Tag: M.W=150-200

Wu, Shixin published the artcileTestis transcriptome profiling identified genes involved in spermatogenic arrest of cattleyak, Product Details of C7H5ClN2S, the publication is PLoS One (2020), 15(2), e0229503, database is CAplus and MEDLINE.

Much attempt has been made to examine the mechanisms of male sterility caused by spermatogenic arrest, but yet there is no research systematically and precisely elucidated testis gene expression profiling between cattleyak and yak. Methods: To explore the higher resolution comparative transcriptome map between the testes of yak and cattleyak, and further analyze the mRNA expression dynamics of spermatogenic arrest in cattleyak. We characterized the comparative transcriptome profile from the testes of yak and cattleyak using high-throughput sequencing. Then we used quant. anal. to validate several differentially expressed genes (DEGs) in testicular tissue and spermatogenic cells. Results: Testis transcriptome profiling identified 6477 DEGs (2919 upregulated and 3558 downregulated) between cattleyak and yak. Further anal. revealed that the marker genes and apoptosis regulatory genes for undifferentiated spermatogonia were upregulated, while the genes for differentiation maintenance were downregulated in cattleyak. A majority of DEGs associated with mitotic checkpoint, and cell cycle progression were downregulated in cattleyak during spermatogonial mitosis. Furthermore, almost all DEGs related to synaptonemal complex assembly, and meiotic progression presented no sign of expression in cattleyak. Even worse, dozens of genes involved in acrosome formation, and flagellar development were dominantly downregulated in cattleyak.

PLoS One published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C30H42NOP, Product Details of C7H5ClN2S.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Tomasic, Tihomir published the artcileDesign, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors, Application of Methyl 2-(2-aminothiazol-4-yl)acetate, the publication is Bioorganic & Medicinal Chemistry (2017), 25(1), 338-349, database is CAplus and MEDLINE.

Two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety was designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC₅₀ values between 0.891 and 10.4 μM). Their “ring-opened” analogs, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC₅₀ values between 15.9 and 169 μM. Mol. docking experiments were conducted to study the binding modes of inhibitors.

Bioorganic & Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C13H15NO6S, Application of Methyl 2-(2-aminothiazol-4-yl)acetate.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Muri, E. M. F. published the artcileMolecular modeling, synthesis and biological evaluation of heterocyclic hydroxamic acids designed as Helicobacter pylori urease inhibitors, Computed Properties of 64987-16-2, the publication is Letters in Drug Design & Discovery (2004), 1(1), 30-34, database is CAplus.

A computer-generated homol. model of the antimicrobial target Helicobacter pylori urease was derived, using the x-ray crystal structure of Klebsiella aerogenes as a template, in order to design novel urease inhibitors. Based on these computational studies, several heterocyclic hydroxamic acid derivatives have been designed, synthesized, and examined for their ability to inhibit urease activity.

Letters in Drug Design & Discovery published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Computed Properties of 64987-16-2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Muri, Estela Maris F. published the artcileDesign and synthesis of heterocyclic hydroxamic acid derivatives as inhibitors of Helicobacter pylori urease, Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate, the publication is Synthetic Communications (2003), 33(12), 1977-1995, database is CAplus.

Helicobacter pylori produces ammonia to help counter the acidic environment in the human stomach. The production of ammonia, essential for the microorganism’s survival and virulence, is the product of enzymic conversion of urea by the H. pylori’s urease. Inhibition of urease activity by dipeptide hydroxamic acids has previously been demonstrated using a variety of fluorides, thiols and hydroxamic acids. Studies employing computer-aided drug design techniques have been utilized to suggest a novel series of heterocyclic hydroxamic acid derivatives as potential urease inhibitors. Heterocyclic compounds such as I, II, III, and IV have been designed, synthesized, and preliminarily tested as dipeptide mimics which offer a structure that is more biol. stable than that of the reported dipeptide inhibitors.

Synthetic Communications published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ahdenov, Reza published the artcileEelectrosynthesis of benzothiazole derivatives via C-H thiolation, Computed Properties of 95-24-9, the publication is Heterocyclic Communications (2022), 28(1), 67-74, database is CAplus.

Benzothiazole derivatives are essential intermediates in synthesizing a wide variety of medical and pharmaceutical compounds, and there is a great demand for a simple and efficient method to synthesize benzothiazoles under mild reaction conditions. Organic electrosynthesis as an energy-efficient process represents an environmentally benign and safer method than traditional methods for organic synthesis. Herein, authors present bromine-free and straightforward synthesis of 2-amino benzothiazole derivatives via the reaction of aniline derivatives and ammonium thiocyanate using electrosynthesis in the presence of sodium bromide both as an electrolyte and as a brominating agent at room temperature in iso-Pr alc. (i-PrOH) as a solvent. The reaction of ammonium thiocyanate via C-H thiolation routes, using various aniline derivatives, resulted in a simple, green, and bromine-free synthesis of 2-amino benzothiazole in moderate to good yields under mild reaction conditions. Riluzole drug can be produced using the same procedure in moderate yields.

Heterocyclic Communications published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Computed Properties of 95-24-9.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Kar, Soumya Ranjan published the artcileGreen synthesis, characterization and antibacterial activity studies of new multifunctional nano polymeric material, which may have multidimensional application in water purification, Category: thiazole, the publication is Polymer Bulletin (Heidelberg, Germany), database is CAplus.

A novel polymeric resin was synthesized by condensing a Schiff base of 6-chloro-2-aminobenzothiazole and salicyldehyde with formaldehyde, which may have multidimensional application. First step of the synthesis of novel polymeric material is synthesis of Schiff base, which is the monomer of the resin. The Schiff base was synthesize by using greener method to reduce hazardous chem. waste and reaction time, so that reduction of environmental pollution and conservation of energy can be achieved. The greener method is compared with the conventional method. The metal polychelates of the polymeric resin with Cu²⁺ and Fe³⁺ were synthesized. The Schiff base, resin and its polychelates were converted to nanodimension and its dimension is measured by DLS method. The structure of the Schiff base, resin and polychelates are ascertained by FTIR, ¹H NMR spectroscopy. The exptl. data are compared with the computational data obtained from Gaussian software to ascertain the synthesis of these materials. These materials have a very wide range of application starting from anal. chem. to biochem. The antibacterial activities of Schiff base, resin and metal polychelates were studied against pathogenic bacteria Escherichia coli by turbidity measurement method. All these materials are found to be effective against the tested bacterial species, whereas the polychelates are shown exceptional results.

Polymer Bulletin (Heidelberg, Germany) published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Category: thiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Dong, Miao published the artcileSynergistic effect of copolymeric resin grafted 1,2-benzisothiazol-3(2H)-one and heterocyclic groups as a marine antifouling coating, COA of Formula: C7H5ClN2S, the publication is RSC Advances (2021), 11(31), 18787-18796, database is CAplus and MEDLINE.

In order to find a new type of antifouling coating with higher biol. activity and more environmental protection, heterocyclic compounds and benzoisothiazolinone were introduced into acrylic resin to prepare a new type of antifouling resin. In this study, a series of grafted acrylic resins simultaneously containing benzoisothiazolinone and heterocyclic monomers were prepared by the copolymerization of an allyl monomer with Me methacrylate (MMA) and Bu acrylate (BA). Inhibitory activities of the copolymers against marine fouling organisms were also investigated. Results revealed that the copolymers exhibit a clear synergistic inhibitory effect on the growth of three seaweeds: Chlorella, Isochrysis galbana and Chaetoceros curvisetus, resp., and three bacteria, Staphylococcus aureus, Vibrio coralliilyticus and Vibrio parahaemolyticus, resp. In addition, the copolymers exhibited excellent inhibition against barnacle larvae. Marine field tests indicated that the resins exhibit outstanding antifouling potency against marine fouling organisms. Moreover, the introduction of the heterocyclic group led to the significantly enhanced antifouling activities of the resins; the addition of the heterocyclic unit in copolymers led to better inhibition than that observed in the case of the resin copolymerized with only the benzoisothiazolinone active monomer.

