Category: thiazole

On June 7, 2018, Wunderlich, Winfried; Huber, Lukas A.; Leban, Johann Jakob; Pato, Janos; Oerfi, Laszlo; Frigyes, Waczek; Banhegyi, Peter; Sipos, Anna; Szantai-Kis, Csaba published a patent.Category: thiazole The title of the patent was Preparation of 3-amino-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-ones as cyclin dependent kinase inhibitors for the treatment and prophylaxis of cancer. And the patent contained the following:

The invention relates to preparation of pyrazolopyrimidinones of formulas I and II wherein X1 and X4 each independently H, halo, C1-6 alkoxy; X2 is H or halo; X3 is H, COOH, etc., as cyclin dependent kinase (CDK) inhibitors, pharmaceutical compositions comprising the same and the use thereof in particular in the prophylaxis and treatment of cancer and other proliferative diseases. Furthermore the invention relates to processes for the preparation of said 3-amino-pyrazolo[3,4d]pyrimidin-4-ones and intermediates to be used in the processes of the invention. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Category: thiazole

The Article related to pyrazolopyrimidinone preparation cdk inhibitor proliferative disease cancer treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Goswami, K. V.; Parajapati, S. N.; Goswami, T. K.; Chaudhari, H. D.; Parmar, Kokila A. published an article in 2019, the title of the article was Spectral and microbial screening of one-pot multicomponent synthesis of fused quinazolinone derivatives.Quality Control of 4-Phenylthiazol-2-amine And the article contains the following content:

Heterocyclic compounds containing 2-chloro-3-formyl pyridine and 2-amino thiazole quinqzolin-6(7H)-one I (R = H, Me, OMe; R1 = H, OMe, OH; R2 = H, Me) are reported to possess significant biol. activity. Synthesis of fused quinazolinone derivatives I have been described. The above synthesized compounds have been evaluated for their antimicrobial activity. Among the series containing some of the compounds showed promising results against standard drugs. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Quality Control of 4-Phenylthiazol-2-amine

The Article related to pyridinyl dihydro thiazoloquinazolinone preparation antibacterial antifungal activity, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-Phenylthiazol-2-amine

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 31, 2009, Muthuppalniappan, Meyyappan; Thomas, Abraham; Kumar, Sukeerthi; Margal, Sanjay; Khairatkar-Joshi, Neelima; Mukhopadhyay, Indranil; Gullapalli, Srinivas published a patent.Reference of 2-Amino-4-(4-iodophenyl)thiazole The title of the patent was Preparation of quinazolinedione derivatives as TRPA1 modulators. And the patent contained the following:

The title compounds I [ring A = (hetero)aryl, heterocyclyl, cycloalkyl; R1, R2 = H, OH, alkyl, etc.; R3, R4 = H, OH, halo, etc.; or R3 and R4 may be joined together to form (un)substituted 3-7 membered (un)saturated cyclic ring which may optionally include one or more heteroatom or group selected from O, S, C(O), S(O)0-2, (un)substituted NH; R5 = H, OH, alkyl, etc.; R6 = H, CN, NO2, etc.; n = 0-5], useful as TRPA (Transient Receptor Potential subfamily A) modulators for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1), were prepared E.g., a multi-step synthesis of II, starting from 2-amino-6-nitrobenzoic acid and urea, was given. Exemplified compounds I were screened for TRPA1 activity. For example, II showed 90.73% inhibition at 10.0 μM using the 45Calcium Uptake Assay. Also provided are processes for preparing compounds I, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Reference of 2-Amino-4-(4-iodophenyl)thiazole

The Article related to quinazolinedione preparation transient receptor potential channel trpa1 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 2-Amino-4-(4-iodophenyl)thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 31, 2021, Wang, Jie; Battini, Narsaiah; Ansari, Mohammad Fawad; Zhou, Cheng-He published an article.Related Products of 24295-03-2 The title of the article was Synthesis and Biological Evaluation of Quinazolonethiazoles as New Potential Conquerors towards Pseudomonas Aeruginosa. And the article contained the following:

Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi-step procedure from o-aminobenzoic acids and 2-acetylthiazole. A series of biol. evaluation showed that compound I [X = 7-Cl; R = O(CH2)5CH3] was the most effective quinazolonethiazole with superior activity to reference drugs chloramphenicol and norfloxacin. This active mol. displayed unobvious bacterial resistance against P. aeruginosa, the low toxicity to normal hepatocytes, suitable pharmacokinetics and drug-likeness. The preliminary biol. interaction suggested that quinazolonethiazole I [X = 7-Cl; R = O(CH2)5CH3] might induce bacterial death by disturbing the membrane permeability, while preventing bacteria from growth by integrating into DNA and binding with topoisomerase IV. These findings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug-resistant pathogens. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Related Products of 24295-03-2

The Article related to quinazolonethiazole preparation antibacterial antifungal sar mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 24295-03-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 31, 2020, Nizamuddin, N. D.; Abdul Ahad, Hindustan; Devanna, Nayakanti published an article.Application In Synthesis of 4-Phenylthiazol-2-amine The title of the article was Synthesis and molecular docking studies of some 1,2-dimethyl-3(4-substituted phenyl-1,3-thiazol-2-yl)2,3-dihydroquinazolin-4(1H)-ones as anticancer agents. And the article contained the following:

Synthesis of 1, 2-dimethyl-3(4-substituted phenyl-1,3-thiazol-2-yl)2,3-dihydro quinazolin-4(1H)-ones derivatives I [R = 4-Me, 2-OH, 4-Cl, etc.] was effected by refluxing 1,2-dimethylbenzoxazine-4-one with different 4-substituted phenyl-1,3-thiazol-2-amines. Synthesized compoundsI were characterized through elemental anal., IR, proton NMR, and Carbon-13 NMR. Mol. docking studies were carried out using Schrodinger Glide (version 2020_1) which was docked into selective P38alpha and Activin A Receptor Type 1 (ACVR1) Activin receptor-like kinase-2 (ALK2) kinase with Protein Data Bank (PDB) code 3GC7, 6GI6. Based on the docking score of synthesized quinazolin-4-one derivatives, I co-crystallized ligands interaction was evaluated with 5-fluorouracil (5-FU) as a reference drug. Compounds I [R = H, 4-MeO, 3-NH2, 2,4-OH] with P38alpha, I [R = 2-OH, 3-NH2, 4-Cl, 2,4-OH] with ACVR1 (ALK2) kinase score were -7.265, -7.078, -7.058 and -6.836; -8.929, -8.749, -8.735 and -8.464 Kcal/mol against enzymes responsible for cancer treatment. The results indicated that quinazolin-4-one derivatives I scored better than ligand and 5-FU. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application In Synthesis of 4-Phenylthiazol-2-amine

The Article related to dimethyl phenyl thiazolyl dihydroquinazolinone preparation mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 4-Phenylthiazol-2-amine

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 16, 2014, Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar published a patent.Application of 1092942-42-1 The title of the patent was Preparation of tetrahydroquinazolinone derivatives as PARP inhibitors for treating cancer. And the patent contained the following:

Disclosed are compounds of formula I, their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, (wherein M is C, CH, and N, and the dotted bond is either a single or double bond with provisos; R1 is H and (un)substituted alkyl; R2 and R3 together with the carbon atom(s) to which they are attached form a (un)substituted carbocycle; each R4 is halogen, cyano, (un)substituted alkyl, etc.; R5 and R6 are independently H, halogen, (un)substituted alkyl, etc., or R5 and R6 together constitute oxo or form part of an (un)substituted carbocycle; R7a, R8a, R7b R8b, R7c, R8c, R7d, and R8d are independently H, halogen, (un)substituted alkyl, etc., or any two form oxo or form part of an (un)substituted carbocycle or (un)substituted heterocycle, thereby making ring A either a spiro-bicycle or a fused-bicycle or a bridged-bicycle; Ar is (un)substituted aryl or (un)substituted heteroaryl; p = 0-3; and n = 1-4), pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject. I can also be used to sensitize a patient that has developed a resistance to other chemotherapeutics. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from intermediates Et 6-oxospiro[2.5]octane-5-carboxylate and 4-(4-(4-chlorophenyl)piperazin-1-yl)butanimidamide, had a PARP 1 inhibition IC50 between 1 nM and 500 nM. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application of 1092942-42-1

The Article related to tetrahydroquinazolinone derivative parp inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Shaikh, Asif R.; Patel, Navin B.; Rajani, Dhanji published an article in 2014, the title of the article was Antimycobacterial and antimicrobial studies of newly synthesized 3-(4-(6-methylbenzo[d]thiazol-2-yl) phenyl)quinazolin-4(3H)-ones.HPLC of Formula: 92-36-4 And the article contains the following content:

