Track topics on Twitter Track topics that are important to you
Modular syntheses of disorazoles A and B analogues in which the epoxide moieties of the natural products were replaced with cyclopropyl units have been achieved. Targeted as part of a structure-activity relationships study, these syntheses were successfully extended to the thiazole counterparts of these analogues. The retrosynthetically defined fragments were assembled through Yamaguchi esterification, Cu/Pd-catalyzed cross-coupling, Yamaguchi macrolactonization, and Cu-catalyzed cross-coupling as the key reactions. Further synthetic and biological investigations of such analogues are expected to lead to the discovery and development of potential payloads for antibody-drug conjugates as targeted cancer therapies.
This article was published in the following journal.
Name: The Journal of organic chemistry
In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogues (11a-d, 12a-d, 16a-c and 17a-d). A bioisosteric replacement approach was adopted to repla...
α-Arylations of cyclopropyl and related nitriles provide access to important synthetic intermediates and pharmacophores for biologically active molecules. However, robust methods for coupling of ster...
Preparation of 2,4,5-trisubstituted thiazole derivatives via a new solid-phase synthetic route has been conducted in this study. The synthetic route begins with synthesis of a core skeleton 2,4-diamin...
In this study, we synthesized 2-amino-5-carboxamide thiazole derivatives on solid phase. The synthesis of the library starts with the reductive amination of the 4-formyl-3-methoxy phenoxy resin in ord...
A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5...
The aim of this study is to elucidate whether GLP-1 analogues influence not only appetite but also thirst perception. It is hypothesized that GLP-1 analogues reduce fluid intake in healthy...
The purpose of this study is to examine the correlation between UGT1A1 genotypes and the safety of CPT-11 plus platinum analogues (cisplatin, carboplatin and nedaplatin) regimens for patie...
This study will evaluate hyperemia and ocular surface tolerability in patients on prostaglandin analogues
This study is to investigate the clinical efficacy of three types of nucleotide/nucleoside analogues in treatment of HBV-related acute-on-chronic liver failure.
The objective of this study is to evaluate, in acromegalic patients with disease persistence after surgery who are treated with somatostatin analogues, the histopathological, clinical, mor...
A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV infection and AIDS.
A white crystalline compound prepared by condensation of benzaldehyde in potassium cyanide and used in organic syntheses. This should not be confused with benzoin gum from STYRAX.
Toluenesulfonyl compounds with general formula CH3C6H4S(O2)R” widely used to block amino groups in the course of syntheses of drugs and other biologically active compounds.
Sulfanilamides consisting of a 4-aminobenzenesulfonamido group at the 2-position of 1,3-thiazole. They are often used as ANTI-INFECTIVE AGENTS.
A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...
An antibody is a protein produced by the body's immune system when it detects harmful substances, called antigens. Examples of antigens include microorganisms (such as bacteria, fungi, parasites, and viruses) and chemicals. Antibodies may be produc...
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...