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CDD-2807
CDD-2807 is a chemical compound which acts as a potent and selective inhibitor of serine/threonine-protein kinase 33 ( STK33), with a IC50 of 9.2 nM. In animal studies it causes production of abnormal sperm with reduced motility, and it has been investigated as a potential male contraceptive drug. See also * JQ1 * TDI-11861 * YCT529 YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clini ... References {{pharm-stub Indazoles Biphenyls Carboxamides Azetidines Piperidines Spiro compounds Ethynyl compounds Nitrogen heterocycles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TDI-11861
TDI-11861 is a chemical compound which acts as a potent and selective inhibitor of soluble adenylyl cyclase (sAC). In animal studies it reversibly inhibits sperm motility, producing temporary infertility without hormonal side effects. While TDI-11861 is at an early developmental stage and is unlikely to be developed for medical uses in humans itself, it represents an important proof of concept which may potentially lead to the development of future male contraceptive drugs. See also * CDD-2807 * JQ1 * YCT529 YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clini ... References {{pharm-stub Chloroarenes Pyrimidines Morpholines Pyrazoles Difluoromethyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
YCT529
YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clinical trials as a potential male contraceptive. The Vitamin A signalling system plays a number of important roles in bodily systems, such as the Immune system “It seems to me inherently unlikely that a compound with such activity would be free of side effects,” says Richard Sharpe, of the University of Edinburgh. See also * Adjudin * CDD-2807 * Dimethandrolone undecanoate * JQ1 JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals. BET inhibitors structurally similar to JQ1 are being tested in ... * TDI-11861 References {{reflist Contraception for males Experimental methods of birth control Pyr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serine/threonine-specific Protein Kinase
A serine/threonine protein kinase () is a kinase enzyme, in particular a protein kinase, that phosphorylates the OH group of the amino-acid residues serine or threonine, which have similar side chains. At least 350 of the 500+ human protein kinases are serine/threonine kinases (STK). In enzymology, the term ''serine/threonine protein kinase'' describes a class of enzymes in the family of transferases, that transfer phosphates to the oxygen atom of a serine or threonine side chain in proteins. This process is called phosphorylation. Protein phosphorylation in particular plays a significant role in a wide range of cellular processes and is a very important posttranslational modification. The chemical reaction performed by these enzymes can be written as :ATP + a protein \rightleftharpoons ADP + a phosphoprotein Thus, the two substrates of this enzyme are ATP and a protein, whereas its two products are ADP and phosphoprotein. The systematic name of this enzyme class is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Male Contraceptive
Male contraceptives, also known as male birth control, are methods of preventing pregnancy that solely involve the male physiology. The most common kinds of male contraception include condoms, outercourse, and vasectomy. In domestic animals, castration is commonly used for contraception. Other forms of male contraception are in various stages of research and development. These include methods like RISUG/VasalGel (which has completed a small phase II clinical trial in humans in India) and ultrasound (with results so far obtained in experimental animals). Methods Surgery Vasectomy is a surgical procedure for male sterilization or permanent birth control. During the procedure, the vasa deferentia of a man are severed, and then tied or sealed to prevent sperm from entering into the seminal stream (ejaculate). Vasectomies are usually performed in a physician's office or medical clinic. CDC research has estimated there is a probability of 11 failures per 1,000 procedures over 2 years ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indazoles
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an Amphoterism, amphoteric molecule which can be protonated to an indazolium cation or deprotonated to an indazolate anion. The corresponding ''pKa'' values are 1.04 for the equilibrium between indazolium cation and indazole and 13.86 for the equilibrium between indazole and indazolate anion. Indazole derivatives display a broad variety of biological activities. Indazoles are rare in nature. The alkaloids nigellicine, nigeglanine, and nigellidine are indazoles. Nigellicine was isolated from the widely distributed plant ''Nigella sativa'' L. (black cumin). Nigeglanine was isolated from extracts of ''Nigella glandulifera''. The Davis–Beirut reaction can generate 2''H''-indazoles. Indazole, C7H6N2, was obtained by E. Fischer (''Ann.'' 1883, 221, p. 280) by heating ortho-hydrazine cinnamic acid, : Some derivatives ; i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azetidines
Azetidine is a saturated heterocyclic organic compound containing three carbon atoms and one nitrogen atom. It is a liquid at room temperature with a strong odor of ammonia and is strongly basic compared to most secondary amines. Synthesis and occurrence Azetidines can be prepared by reduction of azetidinones (β-lactams) with lithium aluminium hydride. Even more effective is a mixture of lithium aluminium hydride and aluminium trichloride, a source of "AlClH2" and "AlCl2H". Azetidine can also be produced by a multistep route from 3-amino-1-propanol. Regio- and diastereoselective synthesis of 2-arylazetidines could be performed from appropriately substituted oxiranes via ring transformation. It is controlled by Baldwin's Rules with remarkable functional group tolerance. Azetidine and its derivatives are relatively rare structural motifs in natural products. They are a component of mugineic acids and penaresidins. Perhaps the most abundant azetidine containing natural product ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, and typical of amines. The name comes from the genus name ''Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be reduce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiro Compounds
In organic chemistry, spiro compounds are compounds that have at least two molecular rings with only one common atom. The simplest spiro compounds are bicyclic (having just two rings), or have a bicyclic portion as part of the larger ring system, in either case with the two rings connected through the defining single common atom. The one common atom connecting the participating rings distinguishes spiro compounds from other bicyclics: from ''isolated ring compounds'' like biphenyl that have no connecting atoms, from ''fused ring compounds'' like decalin having two rings linked by two adjacent atoms, and from ''bridged ring compounds'' like norbornane with two rings linked by two non-adjacent atoms.For all four categories, see The specific chapters can be found aan respectively, same access date. For the description featuring adjacent atoms for all but the isolated category, see Clayden, op. cit. Spiro compounds may be fully carbocyclic (all carbon) or heterocyclic (havi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethynyl Compounds
In organic chemistry, the term ethynyl designates a functional group with a double bond with 2 carbon atoms both with sp hybridisation and a triple bond(1 sigma and 2 pi bond) . It is a species similar to acetylene (or in IUPAC ethyne ) with a less H atom thus joined to root chain. * An ethynyl group (HC≡C–), also designated as acetylenic group (from acetylene), and referred to in IUPAC chemical nomenclature as -yne suffix. Also sometimes designed as ''ethinyl'' in compounds (ethinylestradiol, ethisterone (ethinyltestosterone)). See main page alkynes. * The ethynyl radical (HC≡C·), the compound found in interstellar medium, and transiently on earth during chemical reactions. * The ethynyl carbanion Acetylide (HC≡C−) See also * Ethynylation * Propynyl In organic chemistry, a propynyl group is a propyl In organic chemistry, propyl is a three-carbon alkyl substituent with chemical formula for the linear form. This substituent form is obtained by removing one ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
