Recently, smart communities are heeded to in Japan as a solution to community issues. To properly evaluate the underlying concept, it is necessary to analyze smart cities in terms of local energy and ...environmental aspects, as well as disaster resilience. This research aimed to summarize the requirements for Japanese smart communities, and provide this information to municipalities, city planners, and regional developers in warmer climates, or countries where few precedents exist. Nine cases were reviewed in Japan, and four in Europe and the US to organize smart community requirements into three areas: environment, social, and safety-security. Additionally, bottom-up simulations were used to quantitatively evaluate the effects of energy technology introduction, emergency Life Continuity Plans (LCPs), and changes in energy performance owing to household compositional differences. The results showed that a typical Japanese smart community (containing Fuel cell, PV, and battery) has the capacity to become a positive energy district, generating 1916 GJ yr−1, and maintain power throughout a one-week power outage if shared within the community (save for the highest temperature week in August). Conversely, Japanese smart communities lacked consideration of residential diversity and creative landscapes.
Recently, various non-peptide corticotropin-releasing factor
1 (CRF
1) receptor antagonists have been reported. Structure–affinity relationships (SARs) of non-peptide CRF
1 antagonists suggest that ...such antagonists can be constructed of three units: a hydrophobic unit (Up-Area), a proton accepting unit (Central-Area), and an aromatic unit (Down-Area). We previously presented 4-aryl-1,2,3,6-tetrahydropyridinopyrimidine derivatives including potent CRF receptor ligands
1a and
1b and proposed that the 4-aryl-1,2,3,6-tetrahydropyridino moiety might be useful as a substituent in the Up-Area. Our interest shifted to 5-aryl-1,2,3,6-tetrahydropyridinopyrimidine derivatives
2, among which compound
2m (CRA0165) had highest affinity for CRF
1 receptors (IC
50=11
nM). We report here the design, synthesis and SARs of derivatives
2.
This paper describes the synthesis and structure–affinity relationships of 4-(5-aryl-1,2,3,6-tetrahydropyridino)pyrimidine derivatives as corticotropin-releasing factor
1 receptor antagonists.
Structure–affinity relationships (SARs) of non-peptide CRF
1 antagonists suggest that such antagonists can be constructed of three units: a hydrophobic unit (Up-Area), a proton accepting unit ...(Central-Area), and an aromatic unit (Down-Area). Recently, various non-peptide corticotropin-releasing factor
1 (CRF
1) receptor antagonists obtained by modification of the Central-Area have been reported. In contrast, we modified the Up-Area and presented 4- or 5-aryl-1,2,3,6-tetrahydropyridinopyrimidine derivatives including potent CRF receptor ligands
1a–
c, and proposed that the 4- or 5-aryl-1,2,3,6-tetrahydropyridino moiety might be useful as a substituent in the Up-Area. Our interest shifted to the chemical modification in which the pyrimidine ring of
1a–
c was replaced by other heterocycles, purine ring of
2, 3
H-1,2,3-triazolo4,5-
dpyrimidine ring of
3, purin-8-one ring of
4 and 7
H-pyrrolo2,3-
dpyrimidine ring of
5. Among them, 5-aryl-1,2,3,6-tetrahydropyridinopurine compound
6j (CRA0186) had the highest affinity for CRF
1 receptors (IC
50=20
nM). We report here the synthesis and SARs of derivatives
6–
9.
This paper describes the synthesis and structure–affinity relationships of aryl-1,2,3,6-tetrahydropyridino-purine, -3
H-1,2,3-triazolo4,5-
dpyridine, -purin-8-one, and -7
H-pyrrolo2,3-
dpyrimidine derivatives (Y
1–Y
2: NC(H), NN, N(Me)–C(O) and C(Me)C(H or Me), respectively) as corticotropin-releasing factor
1 receptor antagonists.