The 7-chloro-2-(substituted)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) quinazolin-4(3H)-ones e.g., I (R = furan-2-yl) have been prepared from the substituted acids, which were converted to substituted acetyl chlorides and cyclized with 4-chloro anthranilic acid afforded substituted benzoxazines 4(3H)-ones e.g., II and its further reaction with 4-(6-methylbenzo[d]thiazol-2-yl)aniline a gives desired compounds I. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H37Rv strain using Lowenstein-Jensen medium (conventional method) and antimicrobial activity against various bacteria and fungi using broth microdilution method. The compounds II, I were emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. The compounds II, I showed better antitubercular activities compared to rifampicin and isoniazid. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to quinazolinone preparation antibacterial antifungal antitubercular, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 26, 2017, Mai, Xi; Feng, Lihua; Liao, Yijing; Xu, Zhaoxing published a patent.SDS of cas: 64987-16-2 The title of the patent was Purine hydroxamic acid derivative and its preparation method and application in preparing drug for treating histone deacetylases mediated disease. And the patent contained the following:

The title purine hydroxamic acid derivative has structural formula I, wherein R1 is H or Me; R2 is H, halogen, alkyl, alkoxyl, alkylamino, hydroxyl, cyano or nitro. The derivative and its pharmaceutical composition can be used in preparing drug for treating histone deacetylases mediated disease, and has obvious inhibiting effect on histone deacetylases and anti-tumor activity. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).SDS of cas: 64987-16-2

The Article related to purine hydroxamic acid preparation histone deacetylase antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On April 9, 2020, Qiu, Yunguang; Huang, Lu; Fu, Jie; Han, Chenxia; Fang, Jing; Liao, Ping; Chen, Zhuo; Mo, Yiqing; Sun, Peihua; Liao, Daqing; Yang, Linghui; Wang, Jing; Zhang, Qiansen; Liu, Jin; Liu, Feng; Liu, Tingting; Huang, Wei; Yang, Huaiyu; Jiang, Ruotian published an article.Product Details of 92-36-4 The title of the article was TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation. And the article contained the following:

TWIK-related K+ (TREK) channels are potential analgesic targets. However, selective activators for TREK with both defined action mechanism and analgesic ability for chronic pain have been lacking. Here, we report (1S,3R)-3-((4-(6-methylbenzo[d]thiazol-2-yl)phenyl)carbamoyl)cyclopentane-1-carboxylic acid (C3001a), a selective activator for TREK, against other two-pore domain K+ (K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1, as suggested by computational modeling and exptl. anal. Furthermore, we identify the carboxyl group of C3001a as a structural determinant for binding to TREK-1/2 and the key residue that defines the subtype selectivity of C3001a. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mech. allodynia and inflammation. Together, C3001a represents a lead compound which could advance the rational design of peripherally acting analgesics targeting K2P channels without opioid-like adverse effects. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Product Details of 92-36-4

The Article related to trek channel activator preparation pain neuroinflammation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Product Details of 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On October 22, 2009, Hahn, Michael G.; Becker, Eva-Maria; Knorr, Andreas; Schneider, Dirk; Stasch, Johannes-Peter; Schlemmer, Karl-Heinz; Wunder, Frank; Stoll, Frederike; Heitmeier, Stefan; Muenter, Klaus; Griebenow, Nils; Lampe, Thomas; El Sheikh, Sherif; Li, Volkhart Min-Jian published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of phthalazinones as soluble guanylate cyclase inhibitors. And the patent contained the following:

Title compounds I [X = L1-M-L2CO2H; L1 = bond, methylene, etc.; M = phenylene, 5 or 6-membered heteroaryl with provisos; L2 = bond, methylene with provisos; A = 5-7 membered heterocycle ring with provisos; R1 = H, alkyl, cycloalkyl; R2 = H, halo, CN, etc.; R3 = alkyl, alkenyl, etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, NaOH/dioxane/H2O mediated saponification of ester II [Y = Me] afforded acid II [Y = H]. In soluble guanylate cyclase inhibition assays, 48-examples of compounds I exhibited MEC values ranging from 0.1-300 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to phthalazinone preparation soluble guanylate cyclase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.HPLC of Formula: 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica