(4-oxo-5-(thiophen-2-ylmethylene)-2-thioxothiazolidin-3-yl)propanamide is an active chemical compound characterized by its complex structure, featuring a central thiazolidine ring substituted with a thiophene group, a 4-chlorophenyl group, and a propanamide side chain. This compound engages in various chemical reactions due to its active functional groups.

alpha-Methylcinnamaldehyde is an α-substituted derivative of Cinnamaldehyde, which can be used as an inhibitor of mushroom tyrosinase.

N-3-oxo-hexadecanoyl-L-Homoserine lactone is an unusual, substituted, long-chain N-acyl-homoserine lactone (AHL) produced by some bacteria, including strains of Agrobacterium vitis and Pseudomonas. Like other AHLs, this C16-containing form is thought to be involved in quorum sensing. Substituted, long-chain AHLs, including N-3-oxo-tetradecanoyl-L-homoserine lactone , prime for systemic acquired resistance to pathogen attack in plants.

BChE-IN-19 (Compound 7b), a para-substituted indone derivative, exhibits potent inhibitory activity against butyryl cholinesterase (BChE) with an IC50 value of 0.04 μM. It enhances cholinergic neurotransmission and has potential therapeutic application in Alzheimer's disease [1].

RU 45196 is an 11 beta-substituted 19-norsteroid of the estra-4,10-diene series.

6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

A series of a hydroxy substituted derivatives 21-28 at C-17 of the Picraline-type alkaloids have been derived as having potent SGLT inhibitory activity.

RS 49676 is an N-substituted imidazole.

ML 23 is a melatonin analogue in the treatment and management of Parkinson's disease. ML-23 is a potential clinical candidate for the treatment of PD, and the present study has been undertaken to determine the efficacy of ML-23 in the 1-methyl-4-phenyl, 1

Kaurenoic acid (kaurenoate) has anti-inflammatory potential in acetic acid-induced colitis, decreases in MDA level. Kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of ATP-sensitive potassium channels. Kaurenoic acid exhibits an analgesic effect in a consistent manner and that its mechanisms involve the inhibition of cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. Kaurenoic acid derivatives have an antimicrobial activity of substituted on carbon-15 at concentrations greater than or equal to 250 μg/ml. Kaurenoic acid has inhibitory effects on the LPS-induced inflammatory response in RAW264.7 macrophages.

p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor. Drug Metab.Dispos. 35 875 PMID:17344341

S-Methylglutathione (S-Methyl glutathione) is an S-substituted glutathione, an inhibitor of the 1-chloro-2,4-dinitrobenzene coupling catalyzed by transferase A and an XOCl scavenger.S-Methylglutathione inhibits glyoxalase 1 (glyoxalase 1), which induces the development of the glyoxalase 1 enzyme. S-Methylglutathione inhibits glyoxalase 1 (glyoxalase 1) and induces the formation of hydroid tentacle balls.

(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10;11(7):1463-1469.