RSC Advances published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, COA of Formula: C7H5ClN2S.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Ke, Chaoqi published the artcileOrganocatalytic asymmetric synthesis of benzothiazolopyrimidines via a [4+2] cycloaddition of azlactones with 2-benzothiazolimines, Formula: C7H5ClN2S, the publication is Organic Chemistry Frontiers (2021), 8(20), 5705-5709, database is CAplus.

An easily available L-proline-derived guanidine-amide were found to be efficient at catalyzing a [4+2] cycloaddition of azlactones with 2-benzothiazolimines by affording various benzothiazolopyrimidines bearing adjacent tertiary and quaternary stereogenic centers in excellent yields at 2 mol% loading. The diastereoisomers of the main adducts differed from those in a previous bifunctional organocatalytic system.

Organic Chemistry Frontiers published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Formula: C7H5ClN2S.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Laghezza, Antonio published the artcileVirtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors, Category: thiazole, the publication is Bioorganic & Medicinal Chemistry (2020), 28(3), 115257, database is CAplus and MEDLINE.

Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor progression and invasiveness. This encouraged over the years the approach of MMP, and particularly MMP-2, targeting for anticancer treatment. Early generations of MMP inhibitors, based on aspecific zinc binding groups (ZBGs) assembled on (pseudo)peptide scaffolds, have been discontinued due to the clin. emergence of toxicity and further drawbacks, giving the way to inhibitors with alternative zinc-chelator moieties or not binding the catalytic zinc ion. In the present paper, we continue the search for new non-zinc binding MMP-2 inhibitors: exploiting previously identified compounds, a virtual screening (VS) campaign was carried out and led to the identification of a new class of ligands. The structure-activity relationship (SAR) of the benzimidazole scaffold was explored by synthesis of several analogs whose inhibition activity was tested with enzyme inhibition assays. By performing the mol. simplification approach, we disclosed different sets of single-digit micromolar inhibitors of MMP-2, with up to a ten-fold increase in inhibitory activity and ameliorated selectivity towards off-target MMP-8, compared to selected lead compound Mol. dynamics calculations conducted on complexes of MMP-2 with docked privileged structures confirmed that analyzed inhibitors avoid targeting the zinc ion and dip inside the S1′ pocket. Present results provide a further enrichment of our insights for the design of novel MMP-2 selective inhibitors.

Bioorganic & Medicinal Chemistry published new progress about 95-24-9. 95-24-9 belongs to thiazole, auxiliary class Organic Pigment, name is 6-Chlorobenzothiazol-2-ylamine, and the molecular formula is C7H5ClN2S, Category: thiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Prier, Christopher K. published the artcileAmine α-heteroarylation via photoredox catalysis: a homolytic aromatic substitution pathway, Category: thiazole, the publication is Chemical Science (2014), 5(11), 4173-4178, database is CAplus and MEDLINE.

The direct α-heteroarylation of tertiary amines has been accomplished via photoredox catalysis to generate valuable benzylic amine pharmacophores. A variety of five- and six-membered chloroheteroarenes are shown to function as viable coupling partners for the α-arylation of a diverse range of cyclic and acyclic amines. Evidence is provided for a homolytic aromatic substitution mechanism, in which a catalytically-generated α-amino radical undergoes direct addition to an electrophilic chloroarene.

Chemical Science published new progress about 329794-40-3. 329794-40-3 belongs to thiazole, auxiliary class Thiazole,Chloride,Benzene, name is 2-Chloro-5-phenylthiazole, and the molecular formula is C9H6ClNS, Category: thiazole.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica