Month: December 2022

Timari, Geza published the artcileSynthesis of novel ellipticine analogs and their inhibition of Moloney leukemia reverse transcriptase, Product Details of C11H16BNO3, the publication is Bioorganic & Medicinal Chemistry Letters (1996), 6(23), 2831-2836, database is CAplus.

Two new ellipticine analogs I [R = H, Cl] were synthesized as potential non-nucleoside inhibitors of reverse transcriptase and were tested on Moloney leukemia virus reverse transcriptase in vitro. Both I showed considerable inhibitory effect with ID₅₀ of 2.8 to 4.5 × 10^-5 M.

Bioorganic & Medicinal Chemistry Letters published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C7H8BBrO3, Product Details of C11H16BNO3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Timari, Geza published the artcileA convenient synthesis of two new indoloquinoline alkaloids, HPLC of Formula: 146140-95-6, the publication is Synlett (1997), 1067-1068, database is CAplus.

A concise synthesis of cryptosanguinolentine and cryptotackieine (neocryptolepine), isolated from Cryptolepis sanguinolenta is reported. The Pd-catalyzed cross-coupling reaction of 3-bromoquinoline or 3-bromo-N-methyl-2-quinolinone with 2-(pivaloylamino)phenylboronate gave the corresponding biaryls from which the indoloquinolines could be synthesized.

Synlett published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C7H8BBrO2, HPLC of Formula: 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhang, Yu published the artcileFacile and scalable synthesis of topologically nanoengineered polypeptides with excellent antimicrobial activities, Formula: C11H22N2O4, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(3), 356-359, database is CAplus and MEDLINE.

A facile and scalable strategy for the quick library synthesis of linear-, hinged-, star-, and cyclic-polypeptides with broad-spectrum antimicrobial activity has been reported. The topol. nanoengineered polypeptides show superior antimicrobial activity against Gram-pos. and Gram-neg. bacteria and low toxicity, allowing screening of architectural polypeptides as mimics of host defense peptides for antimicrobials.

Chemical Communications (Cambridge, United Kingdom) published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C5H5NO3S, Formula: C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhang, Zhichao published the artcileNovel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach, HPLC of Formula: 15029-36-4, the publication is European Journal of Medicinal Chemistry (2013), 141-149, database is CAplus and MEDLINE.

Based on a known nanomolar Bcl-2 homol. domain 3 (BH3) mimetic 3-thiomorpholin-8-oxo-8H-acenaphtho[1,2-b] pyrrole-9-carbonitrile (I, MW: 331), we applied a fragment-based approach to obtain BH3 mimetics with improved affinity and improved solubility in a water-ethanol (9:1) cosolvent. After the deconstruction of I, we obtained fragment cyanoacetamide (II), which was determined to be a ligand efficiency (LE) hot part. After a rational optimization through fragment evolution beginning with fragment II, a smaller Mcl-1 inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (III, MW: 288) with a 6-fold increase in affinity compared to I was obtained, as predicted by our optimization curve and identified by Mcl-1 protein NMR (NMR).

European Journal of Medicinal Chemistry published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C9H7NO2, HPLC of Formula: 15029-36-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Peng, Yanqing published the artcileAmides by microwave-assisted dehydration of ammonium salts of carboxylic acids, Synthetic Route of 2447-79-2, the publication is Organic Preparations and Procedures International (2002), 34(1), 95-97, database is CAplus.

A direct and rapid procedure for the preparation of primary amides from ammonium salts of carboxylic acids in formamide under microwave irradiation is presented. Different types of carboxylic acids were converted to their corresponding amides by this procedure with satisfactory yields. The ammonium salts of carboxylic acids were formed in situ from ammonium bicarbonate and corresponding carboxylic acids. Formamide was suitable for this procedure both as a solvent and a dehydrating agent. This procedure compares favorably to other classical methods and it has the advantages of simple work-up, short reaction time, and the use of inexpensive and readily available reagents.

Organic Preparations and Procedures International published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Synthetic Route of 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Aksinenko, A. Yu. published the artcileModification of phenothiazine and carbazole derivatives with trifluoromethyl-containing 1,3,5-oxadiazines and imidazolidinediones, Formula: C2H4ClNO, the publication is Russian Chemical Bulletin (2021), 70(11), 2180-2184, database is CAplus.

Modification of phenothiazine and carbazole derivatives with trifluoromethyl-containing 1,3,5-oxadiazines and imidazolidinediones based on the copper(I)-catalyzed alkyne-azide 1,3-cycloaddition was carried out.

Russian Chemical Bulletin published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Formula: C2H4ClNO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Secatto, Adriana published the artcileThe leukotriene B4/BLT1 axis is a key determinant in susceptibility and resistance to histoplasmosis, Application In Synthesis of 321673-30-7, the publication is PLoS One (2014), 9(1), e85083/1-e85083/9, 9 pp., database is CAplus and MEDLINE.

The bioactive lipid mediator leukotriene B4(LTB4) greatly enhances phagocyte antimicrobial functions against a myriad of pathogens. In murine histoplasmosis, inhibition of the LT-generating enzyme 5-lipoxygenase (5-LO) increases the susceptibility of the host to infection. In this study, we investigated whether murine resistance or susceptibility to Histoplasma capsulatum infection is associated with leukotriene production and an enhancement of in vivo and/or in vitro antimicrobial effector function. We show that susceptible C57BL/6 mice exhibit a higher fungal burden in the lung and spleen, increased mortality, lower expression levels of 5-LO and leukotriene B4 receptor 1 (BLT1) and decreased LTB4 production compared to the resistant 129/Sv mice. Moreover, we demonstrate that endogenous and exogenous LTs are required for the optimal phagocytosis of H. capsulatum by macrophages from both murine strains, although C57BL/6 macrophages are more sensitive to the effects of LTB4 than 129/Sv macrophages. Therefore, our results provide novel evidence that LTB4 production and BLT1 signaling are required for a histoplasmosis-resistant phenotype.

PLoS One published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C5H11NO2S, Application In Synthesis of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhao, Yigang published the artcileC-H Activation by Amide Chelation Control: Ruthenium-Catalyzed Direct Synthesis of 2-Aryl-3-furanamides, Formula: C10H14N2O, the publication is Advanced Synthesis & Catalysis (2014), 356(7), 1527-1532, database is CAplus.

A new, catalytic methodol. for the synthesis of heterobiaryls by the ruthenium-catalyzed C-H activation/cross-coupling of heterocyclic amides with 2-aryl-1,3,2-dioxaborinanes is surveyed. From this survey, the highly regioselective reaction of furan-3-carboxamide to give 2-aryl-3-furanamides is optimized and generalized in scope with respect to the 2-aryl-1,3,2-dioxaborinane partners. E.g., in presence of RuH₂(CO)(PPh₃)₃ in toluene, reaction of N,N-diethylfuran-3-carboxamide with 2-aryl-1,3,2-dioxaborinane derivative (I) gave 92% heterobiaryl (II). Established thereby is a one-step synthetic method which may supercede the broadly applied two-step directed ortho metalation (DoM)-cross coupling reaction involving cryogenic and strong base conditions and which has potential for further ortho and remote metalation chem.

Advanced Synthesis & Catalysis published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C11H10N4, Formula: C10H14N2O.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Watanabe, M. published the artcileTandem directed metalation reactions. Short syntheses of polycyclic aromatic hydrocarbons and ellipticine alkaloids, COA of Formula: C10H14N2O, the publication is Journal of the American Chemical Society (1980), 102(4), 1457-60, database is CAplus.

Starting with N,N-diethylbenzamides and aromatic aldehydes and proceeding via ortho lithiated intermediates, a one-pot synthesis of anthraquinones, e.g. I and II, was achieved. The scope and limitations of this tandem metalation sequence was explored for a variety of aromatic and heteroaromatic amides and aldehydes. The use of this reaction for the short syntheses of carcinogenic polycyclic aromatic hydrocarbons and antitumor ellipticine alkaloids, e.g. III was demonstrated.

Journal of the American Chemical Society published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C12H25Br, COA of Formula: C10H14N2O.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nasibullin, Igor published the artcileSynthetic prodrug design enables biocatalytic activation in mice to elicit tumor growth suppression, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Nature Communications (2022), 13(1), 39, database is CAplus and MEDLINE.

Considering the intrinsic toxicities of transition metals, their incorporation into drug therapies must operate at minimal amounts while ensuring adequate catalytic activity within complex biol. systems. As a way to address this issue, this study investigates the design of synthetic prodrugs that are not only tuned to be harmless, but can be robustly transformed in vivo to reach therapeutically relevant levels. To accomplish this, retrosynthetic prodrug design highlights the potential of naphthylcombretastatin-based prodrugs, which form highly active cytostatic agents via sequential ring-closing metathesis and aromatization. Structural adjustments will also be done to improve aspects related to catalytic reactivity, intrinsic bioactivity, and hydrolytic stability. The developed prodrug therapy is found to possess excellent anticancer activities in cell-based assays. Furthermore, in vivo activation by i.v. administered glycosylated artificial metalloenzymes can also induce significant reduction of implanted tumor growth in mice.

Nature Communications published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics